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CDK2, a member of the eukaryotic S/T protein kinase family, catalyzes the phosphoryl transfer of ATP γ-phosphate to serine or threonine hydroxyl (denoted as S0/T0) in a protein substrate. Activity of CDK2 is maximal during S phase and G2; activated by interaction with cyclin E during the early stages of DNA synthesis to permit G1-S transition, and subsequently activated by cyclin A2 (cyclin A1 in germ cells) during the late stages of DNA replication to drive the transition from S phase to mitosis, the G2 phase. Synonyms: Cell division protein kinase 2; kinase Cdk2; p33 protein kinase; Anti-Gastric receptor I; Anti-H2R; His-His-Ala-Ser-Pro-Arg-Lys; L-histidyl-L-histidyl-L-alanyl-L-seryl-L-prolyl-L-arginyl-L-lysine. Grades: ≥95%. CAS No. 255064-79-0. Molecular formula: C35H57N15O9. Mole weight: 831.92.
CDK2
CDK2 is a member of the eukaryotic S/T protein kinase family and its function is to catalyze the phosphoryl transfer of ATP γ-phosphate to serine or threonine hydroxyl (denoted as S 0 /T 0 ) in a protein substrate. Uses: Scientific research. Group: Peptides. CAS No. 255064-79-0. Pack Sizes: 5 mg. Product ID: HY-P0235.
Cdk2/9 Inhibitor - CAS 507487-89-0
The Cdk2/9 Inhibitor, also referenced under CAS 507487-89-0, controls the biological activity of Cdk2/9. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy.
CDK2 acetate
CDK2 acetate, a member of the eukaryotic S/T protein kinase family, catalyzes the phosphoryl transfer of ATP γ-phosphate to serine or threonine hydroxyl (denoted as S0/T0) in a protein substrate. Synonyms: H-His-His-Ala-Ser-Pro-Arg-Lys-OH.CH3CO2H; L-histidyl-L-histidyl-L-alanyl-L-seryl-L-prolyl-L-arginyl-L-lysine acetic acid. Grades: ≥95%. Molecular formula: C37H61N15O11. Mole weight: 891.99.
CDK2-IN-30 (Formula (I)) is a CDK2 inhibitor with an IC 50 value ≤20 nM. CDK2-IN-30 can be used in tumor research [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2640038-22-6. Pack Sizes: 1 mg; 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-164664.
CDK2 inhibitor II
CDK2 inhibitor II. Group: Biochemicals. Alternative Names: 4- [2- (5-Bromo-1, 2-dihydro-2-oxo-3H-indol-3-ylidene) hydrazinyl] benzenesulfonamide; 4- [ (5-Bromo-1, 2-dihydro-2-oxo-3H-indol-3-ylidene) hydrazino] benzenesulfonamide; SC 221409. Grades: Highly Purified. CAS No. 222035-13-4. Pack Sizes: 5mg. Molecular Formula: C14H11BrN4O3S, Molecular Weight: 395.23. US Biological Life Sciences.
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CDK2 Inhibitor II
The cyclin-dependent kinase 2 (Cdk2) works with cyclins A or E to regulate S phase and G2-M transition during the cell cycle. Cdk2 Inhibitor II is a potent, cell-permeable, ATP-competitive, and selective inhibitor of Cdk2. It is a 3-(benzylidne)indolin-2-one analog that selectively and potently inhibits Cdk2 with IC50 of 60 nM. Synonyms: Cyclin-dependent kinase 2 Inhibitor II; SC-221409. Grades: ≥95%. CAS No. 222035-13-4. Molecular formula: C14H11BrN4O3S. Mole weight: 395.2.
Cdk2 Inhibitor II - CAS 222035-13-4
The Cdk2 Inhibitor II, also referenced under CAS 222035-13-4, controls the biological activity of Cdk2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy.
Cdk2 Inhibitor III - CAS 199986-75-9
The Cdk2 Inhibitor III, also referenced under CAS 199986-75-9, controls the biological activity of Cdk2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy.
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.
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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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1-Naphthyl PP1
1-Naphthyl PP1 (1-NA-PP 1) is a selective inhibitor of src family kinases and Protein Kinase D. 1-Naphthyl PP1 inhibits v-Src and c-Fyn, c-Abl, CDK2 and CAMK II with IC 50 s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively [1] [2] [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: 1-NA-PP 1. CAS No. 221243-82-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-13941.
1-Naphthyl PP1
Selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl. (IC50 values are 1.0, 0.6, 0.6, 18 and 22 uM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively). Preferentially inhibits mutant over wild-type kinases (IC50 values are 1.5 vs 1000 nM for I338G v-src and v-src respectively). Group: Biochemicals. Grades: Highly Purified. CAS No. 221243-82-9. Pack Sizes: 10mg, 50mg. Molecular Formula: C19H19N5. US Biological Life Sciences.
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1-Naphthyl PP1 hydrochloride
1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) is a selective inhibitor of src family kinases. 1-Naphthyl PP1 hydrochloride inhibits v-Src and c-Fyn, c-Abl, CDK2 and CAMK II with IC 50 s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: 1-NA-PP 1 hydrochloride. CAS No. 956025-47-1. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-13941B.
1-Naphthyl PP1 hydrochloride
1-Naphthyl PP1 hydrochloride is a selective inhibitor of src family kinases, including v-Src and c-Fyn, tyrosine kinase c-Abl and CAMK II with IC50 values of 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively. It was considerably more potent and showed distinct substituent effects at the pyrazolopyrimidine core. It was cell-active, and potently blocked prostate cancer cell proliferation by inducing G2/M arrest. Uses: 1-naphthyl pp1 hydrochloride could potently block prostate cancer cell proliferation by inducing g2/m arrest. Synonyms: 1-Tert-butyl-3-(naphthalen-1-yl)-1H-pyrazolo[3,4-d]pyriMidin-4-aMine hydrochloride;1-NA-PP 1 hydrochloride. Grades: >98 %. CAS No. 956025-47-1. Molecular formula: C19H20ClN5. Mole weight: 353.85.
2-(4-Aminophenyl)propanoic Acid
2-(4-Aminophenyl)propanoic acid is a reagent in the preparation of 3-aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents (Erratum). Group: Biochemicals. Grades: Highly Purified. CAS No. 59430-62-5. Pack Sizes: 250mg, 1g. Molecular Formula: C9H11NO2, Molecular Weight: 165.19. 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.
An analogue of Olomoucine that acts as a potent inhibitor of Cdk 1 (IC50=100nm) and Cdk2 (IC50=80nm). Also displays antiproliferative and proapoptotic effects. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. US Biological Life Sciences.
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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.
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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.
AG 494
AG-494 is a EGFR (epidermal growth factor receptor) kinase inhibitor with IC50 value of 0.7 μM. It is selective over ErbB2, PDGFR and insulin receptor kinase (IC50 values are 42, 6 and > 100 μM respectively). AG-494 tyrphostin also can block Cdk2 activation. Synonyms: alpha-Cyano-(3,4-dihydroxy)-N-phenylcinnamide; Tyrphostin AG-494; Tyrphostin B48. Grades: 98%. CAS No. 139087-53-9. Molecular formula: C16H12N2O3. Mole weight: 280.28.
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.
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.
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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.
Isolated from Streptomyces sp., Antibiotic UCN-01 inhibits protein kinase C (PKC) and cyclin-dependent kinase 2 (CDK2) resulting in accumulation of cells in the G1 phase and induction of apoptosis. UCN-01 also enhances the cytotoxicity of other anti-cancer drugs, such as DNA-damaging agents and anti-metabolite drugs, through putative abrogation of G2 and/or S phase accumulation induced by these anti-cancer agents. Group: Biochemicals. Alternative Names: 7-Hydroxystaurosporine, UCN-01. Grades: Highly Purified. CAS No. 112953-11-4. Pack Sizes: 1mg. US Biological Life Sciences.
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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.
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.
Bisindolylmaleimide III
Potent and selective protein kinase C (PKC) inhibitor. Inhibits panel of protein kinases (e.g. GSK-3beta, CDK2). Group: Biochemicals. Grades: Highly Purified. CAS No. 137592-43-9. Pack Sizes: 1mg, 5mg. Molecular Formula: C23H20N4O2. US Biological Life Sciences.
Worldwide
Bisindolylmaleimide VIII acetate
Selective protein kinase C (PKC) inhibitor. Inhibits proliferation of cultured mouse epidermal keratinocytes. Enhances Fas- and TRAIL-mediated apoptosis. Inhibits T cell-mediated autoimmune diseases. Inhibits stimulation of insulin secretion by glucose. Inhibits panel of protein kinases (e.g. GSK-3beta, CDK2). Group: Biochemicals. Alternative Names: Ro 31-7549, BIM VIII. Grades: Highly Purified. CAS No. 138516-31-1. Pack Sizes: 1mg, 5mg. Molecular Formula: C24H22N4O2. CH3COOH. US Biological Life Sciences.
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Bisindolylmaleimide X hydrochloride
Bisindolylmaleimide X hydrochloride is a potent and selective cell-permeable protein kinase C (PKC) inhibitor with IC50 of 15 nM for rat brain PKC. It has also been identified as an inhibitor of Cdk2 with IC50 of 200. It has been used to activate mesenchymal stem cells, which increases the surface expression of homing ligands that bind to intercellular adhesion molecule and target delivery of these cells to sites of inflammation. Uses: Enzyme inhibitors. Synonyms: BIM X; Ro 31-8425. Grades: ≥98%. CAS No. 145317-11-9. Molecular formula: C26H24N4O2·HCl. Mole weight: 461.
Bisindolylmaleimide X hydrochloride
Selective protein kinase C (PKC) inhibitor. Inhibits panel of protein kinases (e.g. GSK-3beta, CDK2). Inhibits superoxide generation in human neutrophils. Group: Biochemicals. Alternative Names: Ro 31-8425, BIM X. Grades: Highly Purified. CAS No. 131848-97-0, 145317-11-9. Pack Sizes: 1mg, 5mg. Molecular Formula: C26H24N4O2 HCl. US Biological Life Sciences.
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Bml-259
BML-259 is a potent cyclin-dependent kinase 5 (Cdk5) inhibitor, with IC50s of 64 and 98 nM for Cdk5 and Cdk2, respectively. Uses: Designed for use in research and industrial production. Product Category: Inhibitors. Appearance: White to off-white solid. CAS No. 267654-00-2. Molecular formula: C14H16N2OS. Mole weight: 260.4. Purity: >98%. IUPACName: 2-phenyl-N-(5-propan-2-yl-1,3-thiazol-2-yl)acetamide. Canonical SMILES: O=C(NC1=NC=C(C(C)C)S1)CC2=CC=CC=C2. Product ID: ACM267654002. Alfa Chemistry ISO 9001:2015 Certified.
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.
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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.
BS181
BS-181 is a highly selective CDK inhibitor for CDK7 with an IC(50) of 21 nmol/L. Testing of other CDKs as well as another 69 kinases showed that BS-181 only inhibited CDK2 at concentrations lower than 1 micromol/L, with CDK2 being inhibited 35-fold less potently (IC(50) 880 nmol/L) than CDK7. In MCF-7 cells, BS-181 inhibited the phosphorylation of CDK7 substrates, promoted cell cycle arrest and apoptosis to inhibit the growth of cancer cell lines, and showed antitumor effects in vivo. The drug was stable in vivo with a plasma elimination half-life in mice of 405 minutes after i.p. administration of 10 mg/kg. The same dose of drug inhibited the growth of MCF-7 human xenografts in nude mice. BS-181 therefore provides the first example of a potent and selective CDK7 inhibitor with potential as an anticancer agent. Synonyms: BS-181; BS181; BS 181. CAS No. 1092443-52-1. Molecular formula: C22H32N6. Mole weight: 380.53.
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.
Ca2+ Channel Agonist 1
A Ca2+ Channel Agonist that selectively acting on N-type Ca2+ channel and also be found to restrain the cdk activity at some extent. IC50: 14.23 uM (EC50, Ca2+ channel) 3.34 uM (EC50, cdk2). Uses: A ca2+ channel agonist that selectively acting on n-type ca2+ channel and also be found to restrain the cdk activity at some extent. Synonyms: Ca2+ channel agonist 1; SCHEMBL17628623; CS-5169; CS 5169; CS5169. Grades: 98%. CAS No. 1402821-24-2. Molecular formula: C19H26N6O. Mole weight: 354.46.
CAY10554
Cyclin-dependent kinases (CDKs) are the families of protein kinases first discovered for their role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells. They are key regulators of cell cycle progression and are therefore promising therapeutic targets for cancer and neurodegenerative diseases. CAY10554 is a potent inhibitor of Cdk5 and Cdk2, with IC50 values of 64 and 98 nM, respectively. Synonyms: BML-259; BML 259; CAY 10554; CAY-10554. Grades: ≥95%. CAS No. 267654-00-2. Molecular formula: C14H16N2OS. Mole weight: 260.4.
CAY10574
Cyclin-dependent kinases (CDKs) are the families of protein kinases first discovered for their role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells. They are key regulators of cell cycle progression and are therefore promising therapeutic targets for cancer and neurodegenerative diseases. CAY10574, also known as Cdk9 Inhibitor II, is a potent, selective inhibitor with an IC50 of 0.35 μM. It is also a competitive inhibitor of Cdk2-cyclin E with Ki of 13.3 μM and IC50 values 20 μM. Synonyms: CAY 10574; CAY-10574; Cdk9 Inhibitor II. Grades: ≥95%. CAS No. 140651-18-9. Molecular formula: C9H10N6O. Mole weight: 218.2.
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.
Worldwide
Cirtociclib
Cirtociclib (BLU-222) is an orally active and highly selective CDK2 inhibitor. Cirtociclib disrupts Rb signaling and causes G1 arrest and apoptosis in CCNE1-amplified endometrial cancer cells [1] [2] [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: BLU-222. CAS No. 2888704-84-3. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-160701.
CK7
CK7, a Cdk2/9 inhibitor, can be used for the synthesis of Nek1 inhibitor BSc5231 and BSc5367 [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 507487-89-0. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-103646.
CPS2
CPS2 is a first-in-class, highly potent, selective and irreversible PROTAC CDK2 degrader ( IC 50 = 24 nM). CPS2 can be used for the research of acute myeloid leukemia [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2756741-90-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-141680.
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.
CVT-313
CVT-313 (Cdk2 Inhibitor III) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC 50 of 0.5 μM. CVT-313 inhibits CDC5L phosphorylation [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: Cdk2 Inhibitor III. CAS No. 199986-75-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg. Product ID: HY-15339.
CYC065
CYC065 is a second-generation, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with potential antineoplastic and chemoprotective activities. Synonyms: CYC065; CYC 065; CYC-065; (2R,3S)-3-[[6-[(4,6-dimethylpyridin-3-yl)methylamino]-9-propan-2-ylpurin-2-yl]amino]pentan-2-ol. CAS No. 1070790-89-4. Molecular formula: C21H31N7O. Mole weight: 397.52.
cyclin-dependent kinase
Activation of cyclin-dependent kinases requires association of the enzyme with a regulatory subunit referred to as a cyclin. It is the sequential activation and inactivation of cyclin-dependent kinases, through the periodic synthesis and destruction of cyclins, that provides the primary means of cell-cycle regulation. Group: Enzymes. Synonyms: Bur1; Bur1 Cdk; Cak1; Cak1p; cdc2; cdc2 kinase; Cdc28p; CDK; cdk-activating kinase; Cdk-activating protein kinase; cdk1; cdk2; Cdk2; cdk3; cdk4; cdk5; cdk6; cdk7; cdk8; cdk9; cyclin A-activated cdc2; cyclin A-activated cdk2; cyclin D-cdk6 kinase; cyclin D-depende. Enzyme Commission Number: EC 2.7.11.22. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-3142; cyclin-dependent kinase; EC 2.7.11.22; Bur1; Bur1 Cdk; Cak1; Cak1p; cdc2; cdc2 kinase; Cdc28p; CDK; cdk-activating kinase; Cdk-activating protein kinase; cdk1; cdk2; Cdk2; cdk3; cdk4; cdk5; cdk6; cdk7; cdk8; cdk9; cyclin A-activated cdc2; cyclin A-activated cdk2; cyclin D-cdk6 kinase; cyclin D-dependent kinase; cyclin E kinase; cyclin-A associated kinase; cyclin-dependent kinase 6; cyclin-dependent kinase-2; cyclin-dependent kinase-4; cyclin-dependent protein kinase activating kinase; cyk; D-type cyclin kinase; nclk; neuronal cdc2-like kinase; PCTAIRE-1; STK25. Cat No: EXWM-3142.
Decursin
Decursin ((+)-Decursin) is a potent anti-tumor agent. Decursin also is a cytotoxic agent and a potent protein kinase C activator. Decursin induces apoptosis and cell cycle arrest at G1 phase. Decursin decreases the expression of CDK2, CDK4, CDK6, cyclin D1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities [1] [2] [3] [4]. Uses: Scientific research. Group: Natural products. Alternative Names: (+)-Decursin. CAS No. 5928-25-6. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-18981.
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.
(E)-β-Farnesene
(E)-β-Farnesene (trans-β-Farnesene) is an aphid alarm pheromone, which can be found in Phlomis aurea Decne essential oil. (E)-β-Farnesene shows good binding score with a value of -30.64 kcal/mol to the CDK2 receptor. (E)-β-Farnesene also exhibits good affinity to odorant-binding protein 3 ( OBP3 ). (E)-β-Farnesene can be used as a feeding stimulant for the sand fly Lutzomyia longipalpis [1] [2] [3] [4]. Uses: Scientific research. Group: Natural products. Alternative Names: trans-β-Farnesene. CAS No. 18794-84-8. Pack Sizes: 10 mM * 1 mL; 100 mg; 250 mg; 500 mg; 1 g. Product ID: HY-N7364.
ERK Inhibitor VIII ((S)-4-(2-(2-Chloro-4-fluorophenylamino)-5-methylpyrimidin-4-yl)-N-(1-(3-chlorophenyl)-2-hydroxyethyl)-1H-pyrrole-2-carboxamide)
A cell-permeable pyrimidylpyrrole compound that acts as an active site-targeting, highly potent and selective ERK1/2 inhibitor (KI <2nM against Erk2; [ATP] = 65uM), while inhibiting GSK-3, Aurora A, Cdk2 only at much higher concentrations (KI = 395, 540, and 852nM, respectively) and exhibiting much reduced or little potency toward a panel of more than 130 other kinases (KI ≥1.4uM; IC50 ≥1uM). Shown to effectively inhibit human colon carcinoma HT-29 proliferation (IC50 = 48nM) and restore EGFR inhibitor WZ4002 antiproliferation activity in WZR10 cultures (84% and no inhibition, respectively, by 100nM WZ4002 with or without 1uM Erk Inhibitor VIII co-treatment). Orally available in both mice and rats in vivo. Group: Biochemicals. Grades: Highly Purified. CAS No. 896720-20-0. Pack Sizes: 10mg. Molecular Formula: C??H??Cl?FN?O?. US Biological Life Sciences.
Worldwide
Fadraciclib
Fadraciclib (CYC065) is a second-generation, orally available ATP-competitive inhibitor of CDK2 / CDK9 kinases [1] with IC 50 s of 5 and 26 nM, respectively [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: CYC065. CAS No. 1070790-89-4. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-101212.
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