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CDK
| Cat. No. | Product Name | CAS No. | Information |
|---|---|---|---|
| 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]. |
| CSN11250 | Kenpaullone | 142273-20-9 | Kenpaullone is an ATP-competitive inhibitor of CDK1cyclin B (IC50 0.4 M), CDK2cyclin A (IC50 0.68 M), CDK5p25 (IC50 0.85 M), lymphocyte kinase (IC50 0.47 M) , and GSK-3 (C50 0.23 M). |
| 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. |
| 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. |
| 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 CDK129 with IC50 of 16620 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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