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CDK

CDK

货号 产品名 CAS号 信息
CSN28803 YKL-5-124 1957203-01-8 YKL-5-124 is a highly selective, covalent CDK7 inhibitor with IC50 value of 9.7nM. It causes arrest at the G1/S transition and inhibition of E2F-driven gene expression, but resulted in no change to Pol II CTD phosphorylation.
CSN28491 XY028-133 2229974-73-4 XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity.
CSN25265 Trilaciclib 1374743-00-6 Trilaciclib is an inhibitor of CDK4 and CDK6 with IC50s of 1 nM and 4 nM, respectively.
CSN22094 Trilaciclib hydrochloride 1977495-97-8 Trilaciclib hydrochloride is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively.
CSN24801 TP-353   1253799-29-9 TP353 is a CDK7 inhibitor.
CSN26130 Simurosertib 1330782-76-7 TAK-931 is an oral CDC7-selective inhibitor as a candidate clinical anticancer drug. It induced S phase delay and replication stress.
CSN26176 Mevociclib 1816989-16-8 SY-1365 is a first-in-class selective CDK7 inhibitor with Ki of 17.4 nM.
CSN25349 SR-4835 2387704-62-1 SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13 with IC50 of 99 nM, Kd of 98 nM for CDK12 and Kd of 4.9 nM for CDK13. It acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death.
CSN23869 4-((2-(6-(4-Methylpiperazine-1-carbonyl)naphthalen-2-yl)ethyl)amino)quinazoline-6-carbonitrile 1449228-40-3 Senexin B is a potent and selective CDK8/19 inhibitor.
CSN28485 PROTAC CDK9 degrader-2 2435721-30-3 PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC.
CSN25543 PNU112455A hydrochloride 21886-12-4 PNU112455A HCl is an ATP site competetive inhibitor of CDK2 and CDK5. The Km for binding to the ATP site of CDK2 and CDK5 is 3.6 and 3.3 mM, respectively.
CSN33169 PF-07104091 2460249-19-6 PF-07104091 is an orally bioavailable inhibitor of cyclin-dependent kinase 2.
CSN24146 PF-06873600 2185857-97-8 PF-06873600 is a selective and orally bioavailable inhibitor of cyclin-dependent kinase (CDK) with Ki of 0.09 nM, 0.13 nM and 0.16 nM for CDK2, CDK4 and CDK6 respectively. PF-06873600 has potential antineoplastic activity.
CSN27187 NVP-2   1263373-43-8 NVP-2 is a potent and selective ATP-competitive CDK9 inhibitor with IC50 value of 0.5nM.
CSN25344 NU6140 444723-13-1 NU6140 is a selective CDK2 inhibitor with IC50 value of 0.94μM, as well as potently inhibits Aurora kinase A/B with IC50 values of 0.035 and 0.067μM, respectively.
CSN25261 NSC 95397 93718-83-3 NSC 95397 is irreversible Cdc25 dual specificity phosphatase inhibitor with Ki values of 32, 96, and 40 nM for Cdc25A, Cdc25B, and Cdc25C, respectively.
CSN26520 Mps1-IN-1 dihydrochloride 1883548-93-3 Mps1-IN-1 dihydrochloride is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM[1].
CSN28423 LY3177833 monhydrate 1627696-53-0 LY3143921 is an orally administered ATP-competitive inhibitor of CDC7 with potential antineoplastic activity.
CSN11250 Kenpaullone 142273-20-9 Kenpaullone is an ATP-competitive inhibitor of CDK1/cyclin B (IC50 = 0.4 µM), CDK2/cyclin A (IC50 = 0.68 µM), CDK5/p25 (IC50 = 0.85 µM), lymphocyte kinase (IC50 = 0.47 µM) , and GSK-3β (C50 = 0.23 μM).
CSN26115 JSH-150 2247481-21-4 JSH-150 is a highly selective CDK9 kinase inhibitor with IC50 value of 1nM. It dose-dependently inhibited the phosphorylation of RNA Pol II, suppress the expression of MCL-1 and c-Myc, arrested the cell cycle and induced the apoptosis in the leukemia cells.
CSN26608 Lerociclib dihydrochloride 2097938-59-3 in Rb null cells. In vivo, daily oral treatment with G1T38 causes significant, durable growth inhibition of tumors in a HER2/neu GEMM and in MCF7 xenograft breast cancer models.
CSN33095 HQ461 1226443-41-9 HQ461 is a molecular glue degrader. It acts by promoting an interaction between CDK12 and DDB1-CUL4-RBX1 E3 ubiquitin ligase, leading to polyubiquitination and degradation of CDK12-interacting protein Cyclin K (CCNK).
CSN26525 FIT-039 1113044-49-7 for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.
CSN26610 FN-1501-propionic acid 2408642-48-6 FN-1501-propionic acid is a CDK2/9 ligand for PROTAC. FN-1501-propionic acid and a CRBN ligand have been used to design PROTAC CDK2/9 degrader (HY-130709)[1].
CSN26613 Fadraciclib 1070790-89-4 Fadraciclib, also known as CYC065, is an orally bioavailable inhibitor of cyclin dependent kinases 2, 5 and 9 (CDK2/5/9) with potential antineoplastic and chemoprotective activities. CYC065 selectively binds to and inhibits the activity of CDK2, 5 and 9, which leads to inhibition of CDK2, 5 and 9-dependent cellular pathways, downregulation of genes involved in the pro-survival pathway, prevention of the activation of DNA double-strand break repair pathways, and induction of both cell cycle arrest and apoptosis. This inhibits the proliferation of CDK2/5/9-overexpressing tumor cells. In addition, CYC065 protects hematopoietic stem and progenitor cells (HSPCs), prevents myelosuppression, and preserves the function of the bone marrow.
CSN24779 EHT 1610 1425945-60-3 EHT 5372 is a strong inhibitor of DYRK’s family kinases, with IC50s of 0.22, 0.28 nM for DYRK1A and DYRK1B, respectively.
CSN33099 dCeMM4 1281683-44-0 dCeMM4 is a molecular glue degrader, inducing ubiquitination and degradation of cyclin K by prompting an interaction of CDK12:cyclin K with a CRL7B ligase complex.
CSN33098 dCeMM3 311787-85-6 dCeMM3 is a molecular glue degrader, inducing ubiquitination and degradation of cyclin K by prompting an interaction of CDK12:cyclin K with a CRL6B ligase complex.
CSN33097 dCeMM2 296771-07-8 dCeMM2 is a molecular glue degrader, inducing ubiquitination and degradation of cyclin K by prompting an interaction of CDK12:cyclin K with a CRL5B ligase complex.
CSN33096 N'-(5-Bromo-2-hydroxybenzylidene)-4-methylbenzenesulfonohydrazide 118719-16-7 dCeMM1 is a molecular glue degrader, inducing ubiquitination and degradation of cyclin K by prompting an interaction of CDK12:cyclin K with a CRL4B ligase complex.
CSN28413 Dalpiciclib 1637781-04-4 Dalpiciclib is a novel CDK 4/6 inhibitor which demonstrated promising anti-tumor potency in preclinical models.
CSN28450 CP5V 2509359-75-3 CP5V is a PROTAC targeting on Cdc20 with DC50 value of 1.6μM, comprising a Cdc20 ligand and VHL binding moiety bridged by a PEG5 linker. It leads to significant inhibition of breast cancer cell proliferation and resensitization of Taxol-resistant cell lines and suppressed breast tumor progression in vivo.
CSN28453 CP-10 2366268-80-4 CP-10 is a PROTAC targeting on CDK4/6 with DC50 values of 150-180 nM and 2.1 nM, respectively. It was generated by linking CDK6 inhibitor palbociclib and E3 ligase CRBN recruiter pomalidomide.
CSN26611 CDK6/9-IN-1 2414373-55-8 CDK6/9-IN-1 (compound 66) is an oral available and dual CDK 6 and CDK 9 inhibitor, with IC50 values of 40.5 nM and 39.5 nM for CDK6 anmd CDK9, respectively[1].
CSN26612 CDK5 inhibitor 20-223 865317-30-2 CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC50s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent[1].
CSN26129 CDK2-IN-4 2079895-42-2 CDK2 inhibitor 73 is a selective CDK2 inhibitor with IC50 value of 44nM.
CSN28766 BSJ-4-116 2519823-34-6 BSJ-4-116 is a CDK12-specific degrader with IC50 value of 6nM. Degradation of CDK12 by BSJ-4-116 resulted in premature cleavage and poly(adenylation) of DDR genes.
CSN28466 BSJ-04-132 2349356-39-2 BSJ-04-132 is a potent and selective Ribociclib-based CDK4 degrader (PROTAC), with IC50s of 50.6 nM and 30 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-04-132 does not induce CDK6 and IKZF1/3 degradation. BSJ-04-132 has anti-cancer activity.
CSN28469 BSJ-03-204 2349356-09-6 BSJ-03-204 is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 does not induce IKZF1/3 degradation and has anti-cancer activity.
CSN23969 BSJ-03-123 2361493-16-3 BSJ-03-123 is a PROTAC selectively targeting on CDK6, consist of a warhead palbociclib (a CDK inhibitor) linked to a CRBN ligand pomalidomide.
CSN25245 BS-194 1092443-55-4 BS-194 is a selective and potent CDK inhibitor with IC50 values of 3, 30, 30, 250, and 90nM for CDK2, CDK1, CDK5, CDK7, and CDK9, respectively.
CSN17259 Briciclib 865783-99-9 Briciclib is a small molecule that suppresses cyclin D1 accumulation in cancer cells.
CSN24819 Bohemine 189232-42-6 Bohemine is a potent and selective, cell-permeable, cyclin-dependent kinase (CDK) inhibitor with IC50 = 1 µM. Bohemine is structurally similar to Olomoucine and Roscovitine.
CSN25300 BI-1347 2163056-91-3 BI-1347 is a potent CDK8 inhibitor with an IC50 of 1.1 nM.
CSN21503 AZD-5438 602306-29-6 AZD5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16/6/20 nM.
CSN25869 Atuveciclib 1414943-94-4 Atuveciclib is an orally available and selective PTEFb/CDK9 inhibitor for the treatment of cancer.
CSN24882 6-(Dimethylamino)purine 938-55-6 6-(Dimethylamino)purine is a dual inhibitor of protein kinase and CDK.
CSN27194 (±)-Enitociclib 1610358-53-6 (±)-BAY-1251152 is a racemic mixture form of BAY-1251152. BAY 1143572 is the first selective, orally available PTEFb/CDK9 inhibitor that entered clinical development with IC50 value of 3nM.
CSN26940 (-)-Enitociclib 1610358-59-2 (-)-BAY-1251152 is an enanthiomer of BAY-1251152 with rotation (-). BAY-1251152 is a potent and highly selective PTEF/CDK9 inhibitor.
CSN84227 ABC1183 1042735-18-1
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