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Cdk1 inhibitor is a cell-permeable indolylmethylene-2-indolinone derivative that exhibits potent anti-proliferative properties with IC50 of 2 μM. Cdk1 inhibitor acts as a selective and ATP-competitive inhibitor of Cdk1/cyclin B with IC50 of 5.8 μM. It also inhibits Cdk5 with IC50 of 25 μM. Synonyms: Cyclin-dependent Kinase 1 Inhibitor. Grades: ≥95%. CAS No. 220749-41-7. Molecular formula: C17H11ClN2O. Mole weight: 294.7.
Cdk1 Inhibitor - CAS 220749-41-7
The Cdk1 Inhibitor, also referenced under CAS 220749-41-7, controls the biological activity of Cdk1. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy.
Cdk1 Inhibitor IV, RO-3306
RO-3306 is a cell-permeable, potent and ATP-competitive inhibitor of Cdk1 (Ki = 35 nM and 110 nM for Cdk1/B1 and Cdk1/A, respectively). Group: Fluorescence/luminescence spectroscopy.
CDK1/2 Inhibitor III
Cdk1/2 Inhibitor III is a selective inhibitor of Cdk1/2 with an IC50 of 2.1 μM for CDK1/cyclin B. It is a cell-permeable triazolo-diamine compound with anti-proliferative properties in various human cancer cells (IC50 = 20 nM, 35 nM and 92 nM in HCT-116, HeLa and A375 cells, respectively). Synonyms: Cyclin-dependent Kinase 1/2 Inhibitor III; 1H-1,2,4-Triazole-1-carbothioamide, 3-amino-5-[[4-(aminosulfonyl)phenyl]amino]-N-(2,6-difluorophenyl)-; 3-Amino-5-[[4-(aminosulfonyl)phenyl]amino]-N-(2,6-difluorophenyl)-1H-1,2,4-triazole-1-carbothioamide; 3-amino-N-(2,6-difluorophenyl)-5-((4-sulfamoylphenyl)amino)-1H-1,2,4-triazole-1-carbothioamide. Grades: >95%. CAS No. 443798-55-8. Molecular formula: C15H13F2N7O2S2. Mole weight: 425.44.
Cdk1/2 Inhibitor III - CAS 443798-55-8
The Cdk1/2 Inhibitor III, also referenced under CAS 443798-55-8, controls the biological activity of Cdk1/2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy.
Cdk1/2 Inhibitor II, NU6102 - CAS 444722-95-6
The Cdk1/2 Inhibitor II, NU6102, also referenced under CAS 444722-95-6, controls the biological activity of Cdk1/2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy.
Cdk1/5 Inhibitor - CAS 40254-90-8
The Cdk1/5 Inhibitor, also referenced under CAS 40254-90-8, controls the biological activity of Cdk1/5. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy.
InSolution Cdk1 Inhibitor IV, RO-3306
The Cdk1 Inhibitor IV, RO-3306 controls the biological activity of Cdk1. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy.
10Z-Hymenialdisine
10Z-Hymenialdisine is a pan kinase inhibitor (IC50 values are 6, 10, 22, 28, 35, 40, 70, 80, 100, 470, 500, 600, 700 and 700 nM for MEK1, GSK-3β, Cdk1/cyclin B, Cdk5/p25, CK1, Cdk2/cyclin A, Cdk2/cyclin E, ASK-γ, Cdk3/cyclin E, Erk1, PKCγ, Cdk4/cyclin D1, Cdk6/cyclin D2 and PKCα, respectively). 10Z-Hymenialdisine inhibits NF-κB activation and suppresses inflammatory gene expression. Synonyms: Hymenialdisine; (Z)-Hymenialdisine; 4-(2-amino-4-oxo-1H-imidazol-5(4H)-ylidene)-2-bromo-4,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8(1H)-one. Grades: ≥97% by HPLC. CAS No. 82005-12-7. Molecular formula: C11H10BrN5O2. Mole weight: 324.13.
10Z-Hymenialdisine
Insecticidal and cytotoxic. Potent NF-kappaB inhibitor. Inhibits various pro-inflammatory cytokines such as IL-1, IL-2, IL-6, IL-8, TNF-alpha and nitric oxide (NO) in a variety of cell lines. ATP-competitive kinase inhibitor. Inhibits DNA damage checkpoint at G2, cyclin-dependent kinases CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, CDK5/p25, GSK-3beta and casein kinase 1 (CK1). Potent mitogen-activated protein kinase kinase-1 (MEK-1) inhibitor. MARK (microtubule affinity-regulating kinase) inhibitor. Group: Biochemicals. Grades: Highly Purified. CAS No. 82005-12-7. Pack Sizes: 500ug, 1mg. Molecular Formula: C??H??BrN?O?, Method for Determining. US Biological Life Sciences.
Isolated from sponge Axinella carteri. A potent inhibitor of mitogen-activated protein kinase kinase-1 (MEK-1) (IC50=6nm). Blocks the in vivo phosphorylation of the microtubule-binding protein tau at sites that are hyperphosphorylated by glycogen synthase kinase-b (GSK-3b) and CDK5/p35 in Alzheimers disease. Inhibitor of DNA damage checkpoint at G2 phase (IC50=6uM), cyclin-dependent kinases CDK1/cyclin B (IC50=22nm), CDK2/cyclin A (IC50=70 nm), CDK2/cyclin E (IC50=40nm), CDK4/cyclin D1 (IC50 = 600nm), CDK5/p25 (IC50=28nm), GSK-3b (IC50=10nm), and casein kinase 1 (CK1) (IC50=35nm). Group: Biochemicals. Grades: Highly Purified. CAS No. 82005-12-7. Pack Sizes: 250ug, 1mg. US Biological Life Sciences.
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2-Amino-3-methoxybenzoic Acid
2-Amino-3-methoxybenzoic Acid is used in the preparation of CDK1/cyclin B inhibitors for application towards antitumor treatment. In addition, it is used in the synthesis of Alogliptin, an inhibitor of dipeptidy peptidase, which aids in the lowering of blood-glucose for potential treatment of diabetes. Group: Biochemicals. Alternative Names: 2-Amino-m-Anisic Acid; 2-Amino-3-(methyloxy)benzoic Acid; 2-Amino-3-methoxybenzoic Acid; 3-Methoxy-2-aminobenzoic Acid; 3-Methoxyanthranilic Acid; NSC 81443. Grades: Highly Purified. CAS No. 3177-80-8. Pack Sizes: 2.5g. US Biological Life Sciences.
(2S,3S,4S,5S)-5-(4-benzamido-2-oxopyrimidin-1(2H)-yl)-2-((benzoyloxy)methyl)-4-fluoro-4-methyltetrahydrofuran-3-yl benzoate is a potential drug candidate used in biomedicine for treating cancer. It is a small molecule inhibitor of WEE1, a protein kinase that regulates the G2/M checkpoint of the cell cycle. Inhibition of WEE1 leads to the activation of CDK1 and CDK2, causing DNA damage and cell death in cancer cells. Synonyms: (2S,3S,4S,5S)-5-(4-benzoylamino-2-oxopyrimidine-1(2H)-yl)-2-((benzoyloxy)methyl)-4-Fluoro-4-methyltetrahydrofuran-3-yl benzoate. Grades: 97%. Molecular formula: C31H26FN3O7. Mole weight: 571.55.
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.
AG-012986
AG-012986 is a multitargeted cyclin-dependent kinase (CDK) inhibitor active against CDK1, CDK2, CDK4/6, CDK5, and CDK9, with selectivity over a diverse panel of non-CDK kinases. AG-012986 showed antiproliferative activities in vitro with IC(50)s of <100 nmol/L in 14 of 18 tumor cell lines. In vivo, significant antitumor efficacy induced by AG-012986 was seen (tumor growth inhibition,>83.1%) in 10 of 11 human xenograft tumor models. AG-012986 also showed dose-dependent retinoblastoma Ser(795) hypophosphorylation, cell cycle arrest, decreased Ki-67 tumor staining, and apoptosis in conjunction with antitumor activity. Synonyms: AG 012986; AG012986; Benzamide, 4-((4-amino-5-(2,6-difluorobenzoyl)-2-thiazolyl)amino)-N-((1R)-2-(dimethylamino)-1-methylethyl)-. Grades: >98%. CAS No. 486414-35-1. Molecular formula: C22H23F2N5O2S. Mole weight: 459.51.
AG-024322
AG-24322 is a second generation CDK inhibitor. AG-024322 is a potent inhibitor of CDK1, CDK2, and CDK4 that produces cell-cycle arrest and antitumor activity in preclinical models. Synonyms: AG-24322; AG 24322; AG24322. Grades: 98%. CAS No. 837364-57-5. Molecular formula: C23H20F2N6. Mole weight: 418.44.
Aloisine A
Aloisine a is a cell-permeable pyrrolo-pyrazine compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of cyclin dependent kinases (Cdks: IC50 =150nM, 120 nM, 400 nM and 200 nM for Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p25, respectively). Uses: A potent and selective cdk and gsk-3 inhibitor. Synonyms: Aloisine A;4-(7-Butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl)phenol. Grades: ≥98%. CAS No. 496864-16-5. Molecular formula: C16H17N3O. Mole weight: 267.33.
Aloisine RP106
A cell-permeable pyrrolo-pyrazine compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of Cdk1/cyclin B, Cdk5/p35, and GSK-3 (IC50 = 700nM, 1.5 uM, and 920 nM, respectively). It is a derivative of the aloisines A and B, which competitively inhibit ATP binding to the catalytic subunit of CDKs and GSKs. Synonyms: RP106; 7-n-Butyl-6-(4-methoxyphenyl)-[5H]pyrrolo[2,3-b]pyrazine. Grades: ≥98%. CAS No. 496864-15-4. Molecular formula: C17H19N3O. Mole weight: 281.4.
Alsterpaullone
Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta with IC50s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders[1]. Alsterpaullone induces apoptosis in leukemia cell line[2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: 9-Nitropaullone; NSC 705701. CAS No. 237430-03-4. Pack Sizes: 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-108359.
Alsterpaullone
Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta with IC50s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders. Alsterpaullone induces apoptosis in leukemia cell line. Uses: Designed for use in research and industrial production. Product Category: Inhibitors. CAS No. 237430-03-4. Molecular formula: C16H11N3O3. Mole weight: 293.28. Purity: >95%. Product ID: ACM237430034. Alfa Chemistry ISO 9001:2015 Certified.
Alsterpaullone
Alsterpaullone is a potent glycogen synthase kinase-3 inhibitor and a potential therapeutic agent for the treatment of Parkinson disease. Alsterpaullone is also known as 9-Nitropaullone and NSC 705701, which is a derivative of kenpaullone and an ATP-competitive inhibitor of several cyclin-dependent kinases (CDKs) and glycogen synthase kinase 3β (GSK3β). Alsterpaullone induces apoptosis by activation of caspase-9 due to perturbation in mitochondrial membrane potential. Alsterpaullone is a derivative of kenpaullone with slightly improved potency over kenpaullone, alsterpaullone selectively inhibits Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p25, and GSK3α/β with IC50 values of 35, 15, 200, 40, and 4 nM, respectively. Synonyms: 9-Nitropaullone; NSC 705701; 7,12-Dihydro-9-nitro-indolo[3,2-d][1]benzazepin-6(5H)-one. Grades: ≥98%. CAS No. 237430-03-4. Molecular formula: C16H11N3O3. Mole weight: 293.3.
Alsterpaullone
Potent CDK1/cyclin B (IC50 = 35 nM) inhibitor. Anti-tumor compound Potent inhibitor of CDK2/cyclin A, CDK2/cyclin E (IC50 = 200 nM), CDK5/p25 (IC50 = 40 nM), CDK5/p35 (IC50 = 40 nM). GSK-3beta (glycogen synthase kinase-3beta) inhibitor. Apoptosis inhibitor. Apoptosis inducer. Angiogenesis inhibitor. Group: Biochemicals. Grades: Highly Purified. CAS No. 237430-03-4. Pack Sizes: 1mg, 5mg. Molecular Formula: C16H11N3O3. US Biological Life Sciences.
Worldwide
Alsterpaullone, 2-Cyanoethyl - CAS 852529-97-0
A cell-permeable and reversible Alsterpaullone derivative that acts as a highly potent, ATP-competitive, selective inhibitor of Cdk1/cyclin B and GSK-3?. Group: Fluorescence/luminescence spectroscopy.
Alsterpaullone - CAS 237430-03-4
A cell-permeable, potent, reversible, and ATP competitive inhibitor of GSK-3? (IC?? = 4 nM) and Cdk1/cyclin B (IC?? = 35 nM). Group: Fluorescence/luminescence spectroscopy.
Aminopurvalanol A
Aminopurvalanol A is a selective, cell-permeable, reversible and ATP-competitive cyclin-dependent kinase (CDK) inhibitor. It is a 2,6,9-trisubstituted purine analog that displays anti-mitotic as well as anti-tumor properties. It induces cell differentiation by preferentially targeting the G2/M-phase and acts intracellularly by inhibiting both Cdks and MAPKs. It potently inhibits Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk5/p35 with IC50s values of 33, 33, 28, and 20 nM, respectively. It also inhibits growth of ovarian leukemic (SR), (IGROV1), colonic (KM12) and lung (NCI-H522) cells in antiproliferative assays in vitro. Synonyms: (2R)-2-[[6-[(3-Amino-5-chlorophenyl)amino]-9-(1-methylethyl)-9H-purin-2-yl]amino]-3-methyl-1-butanol; NG-97; NG97; NG 97; Aminopurvalanol A; Aminopurvalanol-A. Grades: ≥98% by HPLC. CAS No. 220792-57-4. Molecular formula: C19H26ClN7O. Mole weight: 403.91.
Aminopurvalanol A (NG97, (2R)-2-[[6-[(3-Amino-5-chlorophenyl)amino]-9-(1-methylethyl)-9H-purin-2-yl]amino]-3-methyl-1-butanol)
A cell-permeable, reversible and competitive inhibitor of cyclin-dependent kinases. IC50 values are: CDK1/cyclin B (33nm), CDK2/cyclin A (33nm), CDK2/cyclin E (28nm) and CDK5/p35 (20nm). Group: Biochemicals. Grades: Highly Purified. CAS No. 220792-57-4. Pack Sizes: 1mg, 5mg . US Biological Life Sciences.
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AS2863619
AS2863619 enables conversion of antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 inhibition of CDK8/19, which consequently activates the Foxp3 gene[1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2241300-51-4. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-126675A.
Asnuciclib
Asnuciclib (CDKI-73; LS-007) is an orally active and highly efficacious CDK9 inhibitor, with Ki values of 4 nM, 4 nM and 3 nM for CDK9, CDK1 and CDK2, respectively. Asnuciclib down-regulates the RNAPII phosphorylation. Asnuciclib is also a novel pharmacological inhibitor of Rab11 cargo delivery and innate immune secretion[1][2][3][4]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: CDKI-73; LS-007. CAS No. 1421693-22-2. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-12445.
AT7519
AT7519 (AT7519M) as a potent inhibitor of CDKs , with IC 50 s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: AT7519M. CAS No. 844442-38-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-50940.
AT7519 Hydrochloride
AT7519 Hydrochloride is a potent inhibitor of CDKs , with IC 50 s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively. Uses: Scientific research. Group: Signaling pathways. CAS No. 902135-91-5. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-50943.
AT7519 TFA
AT7519 (AT7519M) TFA as a potent inhibitor of CDKs , with IC 50 s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: AT7519M TFA. CAS No. 1431697-85-6. Pack Sizes: 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-50940A.
A cell-permeable, pyrimidine derivative that acts as an ATP-competitive CDK Inhibitor (Ki=2.5uM for CDK1, and Ki=1.3uM for CDK2), and demonstrates cytostatic properties among a panel of 57 cancer cell lines. Also inhibits ATR kinase (IC50=6.7uM in MCF7 cells), but does not interfere with irradiation-induced autophosphorylation of DNA-PK or ATM. Potentiates a range of DNA-damaging cytotoxic drugs such as hydroxyurea (1.8-fold) and cisplatin (1.4-fold) at 10uM, but not the anti-mitotic paclitaxel. Attenuates G2/M arrest following DNA damage and inhibits RAD51 focus formation. Shown to be synthetically lethal when DNA single-strand break repair is impaired in PARP-inhibited cells. Group: Biochemicals. Grades: Highly Purified. CAS No. 220036-08-8. Pack Sizes: 10mg. US Biological Life Sciences.
A cell-permeable quinazoline compound that targets the ATP binding pocket and an adjacent cleft and acts as a potent and reversible inhibitor of Aurora A and Aurora B (IC50=110 and 130nM, respectively) with moderate to excellent selectivity among closely related 16-kinase panel (IC50=0.88, 1.03 and 1.79uM for Lck, Src and MEK1, respectively, and IC50>10uM for Cdk1/2/4, Plk1, Chk1). Blocks phosphorylation of Histone H3-Ser10 in Xenopus cycling egg extracts at 20uM, and reduces mitotic spindle assembly. Shown to repress kinetochore localization of BubR1, Cenp-E, and Mad2, and arrest the growth of proliferating tumor cells. Group: Biochemicals. Grades: Highly Purified. CAS No. 331771-20-1. Pack Sizes: 5mg. US Biological Life Sciences.
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Avotaciclib
Avotaciclib (BEY1107) is an orally active cyclin-dependent kinase 1 (CDK1) inhibitor. Avotaciclib can inhibit the proliferation and induce apoptosis of tumor cells. Avotaciclib can be used in the research of cancer such as pancreatic cancer and lung cancer[1][2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: BEY1107. CAS No. 1983983-41-0. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-137432.
AZD-5438
AZD-5438 is a potent CDK1, CDK2, and CDK9 inhibitor, with IC50s of 16 nM, 6 nM, and 20 nM in cell-free assays, respectively. AZD-5438 shows less inhibition activity against GSK3?, CDK5 and CDK6[1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 602306-29-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-10012.
AZD8421
AZD8421 is a selective CDK2 inhibitor (IC50 = 9 nM) as well as achieving CDK family selectivity in cells versus key off-targets (CDK1, CDK4/6, CDK9), AZD8421 had no significant kinase inhibition outside the CDK family. AZD8421 inhibits cancer cell proliferation by inhibiting pRB phosphorylation, inducing cell cycle arrest in G1/S phase and senescence. AZD8421 can be studied in research for breast cancer and ovarian cancer[1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 3047321-53-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg. Product ID: HY-158106.
BIO-acetoxime
BIO-acetoxime is a potent and selective GSK-3 inhibitor, with IC50s of both 10 nM for GSK-3α/&beta. It shows >240-fold selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B. It has anticonvulsant and anti-infection activity. Synonyms: BIA; GSK-3 Inhibitor X; (2'Z,3'E)-6-Bromoindirubin-3'-acetoxime; (3Z)-3-[(3E)-3-(Acetoxyimino)-1,3-dihydro-2H-indol-2-ylidene]-6-bromo-1,3-dihydro-2H-indol-2-one; 2H-Indol-2-one, 3-[(3E)-3-[(acetyloxy)imino]-1,3-dihydro-2H-indol-2-ylidene]-6-bromo-1,3-dihydro-, (3Z)-; 6-Bromoindirubin acetoxime; 6-Bromoindirubin-3'-acetoxime. Grades: 98%. CAS No. 667463-85-6. Molecular formula: C18H12BrN3O3. Mole weight: 398.21.
BMS-265246
BMS-265246 is a potent and selective CDK1/2 inhibitor with IC50 of 6 nM/9 nM. It is 25-fold more selective for CDK1/2 than CDK4. Synonyms: BMS265246; BMS-265246; BMS 265246. Grades: >98%. CAS No. 582315-72-8. Molecular formula: C18H17F2N3O2. Mole weight: 345.34.
BMS-265246
BMS-265246 is a potent and selective cyclin-dependent kinase CDK1 and CDK2 inhibitor, with IC50 values of 6 and 9 nM, respectively. BMS-265246 inhibits CHI3L1 (chitinase 3-like-1) stimulation of ACE2 (angiotensin converting enzyme 2) and SPP (viral spike protein priming proteases). BMS-265246 can be used for ovarian cancer and COVID-19 research[1][2][3]. Uses: Scientific research. Group: Signaling pathways. CAS No. 582315-72-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-15275.
BMS-265246
BMS-265246 is a potent and selective pyra-zolopyridine based inhibitor of cdk2/cyclinE, cdk1/cyclinB and cdk4/ cyclinD. Group: Biochemicals. Alternative Names: (4-Butoxy-1H-pyrazolo[3, 4-b]pyridin-5-yl) (2, 6-difluoro-4-methylphenyl) methanone. Grades: Highly Purified. CAS No. 582315-72-8. Pack Sizes: 5mg. US Biological Life Sciences.
Worldwide
Bohemine
Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC50 of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities. Uses: Designed for use in research and industrial production. Product Category: Inhibitors. CAS No. 189232-42-6. Molecular formula: C18H24N6O. Mole weight: 340.42. Purity: ≥97%. Product ID: ACM189232426. Alfa Chemistry ISO 9001:2015 Certified. Categories: Bohemanella.
BRD 6989
BRD 6989 is a small molecule inhibitor with high selectivity for CDK8 over CDK19. It is an analog of the natural product cortistatin A (dCA), which inhibits CDK8 and upregulates IL-10. BRD 6989 selectively binds a complex of CDK8 with an IC50 of 200 nM. It also inhibits IFNγ-induced phosphorylation of STAT1 at Ser 727 site in BMDCs. It may be useful for inflammatory disorders. Synonyms: 2-Amino-5,6,7,8-tetrahydro-6-methyl-4-(3-pyridinyl)-3-quinolinecarbonitrile; BRD-6989; BRD6989. Grades: ≥98%. CAS No. 642008-81-9. Molecular formula: C16H16N4. Mole weight: 264.33.
BS-181 HCl
BS-181 HCl is a highly selective CDK7 inhibitor with IC50 of 21 nM. It is more than 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9. Synonyms: BS-181 HCl; BS 181 HCl; BS181 HCl. Grades: >98%. CAS No. 1397219-81-6. Molecular formula: C22H32N6.HCl. Mole weight: 416.99.
BS-181 hydrochloride
BS-181 hydrochloride is a highly selective CDK7 inhibitor with IC50 of 21 nM, and > 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9. Uses: Scientific research. Group: Signaling pathways. CAS No. 1397219-81-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-13266A.
BSJ-4-116
BSJ-4-116 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib (HY-10162)[1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2519823-34-6. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-139039.
Butyrolactone I
It is one of a family of three butyrolactones isolated from aspergillus fumigatus. It exhibits antitumor activity and inhibits the cell cycle at the G1/S and G2/M transitions. It is a selective inhibitor of cyclin-dependent kinases CDK1/cyclin B, CDK2 and CDK5. Synonyms: Olomoucin; 4'-O-Demethylversicolactone D; (2R)-2,5-Dihydro-4-hydroxy-2-[[4-hydroxy-3-(3-methyl-2-butenyl)phenyl]methyl]-3-(4-hydroxyphenyl)-5-oxo-2-furancarboxylic Acid Methyl Ester; (+)-3''-Dimethylallyl-butyrolactone II. Grades: >95% by HPLC. CAS No. 87414-49-1. Molecular formula: C24H24O7. Mole weight: 424.44.
CCT245737
CCT245737 is an orally bioactive CHK1 inhibitor (IC50 of 1.4 nM), displaying >1,000-fold selectivity against CHK2 and CDK1. It potently inhibits cellular CHK1 activity (IC50 30-220nM) and enhances gemcitabine and SN38 cytotoxicity in multiple human tumor cell lines and human tumor xenograft models. It causes inhibition of tumor growth in an Eμ-Myc mouse model of human B-cell lymphocytic leukemia. Synonyms: CCT-245737; CCT 245737; CCT245737; 5-[(4-{[(2R)-morpholin-2-ylmethyl]amino}-5-(trifluoromethyl)pyridin-2-yl)amino]pyrazine-2-carbonitrile. CAS No. 1489389-18-5. Molecular formula: C16H16F3N7O. Mole weight: 379.347.
CCT251545
CCT251545, a small molecule inhibitor of WNT signaling with oral activity, can be used as a selective chemical probe that exhibits >100-fold selectivity for the human Mediator complex-associated protein kinases CDK8 and CDK19 over 291 other kinases. IC50: Synonyms: 8-[3-chloro-5-[4-(1-methylpyrazol-4-yl)phenyl]pyridin-4-yl]-2,8-diazaspiro[4.5]decan-1-oneCCT251545; CCT 251545; CCT-251545; CHEMBL34082138-(3-chloro-5-(4-(1-methyl-1H-pyrazol-4-yl)phenyl)pyridin-4-yl)-2,8-diazaspiro[4.5]decan-1-one8-{3-Chloro-5-[4-(1-Methyl-1h-Pyrazol-4-Yl)ph. CAS No. 1661839-45-7. Molecular formula: C23H24ClN5O. Mole weight: 421.92.
CCT251545
CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with an IC50 of 5 nM in 7dF3 cells[1]. CCT251545 is a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease[2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1661839-45-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-12681.
CDK2-IN-4
CDK2-IN-4 (compound 73) is a potent and selective CDK2 inhibitor with an IC50 of 44 nM for CDK2/cyclin A, shows 2,000-fold selectivity over CDK1/cyclin B (IC50=86 uM)[1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2079895-42-2. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-117535.
CDK4 Inhibitor
Cdk4 inhibitor is a cell-permeable, asymmetrical indolocarbazole that exhibits antiproliferative activity by blocking cyclin D1/Cdk4 with an IC50 of 0.8 μM. It also inhibits the activity of other Cdk's only at much higher concentrations (IC50 = 520 nM and 2.1 μM for Cdk2/E and Cdk1/B, respectively). Cdk4 inhibitor can inhibit tumor cells growth in HCT-116 and NCI-H460 cells (IC50 < 3.0 μM). Synonyms: 2-Bromo-12,13-dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione. Grades: ≥90%. CAS No. 546102-60-7. Molecular formula: C20H10BrN3O2. Mole weight: 404.22.
Cdk4 Inhibitor V (4-(((4-Hydroxy-5-propoxy-pyridin-2-ylmethyl)-amino)-methylene)-6-iodo-4H-isoquinoline-1,3-dione)
A cell-permeable pyridinylmethylamino-isoquinoline dione compound that acts as a potent, ATP-binding site targeting and reversible inhibitor of Cdk4/D1 activity with selectivity over Cdk2/E and Cdk1/B (IC50=0.03, 1.6 and 25.3uM, respectively). Shown to block the phosphorylation of Rb and induce growth arrest in HCT116 and MCF-7 cells (IC50=0.73 and 0.88uM). Displays desirable metabolic stability in rat liver microsomes and in the presence of NADPH and UDPGA cofactors (t1/2 > 30mins). Group: Biochemicals. Grades: Highly Purified. CAS No. 943746-57-4. Pack Sizes: 5mg. Molecular Formula: C??H??IN?O?. US Biological Life Sciences.
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CDK9-IN-1
Among CDKs, CDK9 is a validated pathological target in HIV infection, inflammation and cardiac hypertrophy; however selective CDK9 inhibitors are still not available. We present a selective inhibitor family of CDK9 based on the 4-phenylamino-6- phenylpyrimidine nucleus. We show a convenient synthetic method to prepare a useful intermediate and its derivatisation resulting in novel compounds. The CDK9 inhibitory activity of the derivatives was measured in specific kinase assay and the CDK inhibitory profile of the best ones (IC50 > 100nM) was determined. The most selective compounds had high selectivity over CDK1, 2, 3, 5, 6, 7 and showed at least one order of magnitude higher inhibitory activity over CDK4 inhibition. The most selective molecules were examined in cytotoxicity assays and their ability to inhibit HIV-1 replication was determined in cellular assays. Synonyms: CDK9-IN-1; CDK9 IN 1. Grades: >98%. CAS No. 1415559-43-1. Molecular formula: C26H21N5O4S. Mole weight: 499.54.
CDKI-83
CDKI-83 is a potent CDK9 inhibitor. The compound shows effective anti-proliferative activity in human tumour cell lines with GI50 <1 μM, and is capable of inducing apoptosis in A2780 human ovarian cancer cells as determined by the activated caspase-3, Annexin V/PI double staining and accumulated cells at the sub-G1 phase of cellcycle. The research results suggest that combined inhibition of CDK9 and CDK1 may result in the effective induction of apoptosis and CDKI-83 has the potential to be developed as an anti-cancer agent. Synonyms: CDKI83; CDKI 83. CAS No. 1189558-88-0. Molecular formula: C21H23N7O3S2. Mole weight: 485.58.
CEP-5214
CEP-5214 is a potent, low-nanomolar pan inhibitor of human VEGF-R tyrosine kinases, displaying IC(50) values of 16, 8, and 4 nM for VEGF-R1/FLT-1, VEGF-R2/KDR, and VEGF-R3/FLT-4, respectively, with cellular activity equivalent to the isolated enzyme activity. Compound 21 exhibited good selectivity against numerous tyrosine and serine/threonine kinases including PKC, Tie2, TrkA, CDK1, p38, JNK, and IRK. Synonyms: CEP 5214; CEP5214; 3-(5,6,7,13-tetrahydro-9-((1-methylethoxy)methyl)-5-oxo-12h-indeno(2,1-a)pyrrolo(3,4-c)carbazol-12-yl)propanol; 12-(3-hydroxypropyl)-9-isopropoxymethyl-6,7,12,13-tetrahydro-5H-indeno[2,1-a]pyrrolo[4,3-c]carbazol-5-one. CAS No. 402857-39-0. Molecular formula: C28H28N2O3. Mole weight: 440.54.
CGP74514A
CGP74514A is a cell permeable Cdk inhibitor selective for Cyclin-dependent kinase-1 (Cdk1) (IC50=25nM). CGP74514A was also reported also to affect the activities of other kinases including PKCα (IC50=6.1μM), PKA (IC50=125μM) and EGFR (IC50>10μM), but only at much higher concentrations. Synonyms: 2-N-[(1R,2S)-2-aminocyclohexyl]-6-N-(3-chlorophenyl)-9-ethylpurine-2,6-diamine; CGP 74514A; 481724-82-7 (CGP74514A HCl salt); CGP-74514A; CGP74514A; N(2)-(2-aminocyclohexyl)-N(6)-(3-chlorophenyl)-9-ethyl-9H-purine-2,6-diamine. Grades: >98%. CAS No. 190653-73-7. Molecular formula: C19H24ClN7. Mole weight: 385.9.
CGP 74514 dihydrochloride
CGP 74514 Dihydrochloride is a potent cdk1 inhibitor with IC50 of 25 nM. It can reduce Akt phosphorylation and increase mitochondrial damage in leukemia cells. Synonyms: CGP 74514. Grades: ≥98%. Molecular formula: C19H24ClN7·2HCl. Mole weight: 458.82.
CVT-313
A cell-permeable purine analog that acts as a potent, selective, reversible, and ATP-competitive inhibitor of Cdk2 (IC50 = 0.5 μM for Cdk2/A and Cdk2/E; 4.2 μM for Cdk1/B; 215 μM for Cdk4/D1). Inhibits other kinases only at much higher concentrations (IC50 > 1.25 mM for MAPK, PKA, and PKC). Shown to induce tumor cells growth arrest (IC50 = ~1.25-20 μM) in vitro and prevent neointima formation in vivo. Synonyms: CVT 313; NG 26; CVT313; NG26; NG-26; NG26. Grades: 95%. CAS No. 199986-75-9. Molecular formula: C20H28N6O3. Mole weight: 400.47.
Desmethylglycitein
Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities.Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1). Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes. Uses: Designed for use in research and industrial production. Product Category: Inhibitors. CAS No. 17817-31-1. Molecular formula: C15H10O5. Mole weight: 270.24. Purity: 0.95. Product ID: ACM17817311. Alfa Chemistry ISO 9001:2015 Certified.
Dinaciclib
Cyclin-dependent kinases (CDKs) are critical positive regulators of cell cycle progression and cellular transcription whose dysregulation can lead to the development of cancer. Dinaciclib inhibits CDK1, CDK2, CDK5, and CDK9 activity in vitro with IC50 values of 3, 1, 1, and 4 nM, respectively. Compared to the pan-CDK inhibitor flavopiridol, dinaciclib is an equally potent inhibitor of CDK1 and CDK9 but a 12-14-fold more potent inhibitor of CDK2 and CDK5. It has been shown to inhibit DNA synthesis by blocking thymidine incorporation in A2780 ovarian cancer cells with an IC50 value of 4nM. At 5mg/kg it prevents tumor growth by 50% in an A2780 ovarian carcinoma mouse xenograft model and is active against a broad spectrum of human tumor cell lines in vitro (IC50s = 7-17nM). Group: Biochemicals. Alternative Names: Sch 727965; (2S) -1- [3-Ethyl-7- [ [ (1-oxido-3-pyridinyl) methyl]amino]pyrazolo [1, 5-a]pyrimidin-5-yl]-2-piperidineethanol. Grades: Highly Purified. CAS No. 779353-01-4. Pack Sizes: 5mg. Molecular Formula: C21H28N6O2. US Biological Life Sciences.
Worldwide
Dinaciclib
Dinaciclib, also known as SCH727965, is a potent CDK inhibitor with potential antineoplastic activity. Dinaciclib selectively inhibits cyclin dependent kinases CDK1, CDK2, CDK5, and CDK9 activity in vitro with IC(50) values of 1, 1, 3, and 4 nmol/L, respectively. Compared with flavopiridol, Dinaciclib exhibits superior activity with an improved therapeutic index. Dinaciclib induced regression of established solid tumors in a range of mouse models following intermittent scheduling of doses below the maximally tolerated level. Synonyms: SCH 727965; SCH727965; SCH-727965; PS095760; PS 095760; PS-095760; Dinaciclib. 2-[(2S)-1-[3-ethyl-7-[(1-oxidopyridin-1-ium-3-yl)methylamino]pyrazolo[1,5-a]pyrimidin-5-yl]piperidin-2-yl]ethanol. CAS No. 779353-01-4. Molecular formula: C21H28N6O2. Mole weight: 396.49.
Dinaciclib
Dinaciclib (SCH 727965) is a potent inhibitor of CDK, with IC50s of 1 nM, 1 nM, 3 nM, and 4 nM for CDK2, CDK5, CDK1, and CDK9, respectively[1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: SCH 727965. CAS No. 779353-01-4. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-10492.
Flavopiridol
Flavopiridol (Alvocidib) is a broad spectrum and competitive inhibitor of CDKs , inhibiting CDK1, CDK2, CDK4 with IC 50 s of 30, 170, 100 nM, respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: HMR-1275; Alvocidib; L86-8275. CAS No. 146426-40-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-10005.
Flavopiridol Hydrochloride
Flavopiridol Hydrochloride (Alvocidib Hydrochloride) is a broad inhibitor of CDK , competing with ATP to inhibit CDKs including CDK1, CDK2, CDK4 with IC 50 s of 30, 170, 100 nM, respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: Alvocidib Hydrochloride; L86-8275 Hydrochloride; HMR-1275 Hydrochloride. CAS No. 131740-09-5. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-10006.
FMF-04-159-2
FMF-04-159-2 is a covalent CDK14 inhibitor. FMF-04-159-2 inhibits CDK14 and CDK2 with IC50s of 39.6 nM and 256 nM in NanoBRET assay, respectively[1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2364489-81-4. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-127104.
An orally bioavailable and blood-brain-barrier permeable oxadiazolo-benzofuranyl phenyl sulfoxide compound that acts as a potent, reversible and ATP-competitive inhibitor of GSK-3b (IC50=35nM, 34 and 140nM for racemic, (S)-9b eutomer and (R)-9b distomer). The (S)-9b eutomer displays excellent selectivity (IC50 > 10uM) over Cdk1/2/5, Chk1, p38a, JNK1, MEKK1, IKKb, PKCth, CK1d, EGFR, ErbB2, Src, Lck, IR, Tie2, c-Kit, c-Met, VEGFR2, FGFR3 and PDGFRa/b, and lowers tau phosphorylation at GSK-3b-Thr205 in a CWS (cold water stress) mouse model (3mg/kg, p.o.). Group: Biochemicals. Grades: Highly Purified. CAS No. 1005201-24-0. Pack Sizes: 5mg. US Biological Life Sciences.
Worldwide
GSK 3 Inhibitor IX
GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3?/? and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3?/?)/CDK1/CDK5, respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: 6-Bromoindirubin-3'-oxime; BIO; MLS 2052. CAS No. 667463-62-9. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 50 mg. Product ID: HY-10580.
GSK-3 Inhibitor IX ((2Z,3E)-6-Bromoindirubin-3-oxime)
A cell-permeable bis-indolo (indirubin) compound that acts as a highly potent, selective, reversible, and ATP-competitive inhibitor of GSK-3a/b (IC50=5nM). Its specificity has been tested against various Cdk's (IC50=83, 300, 320, and 10,000nM for Cdk5/p25, Cdk2/A, Cdk1/B, and Cdk4/D1, respectively) as well as many other commonly studied kinases (IC50≥10uM), including MAP kinases, PKA, PKC isoforms, PKG, CK, and IRTK. Inhibition of GSK by BIO has been shown to result in the activation of Wnt-signaling pathway and sustained pluripotency in human and murine ESCs (embryonic stem cells). Reported to maintain self-renewal in human and mouse embryonic stem cells. Also induces the differentiation of neonatal cardiomyocytes. Group: Biochemicals. Grades: Highly Purified. CAS No. 667463-62-9. Pack Sizes: 1mg, 10mg. US Biological Life Sciences.
Worldwide
GW 5074
GW 5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, and has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms[1][2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 220904-83-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-10542.
A cell-permeable indazolyl imidazopyridazinamine compound that acts as a potent and reversible inhibitor of histone kinase haspin activity (IC50 = 2nM) with moderate selectivity over TrkA, GSK-3beta, PIM1, Cdk1/B and Cdk2/A (% inhibition at 100nM = 58, 48, 36, 34 and 33, respectively) among a panel of 27-kinases. Shown to block pH3-Thr3, with no effect on pH3-Ser10 and pH3-Ser28, cause mitotic catastrophe, upregulate BUB1 and cyclin B1 levels, and potently induce apoptosis (IC50 = 473, 500 and 752nM in HeLa, HCT-116 and MDA-MB-231 cells, respectively). Further, efficiently blocks bFGF-induced sprouting vessel by 70% at 1uM (chicken embryo aortic arch ring assay) and suppresses tumor growth in HCT-116 xenografted mouse model (50mg/kg, i.p.). Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
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