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Cat. No. Product Name CAS No. Information
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-62561

CCT 068127

660822-23-1

CCT 068127 (CCT 68127) is a novel potent inhibitor of CDK2 and CDK9 with IC50 of 10 and 90 nM for CDK2/E and CDK9/T, respectively; also inhibits CDK5/p35, CDK2/A, CDK7/H with IC50 of <1 uM, but without significant activity against ABL, AKT, CAMKII, CK2, ERK2, GSK3 etc.; causes a dramatic loss in expression of DUSP6 phosphatase, alongside elevated ERK phosphorylation and activation of MAPK pathway target genes in cancer cells.

PC-62534

IIIM-290

2213468-64-3

IIIM-290 is a potent, orally active cyclin-dependent kinase (CDK) inhiitor with IC50 of 1.9 and 16 nM for Cdk-9/T1 and Cdk-2/A, respectively; selectively inhibits Molt-4/MIAPaCa-2 cell growth with GI50 of <1 uM; inhibits the cell growth of MIAPaCa-2 cells via caspase-dependent apoptosis, demonstrates in vivo efficacy in pancreatic, colon, and leukemia xenografts at 50 mg/kg, po., without CYP/efflux-pump liability, and mutagenic/genotoxic or cardiotoxic effects.

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