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Cat. No. Product Name CAS No. Information
PC-35808

MC180295

2237942-08-2

MC180295 (MC-180295, MC 180295) is a novel potent, highly selective CDK9 inhibitor with IC50 of 5 nM, displays >22-fold selectivity over other CDKs; also shows high selectivity against a panel of 250 kinases at 1 uM; specificly inhibits the phosphorylation levels of Ser2 (pSer2); CDK9-mediated phosphorylation of BRG1 prevents it from being recruited to heterochromatin loci, while CDK9 inhibition allows BRG1 to remodel chromatin and alter gene expression; demonstrates broad anti-cancer activity in vitro and is effective in in vivo cancer models; also sensitize to anti-PD1 in vivo, increases the numbers of CD45+ immune cells and the percentages of CD3+ T cells and activates dendritic cells in the tumor environment, while not kill human T lymphocytes and did not affect the ratio of CD4 and CD8 T cells in vivo.

PC-35532

Compound 919278

2189366-77-4

Compound 919278 is a specific inhibitor of lymphotoxin β receptor (LTβR, IC50=0.169 uM), and TNF receptor superfamily member 12A (FN14)-dependent nuclear translocation of p52 (IC50=0.167 uM) via inhibiting CDK12/CCNK, does not inhibit the TNF-α-mediated nuclear translocation of p65 (RelA); prevents the accumulation of NIK, selectively inhibits the noncanonical NF-kB pathway; prevents the LTβR- and FN14-dependent expression of MAP3K14 (which encodes NIK) as well as NIK accumulation by reducing phosphorylation of the carboxyl-terminal domain of RNA polymerase II; reduces the binding of both CDK12 and its associated protein CCNK with IC50 of 30-60 nM, inhibits CDK12 cellular activity and reduces the phosphorylation of Ser2 on the RNA Pol II CTD; phenocopies the effect of CDK12 knockdown on DEGs.

PC-35250

AZD-4573

2057509-72-3

AZD-4573 (AZD4573) is a potent and selective inhibitor of CDK9, with fast-off binding kinetics and high selectivity versus other kinases, including other CDK family kinases; AZD4573 exhibits a short half-life in multiple preclinical species and good solubility for intravenous administration; dose- and time-dependently decreases cellular pSer2-RNAPII, resulting in activation of caspase 3 and cell apoptosis in a broad range of haematological cancer cell lines; demonstrates in vivo efficacyin xenograft models derived from multiple haematological tumours.

Liver Cancer

Phase 1 Clinical

PC-63305

HSD992

2222045-50-1

HSD992 is a potent, selective CDK2/3 inhibitor with moderate CDK9 inhibition with IC50 of 18 nM, 57 nM and 49 nM for CDK3/cyclin E, CDK2/cyclin A1 and CDK2/cyclin E, respecively; only poorly inhibits the activities of CDKs 1, 4, 5, 6, 14, 16, 17, 18 and 19, and does not inhibit PLK isoforms; inhibits HLY-1 and NCI-H520 with IC50 values of 232 nM and 307 nM, respectively, The IC50 values against other cell lines (LC-2/Ad, K562, HeLa, NCI-H1703 and DMS114) ranged from 427 nM to 723 nM.

PC-63252

BI-1347

2163056-91-3

BI-1347 is a potent, selective inhibitor of CDK8/cyclinC with IC50 of 1 nM; BI-1347 shows tumor growth inhibition in an in vivo xenograft model, BI-1347 is an excellent small molecule tool inhibitor for testing biological hypotheses in vitro and in vivo.

PC-42944

THZ2

1604810-84-5

THZ2, an analogue of THZ1 with improved pharmacokinetic features, is a potent, selective CDK7 inhibitor with IC50 of 13.9 nM, displays a 5-fold improved half-life in vivo compared with THZ1; selectively targets CDK7 and potently inhibits the growth of triple-negative but not ER/PR+ breast cancer cells, efficiently suppresses the clonogenic growth of TNBC cells with IC50 of 10 nM; Like THZ1, THZ2 induces apoptotic cell death in triple-negative but not ER/PR+ breast cancer cells or normal human cells; suppresses the growth of triple-negative breast tumors in xenograft models.

PC-63139

TAK-931

1330782-76-7

TAK-931 (Simurosertib) is a potent, selective, ATP competitive and orally bioavailable inhibitor of Cdc7 with IC50 of <0.3 nM; prevents the initiation of DNA replication during mitosis, which causes cell cycle arrest and induces apoptosis, demonstrates antiproliferative activity with cancer cell lines and tumor growth inhibition (TGI) in murine ectopic xenograft models.

Colon Cancer

Phase 2 Clinical

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