cdk9/cyclint1

CAN508 is a potent ATP-competitive CDK9 cyclin T1 inhibitor with an IC50 of 0.35 μM. It also competitively inhibits Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 μM and 20 μM, respectively. CAN508 exhibits a 38-fold selectivity for CDK9 cyclin T over other CDK cyclin complexes. [Antitumor activity.]

MC180295 ((rel)-MC180295) is a novel, potent, and highly selective CDK9 inhibitor with an IC50 of 5 nM, demonstrating over 22-fold selectivity compared to other CDKs.

Riviciclib hydrochloride (P276-00) is a novel inhibitor of CDK1, CDK4, and CDK9, with IC50 values of 79 nM, 63 nM, and 20 nM, respectively, currently in Phase 2 3.

RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM 2 nM 3 nM 4 nM 5 nM for cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2 cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 respectively; less potent against cyclin H-CDK7 and cyclin D3-CDK6.

CDK9-IN-7 is a highly selective and orally active CDK9 cyclin T inhibitor (IC50: 11 nM), which exhibits more potent over other CDKs (CDK4 cyclinD: 148 nM; CDK6 cyclinD: 145 nM).

NVP-LCQ195 (LCQ-195) (AT9311) is a potent inhibitor of CDK1, CDK2, CDK3 and CDK5 (IC50: 1-42 nM).

Abemaciclib (LY2835219) is a dual inhibitor of CDK4 6 (IC50=2 10 nM) with selectivity and specificity. Abemaciclib has antitumor activity and is used to treat advanced or metastatic breast cancer.

Abemaciclib methanesulfonate (LY2835219) is a specific and effective inhibitor of CDK4(IC50=2 nM) and CDK6(IC50=10 nM).

Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 578 nM), CDK5 and CDK9 respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride has anti-tumor effects.

Bohemine is a cyclin-dependent kinase inhibitor.

PHA-793887 has been used in trials studying the treatment of Advanced Metastatic Solid Tumors.

Voruciclib is an orally active and selective CDK inhibitor (Ki: 0.626 nM-9.1 nM) that represses the expression of MCL-1 in multiple models of diffuse large B-cell lymphoma and effectively blocks CDK9, the transcriptional regulator of MCL-1.

(R)-Atuveciclib is an isomer of Atuveciclib. Atuveciclib (BAY 1143572) is a potent and highly selective PTEFb CDK9 inhibitor with an IC50 value of 13 nm for CDK9 CycT1 and a selectivity ratio of 100 for CDK2, with highly bioavailable and orally available advantages.

Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) is a potent and selective CDK9 inhibitor, inhibiting CDK9 CycT1 with an IC50 of 16 nM.

CDK9-IN-1 is a selective and potent CDK9 inhibitor with antiviral activity used in the study of PRRSV infections.

IIIM-290 is an oral CDK inhibitor (IC50s: 90 and 94 nM for CDK2 A and CDK9 T1).

(R)-CR8 trihydrochloride (CR8, (R)-Isomer trihydrochloride) is a CDK1 2 5 7 9 inhibitor that acts as a molecular glue degrader with neuroprotective activity and induces apoptosis.

Riviciclib is a potent inhibitor of cyclin-dependent kinase (CDK)(CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively),with antitumor activity on cisplatin-resistant cells.

Voruciclib hydrochloride is an orally active and selective CDK inhibitor with a Ki range of 0.626 nM to 9.1 nM.

CDK12-IN-E9 is a cell cycle protein kinase (CDK) inhibitor with anticancer and antitumor activity that can be used in the study of breast cancer.

Roniciclib (BAY 1000394) is a potent pan-CDK inhibitor and a novel oral cytotoxic agent. Roniciclib inhibits the activity of cell-cycle CDKs CDK1, CDK2, CDK3, CDK4, and of transcriptional CDKs CDK7 and CDK9 with IC(50) values in the range between 5 and 25 nmol L.

Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycetes, functioning as an XBP1 inhibitor and inhibiting IRE1α-induced ATP-dependent XBP1 mRNA cleavage (IC50: 80 nM), and induces apoptosis.

CDK9-IN-35 (compound 10j) acts as an inhibitor of CDK9 CyclinT1, exhibiting an IC50 of 10.2 nM. It also shows an IC50 of 20 nM against the HCT-116 cell line.

TMX-2138 is a CDKs PROTAC degrader, with IC50 values of 8.7 nM for CDK1 cyclinB, 10.9 nM for CDK2 cyclinA, 7.0 nM for CDK5 p25, and 25.7 nM for CDK9 cyclinT1. It enhances the ubiquitination and degradation of CDKs and is utilized for ovarian cancer research.