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| Product | Description | |
|---|---|---|
| AKT Kinase Inhibitor | AKT Kinase Inhibitor is a Akt Kinase Inhibitor. Synonyms: 2-Propyn-1-ol, 3-[2-(4-amino-1,2,5-oxadiazol-3-yl)-7-(3-aminopropoxy)-1-ethyl-1H-imidazo[4,5-c]pyridin-4-yl]-. Grades: >98%. CAS No. 842148-40-7. Molecular formula: C16H19N7O3. Mole weight: 357.37. |  |
| AKT Kinase Inhibitor | AKT Kinase Inhibitor is an Akt kinase inhibitor with anti-tumor activity [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 842148-40-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg. Product ID: HY-10249A. |  |
| AKT Kinase Inhibitor hydrochloride | AKT Kinase Inhibitor hydrochloride is an Akt kinase inhibitor with anti-tumor activity [1]. AKT Kinase Inhibitor (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. Uses: Scientific research. Group: Signaling pathways. CAS No. 3026697-00-4. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-10249D. | |
| Akt1/2 kinase inhibitor | ?98% (HPLC). Group: Fluorescence/luminescence spectroscopy. |  |
| 10-DEBC hydrochloride | 10-DEBC hydrochloride is a selective and reversible Akt/PKB inhibitor suppressing the IGF-1-stimulated phosphorylation and activation of Akt (complete inhibition at 2.5 μM), and inhibiting downstream activation of mTOR, p70 S6 kinase and S6 ribosomal protein. 10-DEBC hydrochloride inhibits cell growth (IC50 ~ 2-6 μM) and leads to apoptosis in rhabdomyosarcoma cells. Synonyms: 10H-Phenoxazine-10-butanamine, 2-chloro-N,N-diethyl-, hydrochloride (1:1); Akt Inhibitor X; 2-Chloro-N,N-diethyl-10H-phenoxazine-10-butanamine hydrochloride; 10-[4'-(N,N-Diethylamino)butyl]-2-chlorophenoxazine hydrochloride; 4-(2-chloro-10H-phenoxazin-10-yl)-N,N-diethylbutan-1-amine hydrochloride. Grades: ≥99% by HPLC. CAS No. 925681-41-0. Molecular formula: C20H25N2OCl.HCl. Mole weight: 381.34. | |
| 10-DEBC hydrochloride | Selective inhibitor of Akt/PKB. Inhibits IGF-1-stimulated phosphorylation and activation of Akt (complete inhibition at 2.5uM), suppressing downstream activation of mTOR, p70 S6 kinase and S6 ribosomal protein. Shows no activity at PDK1, SGK1 or PI 3-kinase. Inhibits cell growth (IC50 ~ 2-6uM) and induces apoptosis in rhabdomyosarcoma cells. Group: Biochemicals. Grades: Highly Purified. CAS No. 925681-41-0. Pack Sizes: 10mg, 50mg. Molecular Formula: C20H25N2OCl.HCl, Method for Determining. US Biological Life Sciences. |  Worldwide |
| 2-Bromo-6-chloro-3-pyridinamine | 2-Bromo-6-chloro-3-pyridinamine is a reactant used in the synthesis of kilogram quantities of an akt Kinase inhibitor. It is mainly used as starting material for the production of many pharmaceutical compounds. Group: Biochemicals. Grades: Highly Purified. CAS No. 1050501-88-6. Pack Sizes: 1g, 5g. Molecular Formula: C5H4BrClN2, Molecular Weight: 207.46. US Biological Life Sciences. | Worldwide |
| 6H-Indeno[1,2-e]tetrazolo[1,5-b][1,2,4]triazin-6-one | KP372-1 is a specific Akt inhibitor that demonstrates at least 10-fold selectivity against a panel of additional kinase targets, including CDK1, ERK1, GSK3β, LCK, MEK1, PKA, PKC, and S6K. It blocks Akt signalling through the PI3K pathway, and inhibits cell proliferation while inducing apoptosis of thyroid cancer cells. Synonyms: 6H-Indeno[1,2-e]tetrazolo[1,5-b][1,2,4]triazin-6-one. Grades: ≥95%. CAS No. 1374996-60-7. Molecular formula: C20H8N12O2. Mole weight: 448.4. | |
| A-443654 | A-443654 is a potent small-molecule inhibitor of all three Akt serine/threonine kinases, induces Akt Ser-473 phosphorylation in all human cancer cell lines tested, including PTEN- and TSC2-deficient lines. It inhibits Akt-dependent signal transduction in cells and in vivo in a dose-responsive manner. Synonyms: A443564; A-443564; A 443564. Grades: >98%. CAS No. 552325-16-3. Molecular formula: C24H23N5O. Mole weight: 397.47. | |
| A-674563 | Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBalpha, beta, gamma) modulate cell proliferation, metabolism, and survival, as well as angiogenesis. A-674563 is an orally available, ATP-competitive, and reversible inhibitor of Akt (Ki =11nM for Akt1). It shows inhibitory activity against PKA and Cdk2 with IC50 values of 16 and 46 nM, respectively, but is 10- to >1,800-fold selective for Akt1 versus additional kinases in the CMGC, CAMK, and TK families. A-674563 reduces phosphorylation of Akt downstream targets in cells and slows proliferation of tumor cells in vitro with an EC50 value of 0.4uM.1 In vivo, 40mg/kg/day A-674563 in combination with 15mg/kg/day paclitaxel was shown to decrease tumor growth in a PC-3 prostate cancer mouse xenograft model. Group: Biochemicals. Alternative Names: (αS-[[[5-(3-methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]methyl]- benzeneethanamine). Grades: Highly Purified. CAS No. 552325-73-2. Pack Sizes: 500ug, 1mg, 5mg, 10mg. Molecular Formula: C22H22N4O. US Biological Life Sciences. | Worldwide |
| AAL-993 | AAL-993 is a VEGFR tyrosine kinase inhibitor that possesses dual inhibition of VEGFR signaling and HIF-1α expression through ERK inhibition without affecting Akt phosphorylation. Synonyms: AAL 993; AAL993; 2-((4-pyridyl)methyl)amino-N-(3-(trifluoromethyl)phenyl)benzamide. Grades: >98%. CAS No. 269390-77-4. Molecular formula: C20H16F3N3O. Mole weight: 371.36. | |
| Afuresertib | Afuresertib, also known as GSK2110183, is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor GSK2110183 binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents. Synonyms: GSK-2110183; GSK 2110183; GSK2110183; GSK-2110183B; GSK 2110183B; GSK2110183B; Afuresertib. CAS No. 1047644-62-1. Molecular formula: C18H17Cl2FN4OS. Mole weight: 427.32. | |
| Afuresertib | Afuresertib (GSK2110183) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with K i s of 0.08/2/2.6 nM for Akt1/Akt2/Akt3, respectively [1] [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: GSK2110183; LAE002. CAS No. 1047644-62-1. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-15727. | |
| Afuresertib hydrochloride | Afuresertib hydrochloride (GSK 2110183 hydrochloride) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with K i s of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively [1] [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: GSK2110183 hydrochloride; LAE002 hydrochloride. CAS No. 1047645-82-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-15727A. | |
| Akt1 and Akt2-IN-1 | Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 and Akt2 with the IC50 of 3.5 nM and 42 nM respectively. It has potent and balanced activity. It is dependent on the PH-domain for Akt inhibition. It is selective for Akt1/2 over Akt3 and is highly selective over other members of the AGC family of kinases in vitro. It has potent inhibitory activity against Akt1 and Akt 2 in vivo in a mouse lung and efficacy in a tumor xenograft model. It has moderate activity in an hERG binding assay and is a substrate for human P-glycoprotein. It also shows good physical properties with a human plasma protein binding. Uses: Akt1 and akt2-in-1 has potent inhibitory activity against akt1 and akt 2 and efficacy in a tumor xenograft model. Synonyms: Akt Inhibitor 17; Akti_2008; Akti 2008; Akti2008; Akti-2008; Akt Inhibitor 17; Akt-Inhibitor-17; AktInhibitor17; 3-Phenyl-2-[4-[[4-[5-(2-pyridinyl)-1H-1,2,4-triazol-3-yl]-1-piperidinyl]methyl]phenyl]-1,6-Naphthyridin-5(6H)-one;Akti_2008;3-phenyl-2-[4-[[4-(3-pyridin-2-yl-1H-1,2,4-triazol-5-yl)piperidin-1-yl]methyl]phenyl]-6H-1,6-naphthyridin-5-one. Grades: >98%. CAS No. 893422-47-4. Molecular formula: C33H29N7O. Mole weight: 539.63. | |
| Akt Inhibitor, Isozyme-selective (1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one; Akti-1/2) | Cell-permeable. A potent and selective inhibitor of Akt1/Akt2 activity (IC?? = 58nM (Akt1), 210nM (Akt2) and 2.12uM (Akt3) in in vitro kinase assays). The inhibition appears to be pleckstrin homology (PH) domain-dependent. It does not exhibit any inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations (50uM). Group: Biochemicals. Grades: Highly Purified. CAS No. 612847-09-3. Pack Sizes: 1mg. US Biological Life Sciences. | Worldwide |
| AKT inhibitor VIII | Akt Inhibitor VIII is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity. It does not exhibit any inhibitory effect against pleckstrin homology (PH) domain-lacking Akts, AGC family kinases, PKA, PKC or SGK. It also prevails over Akt1/Akt2-mediated resistance to chemotherapeutics in tumor cells and has been shown to block basal and stimulated phosphorylation/activation of Akt1/Akt2 in cultured cells and in mice. Synonyms: AKT inhibitor VIII; AKT-inhibitor-VIII; AKT inhibitor-8; AKT-inhibitor-8; Akt-I 1,2; Akti-1/2. Sigma-A6730. 2H-Benzimidazol-2-one, 1,3-dihydro-1-[1-[[4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl]methyl]-4-piperidinyl]-. Grades: >98%. CAS No. 612847-09-3. Molecular formula: C34H29N7O. Mole weight: 551.64. | |
| Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 (1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one, Akti-1/2) | A cell-permeable, reversible, potent, and selective inhibitor of Akt1/Akt2 activity (IC50=58nM, 210nM, and 2.12uM for Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays). The inhibition is reported to be pleckstrin homology (PH) domain-dependent. It does not exhibit any inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50uM. Overcomes Akt1/Akt2-mediated resistance to chemotherapeutics in tumor cells and is shown to block basal and stimulated phosphorylation / activation of Akt1/Akt2 both in cultured cells in vitro and in mice in vivo. Group: Biochemicals. Grades: Highly Purified. CAS No. 612847-09-3. Pack Sizes: 1mg, 5mg. US Biological Life Sciences. | Worldwide |
| Akt Inhibitor XVI, AT7867 (p70S6K Inhibitor III, 4-(4-Chlorophenyl)-4-(4-(1H-pyrazol-4-yl)-phenyl)-piperidine, PKA Inhibitor XIV, Chlorophenyl-pyrazolyl-phenyl-piperidine, S6K1 Inhibitor III) | A cell-permeable pyrazolo compound that acts as a potent inhibitor against Akt (IC50 = 32, 17, and 47nM against Akt1, Akt2, and Akt3, respectively), PKA (IC50 = 20nM), and p70S6K (IC50 = 85nM) in an ATP-competitive manner (Ki = 18nM using AKT2), with much reduced potency toward RSK1 (IC50 >100nM) and a panel of 13 other cellular kinases (IC50 >1uM). Shown to reduce cellular phosphorylation of GSK-3beta (IC50 range from 2.08 to 4.45uM), S6R, FKHRL1, and inhibit the proliferation of cancer cells exhibiting constitutive Akt pathway activation both in vitro (IC50 range from 0.94 to 11.86uM) and in mice in vivo (20mg/kg via i.p. or 90mg/kg via p.o.). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??ClN?. US Biological Life Sciences. | Worldwide |
| Alisertib | Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor ( IC 50 =1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity [1] [2] [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: MLN 8237. CAS No. 1028486-01-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg; 200 mg; 500 mg. Product ID: HY-10971. | |
| Alpelisib, Free Base, 99+% | Alpelisib, also known as BYL719, is a potent and selective phosphatidylinositol-3 kinase [alpha] inhibitor. It inhibited P110[alpha], p110[beta], p110[delta], and p110[gamma] with IC50 values of 5 nM, 1.2 µM, 0.29 µM and 0.25 µM, respectively, in biochemical assays. It inhibited the Akt phosphorylation with IC50 values of 74 nM in Rat1-myr-p110[alpha] cells, 2.2 µM in Rat1-myr-p110[beta] cells, and 1.2 µM in Rat1-myr-p110[delta] cells. Furet P., et al. "Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation." Bioorg. Med. Chem. Lett. 23: 3741-3748 (2013). Group: Biochemicals. Alternative Names: BYL-719; NVP-BYL719; (S)-Pyrrolidine-1,2-dicarboxylic Acid 2-Amide 1-[4-Methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-pyridin-4-yl]thiazol-2-yl]amide; (2S) -N1- [4- methyl -5- [2- (2, 2, 2-tri fluoro -1, 1-di methyl ethyl ) -4-pyridinyl ] -2-thiazoly l ] -1, 2-pyrrolidinedicarboxami de . Grades: Highly Purified. CAS No. 1217486-61-7. Pack Sizes: 5mg, 10mg, 25mg, 50mg, 100mg. Molecular Formula: C19H22F3N5O2S, Molecular Weight: 441.47. US Biological Life Sciences. | Worldwide |
| API-1 | Akt/protein kinase B (PKB) inhibitor. Binds the pleckstrin homology domain of Akt and blocks Akt membrane translocation. Inhibits EGF-induced kinase activity of Akt1, Akt2 and Akt3. Induces cell growt h arrest and apoptosis in human cancer cells expressing constitutively active Akt. Synonyms: API 1; API1; NSC177233; NSC 177233; NSC-177233; 4-Amino-5,6,7,8-tetrahydro-5-oxo-8-(beta-D-ribofuranosyl)pyrido[2,3-d]pyrimidine-6-carboxamide. Grades: >98%. CAS No. 36707-00-3. Molecular formula: C28H30FN5O2. Mole weight: 337.29. | |
| AT13148 | AT13148 is an orally active and ATP-competitive, multi- AGC kinase inhibitor with IC 50 s of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Uses: Scientific research. Group: Signaling pathways. CAS No. 1056901-62-2. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-16071. | |
| AT13148 | AT13148 is an orally available multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity. It can block phosphorylation of AKT, p70S6K, PKA, ROCK and SGK substrates, and induce apoptosis in cancer cells. Synonyms: AT-13148; (1S)-2-amino-1-(4-chlorophenyl)-1-[4-(1H-pyrazol-4-yl)phenyl]ethanol. Grades: >98%. CAS No. 1056901-62-2. Molecular formula: C17H16ClN3O. Mole weight: 313.78. | |
| AT7867 | AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively; little activity outside the AGC kinase family. Synonyms: AMG-706; AMG 706; AMG706; AT7867; AT 7867; AT-7867. Grades: >98%. CAS No. 857531-00-1. Molecular formula: C20H20ClN3. Mole weight: 337.85. | |
| AZD-5363 | AZD-5363 is an orally available inhibitor of the serine/threonine protein kinase AKT (protein kinase B) with potential antineoplastic activity. AZD-5363 binds to and inhibits all AKT isoforms. This agent may be used as monotherapy or combination therapy for a variety of human cancers. Synonyms: AZD5363; AZD 5363; Capivasertib. Grades: 98%. CAS No. 1143532-39-1. Molecular formula: C21H25ClN6O2. Mole weight: 428.9152. | |
| AZD8055 | A potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM. It inhibits the phosphorylation of mTORC1 substrates p70S6K and 4E-BP1 as well as phosphorylation of the mTORC2 substrate AKT and downstream proteins. The rapamycin-resistant T37/46 phosphorylation sites on 4E-BP1 were fully inhibited by AZD8055, resulting in significant inhibition of cap-dependent translation. In vitro, AZD8055 potently inhibits proliferation and induces autophagy in H838 and A549 cells. In vivo, AZD8055 induces a dose-dependent pharmacodynamic effect on phosphorylated S6 and phosphorylated AKT at plasma concentrations leading to tumor growth inhibition. Group: Biochemicals. Alternative Names: 5- [2, 4-Bis [ (3S) -3-methyl-4-morpholinyl] pyrido [2, 3-d] pyrimidin-7-yl] -2-methoxy Benzene methanol; [5-[2,4-Bis((3S)-3-methylmorpholin-4-yl)pyrido[2,3-d]pyrimidin-7-yl]- 2-methoxyphenyl] methanol; AZD 8055; [5- [2, 4-Bis ( (3S) -3-methylmorpholin-4-yl) pyrido [5, 6-e] pyrimidin-7-yl] -2-methoxyphenyl] methanol. Grades: Purified. CAS No. 1009298-09-2. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
| Bemcentinib | Bemcentinib is a selective small molecule inhibitor of Axl kinase, which showed activity to blocks tumor spread and prolongs survival in models of metastatic breast cancer. The receptor tyrosine kinase Axl may play an important role in cancer progression, invasion, metastasis, drug resistance, and patient mortality. R428 inhibits Axl with low nanomolar activity and blocked Axl-dependent events, including Akt phosphorylation, breast cancer cell invasion, and proinflammatory cytokine production. Pharmacologic investigations revealed favorable exposure after oral administration such that R428-treated tumors displayed a dose-dependent reduction in expression of the cytokine granulocyte macrophage colony-stimulating factor and the epithelial-mesenchymal transition transcriptional regulator Snail. In support of an earlier study, R428 inhibited angiogenesis in corneal micropocket and tumor models. R428 administration reduced metastatic burden and extended survival in MDA-MB-231 intracardiac and 4T1 orthotopic (median survival, >80 days compared with 52 days; P < 0.05) mouse models of breast cancer metastasis. Additionally, R428 synergized with cisplatin to enhance suppression of liver micrometastasis. Our results show that Axl signaling regulates breast cancer metastasis at multiple levels in tumor cells and tumor stromal cells and that selective Axl blockade confers therapeutic value in prolonging survival of animals bearing metastatic tumors. Synonyms: BGB324; BGB-324; BGB 324; R 428; R-428; R428; 1-(6,7-dihydro-5H-benzo[2,3]cyclohepta[2,4-d]pyridazin-3-yl)-3-N-[(7S)-7-pyrrolidin-1-yl-6,7,8,9-tetrahydro-5H-benzo[7]annulen-3-yl]-1,2,4-triazole-3,5-diamine. CAS No. 1037624-75-1. Molecular formula: C30H34N8. Mole weight: 506.658. | |
| Butein | Butein is a cAMP-specific PDE inhibitor with an IC 50 of 10.4 μM for PDE4 [1]. Butein is a specific protein tyrosine kinase inhibitor with IC 50 s of 16 and 65 μM for EGFR and p60 c-src in HepG2 cells [2]. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a [3]. Butein is a SIRT1 activator (STAC). Uses: Scientific research. Group: Natural products. Alternative Names: 2,3,4,4-tetrahydroxy Chalcone. CAS No. 487-52-5. Pack Sizes: 10 mM * 1 mL; 2 mg; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-16558. | |
| CaMKII Inhibitor XII (Ca2+/Calmodulin-Dependent Protein Kinase II Inhibitor XII) | A pyrimidinyl sulfonamide compound that acts as a potent, reversible and CaM non-competitive inhibitor of CaMKII activities (IC50 = 0.063uM) with excellent selectivity over several kinases (IC50 = >60, 36, 11, 30 and 21uM for CaMKIV, MLCK, p38alpha, Akt1 and PKC, respectively). Shown to exhibit ~25-fold greater potency towards CaMKII than the CaM-competitive inhibitor KN-93. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. US Biological Life Sciences. | Worldwide |
| Capivasertib | Capivasertib (AZD5363) is an orally active and potent pan-AKT kinase inhibitor with IC 50 of 3, 7 and 7 nM for Akt1 , Akt2 and Akt3 , respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: AZD5363. CAS No. 1143532-39-1. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg; 500 mg; 1 g. Product ID: HY-15431. | |
| Capmatinib | Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor ( IC 50 =0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase [1] [2] [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: INC280; INCB28060. CAS No. 1029712-80-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg; 200 mg. Product ID: HY-13404. | |
| Capmatinib dihydrochloride hydrate | Capmatinib (INC280; INCB28060) dihydrochloride hydrate is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor ( IC 50 =0.13 nM). Capmatinib dihydrochloride hydrate can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride hydrate potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride hydrate is largely metabolized by CYP3A4 and aldehyde oxidase [1] [2] [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: INC280 dihydrochloride hydrate; INCB-28060 dihydrochloride hydrate. CAS No. 1865733-40-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-13404C. | |
| Capmatinib hydrochloride | Capmatinib (INC280; INCB28060) hydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor ( IC 50 =0.13 nM). Capmatinib hydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib hydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib hydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase [1] [2] [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: INC280 hydrochloride; INCB-28060 hydrochloride. CAS No. 1029714-89-3. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-13404B. | |
| CAY10567 | AKT1 is one of 3 closely related serine/threonine-protein kinases (AKT1, AKT2 and AKT3) called the AKT kinase, which regulate many processes including metabolism, proliferation, cell survival, growth and angiogenesis. CAY10567 is an AKT1 translocation inhibitor. It can prevent the translocation of AKT1 by apparently compromising the function of the PH domain. CAY10567 also inhibits hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (RdRp) with an IC50 value of 79 μM. Synonyms: BML-257. Grades: ≥98%. CAS No. 32387-96-5. Molecular formula: C21H14N2O2. Mole weight: 326.4. | |
| CTX-0294885 | CTX-0294885 is a novel broad-spectrum kinase inhibitor. CTx-0294885 exhibits inhibitory activity against a broad range of kinases in vitro. Use of a quantitative proteomics approach confirmed the selectivity of CTx-0294885-bound beads for kinase enrichment. Large-scale CTx-0294885-based affinity purification followed by LC-MS/MS led to the identification of 235 protein kinases from MDA-MB-231 cells, including all members of the AKT family that had not been previously detected by other broad-spectrum kinase inhibitors. CTx-0294885 represents a powerful new reagent for analysis of kinome signaling networks that may facilitate development of targeted therapeutic strategies. Synonyms: CTX-0294885; CTX 0294885; CTX0294885; CTx 0294885. Grades: 98%. CAS No. 1439934-41-4. Molecular formula: C22H24ClN7O. Mole weight: 437.93. | |
| CUDC-907 | CUDC-907 is an orally bioavailable inhibitor of both phosphoinositide 3-kinase (PI3K) class I and pan histone deacetylase (HDAC) enzymes, with potential antineoplastic activity. Upon oral administration, CUDC-907 inhibits the activity of both PI3K class I isoforms and HDAC, thereby preventing the activation of the PI3K-AKT-mTOR signal transduction pathway that is often overactivated in many cancer cell types. This may prevent growth of PI3K and/or HDAC-expressing tumor cells. CUDC-907 shows an increased inhibition of tumor cell growth and induction of apoptosis when compared to inhibitors that target either PI3K or HDAC. Synonyms: CUDC907; CUDC 907; CUDC-907. CAS No. 1339928-25-4. Molecular formula: C23H24N8O4S. Mole weight: 508.557. | |
| CZ415 | CZ415 is a highly selective potent mTOR inhibitor with little activity on other lipid and protein kinases with efficacy in a collagen induced arthritis model and exhibits excellent cell permeability. In the issue, Bergamini et al., who has identified CZ415, confirmed with its extraordinary selectivity, drug-like properties and proven efficacy in vivo, CZ415 represents an ideal molecule for the pharmacological investigation of mTOR pathophysiological role in vivo. Assessed in dose response format from HEK293T cells after treatment with CZ415: 1. inhibition of S6RP (downstream of mTORC1) phosphorylation in HEK293T: IC50 = 14.5 nM; 2. inhibition of Akt (mTORC2 substrate) phosphorylation in HEK293T: IC50 = 14.8 nM; 3. inhibition of IFNγ release in stimulated human whole blood: IC50 = 226 nM. Synonyms: CZ415; CZ-415; CZ 415; (S)-1-(4-(7,7-dimethyl-4-(3-methylmorpholino)-6,6-dioxido-5,7-dihydrothieno[3,4-d]pyrimidin-2-yl)phenyl)-3-ethylurea. CAS No. 1429639-50-8. Molecular formula: C22H29N5O4S. Mole weight: 459.57. | |
| DC-120 | DC-120 is an ATP competitive AKT kinase inhibitor that suppressed proliferation and induced apoptosis in liver cancer cells both in vitro and in vivo. DC120 blocked the phosphorylation of downstream molecules in the AKT signal pathway in dose- and time-dependent manners both in vitro and in vivo. DC120 inhibits AKT activity in vitro with an EC(50) of 153 nM. DC120 at 20 mg/kg/day inhibited the CNE2 xenograft tumor growth with a treated group/control group ratio of 38.1%, accompanied by increasing terminal deoxynucleotidyl transferasedUTP nick-end labeling-positive cells in the tumor sample. Synonyms: DC-120; DC 120; DC120. Grades: 98%. CAS No. 1261080-40-3. Molecular formula: C18H18Cl2N6OS. Mole weight: 437.35. | |
| ETP 45658 | ETP 45658 is a PI 3-kinase inhibitor (IC50 = 22, 30, 129 and 710 nM for PI 3-Kα, PI 3-Kδ, PI 3-Kβ and PI 3-Kγ, respectively), and it also inhibits DNA-PK and mTOR (IC50 = 70.6 and 152 nM, respectively). ETP 45658 causes blockade of proliferation in multiple cancer cell lines in vitro and a decrease of Akt phosphorylation levels in vivo. Synonyms: ETP-45658; ETP 45658; ETP45658; 3-[1-Methyl-4-(4-morpholinyl)-1H-pyrazolo[3,4-d]pyrimidin-6-ylphenol. Grades: ≥98% by HPLC. CAS No. 1198357-79-7. Molecular formula: C16H17N5O2. Mole weight: 311.34. | |
| Focal Adhesion Kinase Inhibitor III (FAK Inhibitor III, N-(4-tert-Butylbenzyl)-1,5-dimethyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazin-8-amine-4,4-dioxide) | A cell-permeable pyrazolobenzothiazined ioxide compound that targets and locks FAK in its inactive conformation, resulting in preincubation time-dependent inhibition in kinase assays and FAK autophosphorylation in human prostate cancer PC3M-luc cells (IC50 = 7.1uM with 30 min inhibitor preincubation), while exhibiting little activity toward Akt1, Aurora B, HER2, MEK1, p38alpha, Pyk2, or Src even at concentrations as high as 10uM. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??N?O?S. US Biological Life Sciences. | Worldwide |
| GSK2334470 | GSK2334470 is a potent 3-phosphoinositide-dependent protein kinase (PDK1) inhibitor (IC50 ~ 10 nM), which does not suppress the activity of 93 other protein kinases including 13 AGC-kinases most related to PDK1 at 500-fold higher concentrations. GSK2334470 also inhibited T-loop phosphorylation and activation of Akt. GSK2334470 will be a useful tool for delineating the roles of PDK1 in biological processes. Synonyms: GSK2334470; GSK2334470; GSK2334470. Grades: 0.98. CAS No. 1227911-45-6. Molecular formula: C25H34N8O. Mole weight: 462.602. | |
| GSK-3beta Inhibitor XXVII, CESI (2-(3-chloro-4-hydroxyphenyl)-8-(1,1-dioxidoisothiazolidin-2-yl)-3-hydroxy-6-methyl-4H-chromen-4-one) | A cell-permeable, 3-hydroxychromone derived compound that acts as a selective and reversible inhibitor of GSK-3beta (IC50 < 100nM). Shown to increase phosphorylation at Ser9. Does not show any inhibitory effect on a panel of 15 other protein kinases, including AMPK and Akt. By blocking GSK-3beta activity, it acts as a positive regulator of b-catenin signaling. Does not affect the viability or the growth rate of 3T3-L1 preadipocytes, however, it significantly reduces their differentiation into adipocytes ( 50 to 100nM). Exerts anti-adipogenic activity by down-regulating C/EBPa and PPARg. Shown to reduce adipocyte size and diminish weight gain in diet-induced obese mice without affecting their daily food intake. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??ClNO?S, Primary Target: GSK3b. US Biological Life Sciences. | Worldwide |
| GSK-690693 | GSK690693 is a pan-AKT kinase inhibitor, is also an aminofurazan-derived inhibitor of Akt kinases with potential antineoplastic activity. Pan-AKT kinase inhibitor GSK-690693 binds to and inhibits Akt kinases 1, 2, and 3, which may result in the inhibition of protein phosphorylation events downstream from Akt kinases in the PI3K/Akt signaling pathway, and, subsequently, the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. In addition, this agent may inhibit other protein kinases including protein kinase C (PKC) and protein kinase A (PKA). As serine/threonine protein kinases which are involved in a number of biological processes, AKT kinases promote cell survival by inhibiting apoptosis and are required for glucose transport. Synonyms: GSK-690693; GSK690693. CAS No. 937174-76-0. Molecular formula: C21H27N7O3. Mole weight: 425.48418. | |
| Halicin | Halicin (SU3327) is a potent, selective and substrate-competitive JNK inhibitor with an IC 50 of 0.7 μM. Halicin also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC 50 of 239 nM. Halicin shows less active against p38α and Akt kinase [1] [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: SU3327. CAS No. 40045-50-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-107597. | |
| Hematein | Hematein is a oxidation product of hematoxylin acted as a dye [1]. Hematein is an allosteric casein kinase II inhibitor with an IC 50 of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells [2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 475-25-2. Pack Sizes: 10 mM * 1 mL; 500 mg; 1 g. Product ID: HY-119751. | |
| Hematein | Hematein is a oxidation product of hematoxylin acted as a dye. Hematein is an allosteric casein kinase II inhibitor with an IC50 of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells. Uses: Designed for use in research and industrial production. Product Category: Inhibitors. CAS No. 475-25-2. Molecular formula: C16H12O6. Mole weight: 300.26. Purity: 0.749. Product ID: ACM475252. Alfa Chemistry ISO 9001:2015 Certified. |  |
| ILK Inhibitor, Cpd 22 (N-methyl-3- (1- (4- (piperazin-1-yl) phenyl) -5- (4'- (trifluoromethyl) biphenyl-4-yl) -1H-pyrazol-3-yl) propanamide) | A cell-permeable, tri-substituted pyrazol compound that acts as a potent and specific integrin-linked kinase (ILK) inhibitor (IC50=600nM). Shown to have high in vitro anti-proliferative potency against prostrate and breast cancer cell lines (IC50=1 to 2.5uM) while sparing normal epithelial cells. Its effect on cancer cells have been attributed to induction of autophagy and apoptosis. Suppresses ILK-mediated phosphorylation of Akt at Ser473 site, thereby down-regulating the downstream targets, such as GSK-3b and myosin light chain. Also causes a transcriptional repression of the transcription factor Y-Box binding protein 1 (YB-1). Exhibits minimum toxicity in mouse model. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. Molecular Formula: C30H30F3N5O, Molecular Weight: 553.6. US Biological Life Sciences. | Worldwide |
| Indole-3-carbinol | Indole-3-carbinol is an inhibitor of cell growth via suppressing incorporation of [3H]thymidine, triggering G1 cell cycle arrest and downregulation of cyclin-dependent kinase 6 (CDK6) expression. It exhibits anticancer activity by inhibition of NF-κB and Akt signaling pathways. Nutritional supplement in health care products. Synonyms: 3-Indolemethanol; (1H-Indol-3-yl)methanol; Indole-3-methanol; Indol-3-yl-methanol; 3-Hydroxymethylindole; I3C; Indinol. Grades: 98%. CAS No. 700-06-1. Molecular formula: C9H9NO. Mole weight: 147.17. | |
| Ipatasertib | Ipatasertib, also known as GDC-0068 is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor GDC-0068 binds to and inhibits the activity of Akt in a non-ATP-competitive manner, which may result in the inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents. Uses: Antineoplastic agents. Synonyms: GDC-0068; GDC0068; GDC 0068; RG7440; RG-7440; RG 7440; Ipatasertib. CAS No. 1001264-89-6. Molecular formula: C24H32ClN5O2. Mole weight: 458.0. | |
| JNK Inhibitor XVI, JNK-IN-8 ( (E) -3- (4- (dimethylamino) but-2-enamido) -N- (3-methyl-4- ( (4- (pyridin-3-yl) pyrimidin-2-yl) amino) phenyl) benzamide) | A cell-permeable, selective, and irreversible type 2 inhibitor of c-Jun N-terminal kinases (JNK) (IC50=4.67nM, 18.7nM, 980pM for JNK1, JNK2, and JNK3, respectively). Forms a covalent adduct with the conserved cysteine residue (Cys116 in JNK1) and binds to JNK in an extended type 2 conformation. Blocks the phosphorylation of c-Jun in cells (EC50=486nM in HeLa cells; 338nM in A375 cells). Exhibits greater cellular specificity for JNK when compared to 40 other kinases screened using a cell-based assay. Shows weaker binding to KIT mutants (IC50=92nM for V559D and 56nM for T670I) and RIOK2 (120nM). Does not show any significant inhibitory activity against various other kinases, including ERK, p38, Akt, MSK, and RSK. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
| Ketohexokinase Inhibitor (N8-(Cyclopropylmethyl)-N4-(2-(methylthio)phenyl)-2-(1-piperazinyl)-pyrimido[5,4-d]pyrimidine-4,8-diamine, KHK Inhibitor) | An orally bioavailable pyrimidinopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of human hepatic KHK activity (KHK-C isoform; IC50=12nM in a transcreener ADP assay) and efficiently blocks fructose-1-phosphate secretion (IC50 ≤ 400nM in HepG2 cells). Displays ~50-fold lower potency towards metabolic kinases, namely, ribokinase, hexokinase and adenosine kinase, and minimal binding affinities to diverse receptors and ion-channels, and excellent selectivity among a panel of 31-kinases including Akt1, AMPK, CaMKI/II, InsR, IRAK4, PKA and PKCtheta (IC50 >> 10uM). Shown to minimally affect the activities of human cytochrome p450 isozymes (1A2, 2C19, 2D6, 2C9 and 3A4), and exhibit high volume of distribution and high rate of clearance in rats. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??N?S 2HCl. US Biological Life Sciences. | Worldwide |
| Ku-0063794 | KU-0063794 is an inhibitor of both mTORC1 and mTORC2 with an IC50 of approximately 10 nM, but does not suppress the activity of 76 other protein kinases or seven lipid kinases, including Class 1 PI3Ks (phosphoinositide 3-kinases) at 1000-fold higher concentrations. KU-0063794 is cell permeant, suppresses activation and hydrophobic motif phosphorylation of Akt, S6K and SGK, but not RSK (ribosomal S6 kinase), an AGC kinase not regulated by mTOR. It also inhibited phosphorylation of the T-loop Thr308 residue of Akt phosphorylated by PDK1 (3-phosphoinositide-dependent protein kinase-1). It does not affect Thr308 phosphorylation in fibroblasts lacking essential mTORC2 subunits. KU-0063794 also suppressed cell growth and induced a G1-cell-cycle arrest. KU-0063794 will be useful in delineating the physiological roles of mTOR and may have utility in treatment of cancers in which this pathway is inappropriately activated. Uses: Differentiation. Synonyms: KU0063794; KU-0063794; KU 0063794; Ku0063794; Ku 0063794; Ku-0063794; KU63794; KU 63794; KU-63794; [5-[2-[(2R,6S)-2,6-dimethylmorpholin-4-yl]-4-morpholin-4-ylpyrido[2,3-d]pyrimidin-7-yl]-2-methoxyphenyl]methanol. Grades: 0.98. CAS No. 938440-64-3. Molecular formula: C25H31N5O4. Mole weight: 465.554. | |
| KY-226 | KY-226 is a protein tyrosine phosphatase 1B (PTP1B) inhibitor that protects neurons from cerebral ischemic injury. KY-226 restores Akt (protein kinase B) phosphorylation and extracellular signal-regulated kinase (ERK) reduction in transient middle cerebral artery occlusion (tMCAO) damage. KY-226 protects BBB integrity by restoration of TJ proteins, an effect partly mediated by Akt/FoxO1 pathway activation. Uses: Designed for use in research and industrial production. Additional or Alternative Names: KY-226; KY 226; KY226. Product Category: Inhibitors. Appearance: Fluffy white solid powder. CAS No. 1621673-53-7. Molecular formula: C27H31NO3S2. Mole weight: 481.67. Purity: >97%. IUPACName: 4-(biphenyl-4-ylmethylsulfanylmethyl)-N-(hexane-1-sulfonyl)benzoylamide. Canonical SMILES: O=C(NS(=O)(CCCCCC)=O)C1=CC=C(CSCC2=CC=C(C3=CC=CC=C3)C=C2)C=C1. Product ID: ACM1621673537. Alfa Chemistry ISO 9001:2015 Certified. Categories: KY 2265. | |
| L-2286 | L-2286 is a novel PARP inhibitor. L-2286 exerted significant protective effect against ischemia-reperfusion-induced myocardial injury in both experimental models. More importantly, L-2286 facilitated the ischemia-reperfusion-induced activation of Akt, extracellular signal-regulated kinase, and p38-MAPK in both isolated hearts and in vivo cardiac injury. Synonyms: L 2286; L2286; 2-(2-piperidin-1-ylethylsulfanyl)-1H-quinazolin-4-one. Grades: 98%. CAS No. 684276-17-3. Molecular formula: C15H19N3OS. Mole weight: 289.40. | |
| Luteolin (3',4',5,7-Tetrahydroxyflavone, Luteolol, BRN 0292084, C.I. Natural Yellow 2, Digitoflavone, Flacitran, Flavopurpol, Daphneflavonol, Argemexitin) | Anticancer and antimetastatic. alpha-Glucosidase inhibitor. Topoisomerase I Inhibitor. Apoptosis inducer. Anti-inflammatory. 15-Lipoxygenase (15-LOX) inhibitor. IL-6 production inhibitor. Fatty acid synthase (FAS) inhibitor. Antioxidant. Free radical scavenger. Antiadipogenic. PPAR-y. inhibitor. Neuroprotective. Monoamine transporter activator. Inhibitor of phosphodiesterases 1-5 (PDE1-5). PKC(e) and Src kinase inhibitor. HDAC inhibitor. Autophagy modulator. Phosphatidylinositol 3-kinase (PI3K) / Akt signaling inhibitor. p90 ribosomal S6 kinase (RSK1/RSK2) kinase activity inhibitor. Group: Biochemicals. Grades: Highly Purified. CAS No. 491-70-3. Pack Sizes: 5mg, 25mg. Molecular Formula: C15H10O6. US Biological Life Sciences. | Worldwide |
| LY294002 | Potent, cell permeable, highly specific PI(3)K (phosphoinositide 3-kinase) inhibitor. Acts on the ATP-binding site of the enzyme. Antagonizes P-glycoprotein-mediated multidrug resistance. Blocks Akt phosphorylation. Pim-1 kinase inhibitor. Group: Biochemicals. Grades: Highly Purified. CAS No. 154447-36-6. Pack Sizes: 1mg, 5mg, 25mg. Molecular Formula: C19H17NO3. US Biological Life Sciences. | Worldwide |
| LY-333,531 hydrochloride | Isozyme selective inhibitor of protein kinase Cbeta (PKCbeta). PKCbetaI and PKCbetaII isozyme inhibitor. Amelioriates diabetic retinopathy, diabetic peripheral neuropathy and diabetic nephropathy. Anti-cancer and anti-angiogenic compound. Suppresses glucose-induced adhesion of human monocytes to endothelial cells. Suppresses ERK1/2 and Akt phosphorylation. Group: Biochemicals. Grades: Highly Purified. CAS No. 169939-93-9. Pack Sizes: 1mg, 5mg. Molecular Formula: C28H28N4O3 HCl. US Biological Life Sciences. | Worldwide |
| MBQ-167 | MBQ-167 is a dual Rac/Cdc42 inhibitor with IC50 values of 103 nM and 78 nM respectively, in metastatic breast cancer cells. It decreases Rac and Cdc42 downstream effector p21-activated kinase (PAK) signaling and the activity of STAT3, without affecting Rho, MAPK, or Akt activities. Synonyms: HY-112842; CS-0066907; 9-ethyl-3-(5-phenyltriazol-1-yl)carbazole. CAS No. 2097938-73-1. Molecular formula: C22H18N4. Mole weight: 338.41. | |
| Midostaurin | Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ , Syk , Flk-1 , Akt , PKA , c-Kit , c-Fgr , c-Src , FLT3 , PDFRβ and VEGFR1/2 with IC 50 s ranging from 22-500 nM [1] [2]. Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: PKC412; CGP 41251. CAS No. 120685-11-2. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-10230. | |
| Miransertib hydrochloride | Miransertib is an orally bioavailable and selective AKT pathway inhibitor that suppresses AKT1, 2, 3 isoforms. It binds to both the active and inactive forms of AKT. Miransertib inhibits PIK3CA/AKT1 mutant dependent kinase signaling and exhibits antitumor activity. Synonyms: Miransertib; ARQ 092 HCl; Miransertib HCl; 3-[3-[4-(1-aminocyclobutyl)phenyl]-5-phenylimidazo[4,5-b]pyridin-2-yl]pyridin-2-amine hydrochloride. CAS No. 1313883-00-9. Molecular formula: C27H25ClN6. Mole weight: 468.98. | |
| MK-2206 | MK-2206 is an allosteric inhibitor of Akt that prevents translocation of Akt to membranes. It is also an orally bioavailable allosteric inhibitor of the serine/threonine protein kinase Akt (protein kinase B). It binds to and inhibits the activity of Akt in a non-ATP competitive manner, which may result in the inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. It has potential antineoplastic activity. It exhibits anticancer chemotherapeutic activity in a variety of in vitro cancer models. It induces G1-phase cell cycle arrest in hepatocellular carcinoma cells, inhibits cell proliferation in non-small cell lung cancer cells, and inhibits proliferation in medullary thyroid cancer cells. It also inhibits tumor growth in animal models of nasopharyngeal cancer. It was developed by Merck Sharp & Dohme and in clinic phase 2 trials. Uses: Mk-2206 has potential antineoplastic activity. Synonyms: MK2206; MK 2206; MK-2206; 8-(4-(1-Aminocyclobutyl)phenyl)-9-phenyl-8,9-dihydro-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3(2H)-one;8-[4-(1-Aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one. Grades: 95%. CAS No. 1032349-93-1. Molecular formula: C25H21N5O. Mole weight: 407.47. | |
| MK-2206 hydrochloride | MK-2206 hydrochloride is the hydrochloride form of MK-2206, which is an allosteric inhibitor of Akt and an orally bioavailable allosteric inhibitor of the serine/threonine protein kinase Akt (protein kinase B). It has potential antineoplastic activity. It exhibits anticancer chemotherapeutic activity in a variety of in vitro cancer models. It inhibits tumor growth in animal models of nasopharyngeal cancer. Uses: Mk-2206 hydrochloride has potential antineoplastic activity. Synonyms: MK-2206 hydrochloride; MK 2206 hydrochloride; 8-[4-(1-Aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3-one hydrochloride;MK2206 hydrochloride. Grades: >98 %. CAS No. 1032349-77-1. Molecular formula: C25H22ClN5O. Mole weight: 443.93. | |
| MK-2461 | MK-2461 is a novel ATP-competitive multitargeted inhibitor of activated c-Met. MK-2461 inhibited in vitro phosphorylation of a peptide substrate recognized by wild-type or oncogenic c-Met kinases (N1100Y, Y1230C, Y1230H, Y1235D, and M1250T) with IC50 values of 0.4 to 2.5 nmol/L. In tumor cells, MK-2461 effectively suppressed constitutive or ligand-induced phosphorylation of the juxtamembrane domain and COOH-terminal docking site of c-Met, and its downstream signaling to the phosphoinositide 3-kinase-AKT and Ras-extracellular signal-regulated kinase pathways, without inhibiting autophosphorylation of the c-Met activation loop. In cell culture, MK-2461 inhibited hepatocyte growth factor/c-Met-dependent mitogenesis, migration, cell scatter, and tubulogenesis. In a murine xenograft model of c-Met-dependent gastric cancer, a well-tolerated oral regimen of MK-2461 administered at 100 mg/kg twice daily effectively suppressed c-Met signaling and tumor growth. Synonyms: MK 2461; MK2461; MK-2461. Grades: >98%. CAS No. 917879-39-1. Molecular formula: C24H25N5O5S. Mole weight: 495.554. | |
| MKC-1 | MKC-1 is an orally bioavailable, small-molecule, bisindolylmaleimide cell cycle inhibitor with potential antineoplastic activity. MKC-1 and its metabolites inhibit tubulin polymerization, blocking the formation of the mitotic spindle, which may result in cell cycle arrest at the G2/M phase and apoptosis. In addition, this agent has been shown to inhibit the activities of the oncogenic kinase Akt, the mTOR pathway, and importin-beta, a protein essential to the transport of other proteins from the cytosol into the nucleus. Synonyms: MKC1; MKC 1; R 440; Ro 317453; Ro-317453; Ro317453; 3-(1-methyl-1H-indol-3-yl)-4-(1-methyl-6-nitro-1H-indol-3-yl)-1H-pyrrole-2,5-dione. CAS No. 125313-92-0. Molecular formula: C22H16N4O4. Mole weight: 400.39. | |
| ML-9 | ML-9 is a myosin light chain kinase (MLCK) inhibitor. It enhances the anticancer activity of docetaxel and has potential application as an adjuvant to existing anticancer chemotherapy. It is used as an attractive tool for targeting autophagy in cancer therapy through dual inhibition of both the Akt pathway and the autophagy. Uses: Ml-9 has potential application as an adjuvant to existing anticancer chemotherapy. Synonyms: ML9; ML 9; 1H-1,4-Diazepine, 1-[(5-chloro-1-naphthalenyl)sulfonyl]hexahydro-. Grades: >98%. CAS No. 110448-31-2. Molecular formula: C15H17ClN2O2S. Mole weight: 324.82. | |
| ML-9 | ML-9 is a selective and potent inhibitor of Akt kinase , inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity [3]. ML-9 inhibits inhibits MLCK, PKA and PKC activity with K i values of 4, 32 and 54 μM, respectively [1]. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation [3]. Uses: Scientific research. Group: Signaling pathways. CAS No. 105637-50-1. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg; 250 mg. Product ID: HY-100932. | |
| Narazaciclib | Narazaciclib (ON123300), a strong and brain-penetrant [1] multi-kinase inhibitor, inhibits CDK4 ( IC 50 =3.9 nM), Ark5 ( IC 50 =5 nM), PDGFRβ ( IC 50 =26 nM), FGFR1 ( IC 50 =26 nM), RET ( IC 50 =9.2 nM), and FYN ( IC 50 =11 nM). Single agent Narazaciclib causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors [2]. Narazaciclib inhibits CDK6 with an IC 50 of 9.82 nM [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: ON123300. CAS No. 1357470-29-1. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-12624. | |
| Nimbolide | Nimbolide is a triterpene derived from the leaves and flowers of neem (Azadirachta indica). Nimbolide induces apoptosis through inactivation of NF-κB. Nimbolide inhibits CDK4/CDK6 kinase activity. Nimbolide suppresses the NF-κB, Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways. Uses: Designed for use in research and industrial production. Product Category: Inhibitors. Appearance: Powder. CAS No. 25990-37-8. Molecular formula: C27H30O7. Mole weight: 466.52. Purity: 0.98. IUPACName: methyl 2-[6-(furan-3-yl)-7,9,11,15-tetramethyl-12,16-dioxo-3,17-dioxapentacyclo[9.6.1.02,9.04,8.015,18]octadeca-7,13-dien-10-yl]acetate. Canonical SMILES: CC1=C2C(CC1C3=COC=C3)OC4C2(C(C5(C6C4OC(=O)C6(C=CC5=O)C)C)CC(=O)OC)C. Product ID: ACM25990378. Alfa Chemistry ISO 9001:2015 Certified. | |
| PF-AKT400 | PF-AKT400 is an APT competitor inhibitor of AKR kinase. This compound was first described as compound 42 in J. Med. Chem. 2010, 53, 4615-4622 by a group of Pfizer scientists. The paper describes the design and synthesis of novel, ATP-competitive Akt inhibitors from an elaborated 3-aminopyrrolidine scaffold. Key findings include the discovery of an initial lead that was modestly selective and medicinal chemistry optimization of that lead to provide more selective analogues. Analysis of the data suggested that highly lipophilic analogues would likely suffer from poor overall properties. Central to the discussion is the concept of optimization of lipophilic efficiency and the ability to balance overall druglike propeties with the careful control of lipophilicity in the lead series. Discovery of the nonracemic amide series and subsequent modification produced an advanced analogue that performed well in advanced preclinical assays, including xenograft tumor growth inhibition studies, and this analogue was nominated for clinical development. The compound has no official name, has molecule weight 400.43. We temporally call this compound as PF-AKT400. Synonyms: PF-AKT400; PFAKT400; Lig1; Lig-1; Lig 1; PF AKT400; AKT-0286; AKT 0286; AKT0286. CAS No. 1004990-28-6. Molecular formula: C20H22F2N6O. Mole weight: 400.43. | |
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