cdk9

CDK9-IN-9 is a potent and selective CDK9 inhibitor (IC50: 1.8 nM) with anti-cancer activity. It inhibits CDK2 (IC50: 155 nM).

CDK9-IN-2 is a specific CDK9 inhibitor with an IC50 of 5 nM in the A2058 skin cell line (72 hours) and 7 nM in the H929 multiple myeloma cell line (72 hours).

CDK9-IN-8 is a highly potent and selective CDK9 inhibitor (IC50: 12 nM).

CDK9-IN-10 is a potent inhibitor of CDK9 and serves as the ligand for the PROTAC CDK9 degrader-2.

CDK9 inhibitor HH1 (8019-9719) is an inhibitor of the human CDK2-cyclin A2 complex with an IC50 value of 2 μM.

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).

CDK9-IN-30 is one of the Tat peptide derivatives and inhibits HIV-1 long terminal repeat-activated transcription.

CDK9 Antagonist-1 (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[1]. CDK9|17 μM (IC50, MCF-7 cells) [1]. Bian J , et al. Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity. Bioorg Chem. 2018 Dec;81:373-381.

PROTAC CDK9 Degrader-8 (Compound 21) is a potent degrader of CDK9 with an IC50 of 0.01 μM, utilized in cancer research [1].

CDK9-IN-24 (compound 21a) is a potent and selective CDK9 inhibitor that significantly inhibits tumor proliferation, impedes cell growth, and triggers apoptosis via downregulation of Mcl-1 and c-Myc, making it valuable for acute myeloid leukemia research [1].

PROTAC CDK9 CycT1 Degrader-1 (compounds 10), a potent CDK9 inhibitor and target protein ligand for PROTAC synthesis, exhibits substantial anti-proliferative activity in solid tumors [1], making it instrumental in the targeted degradation of CDK9 CycT1.

PROTAC CDK9 degrader-7 is a proteolysis-targeting chimera (PROTAC) engineered to selectively target and mediate the degradation of Cyclin-Dependent Kinase 9 (CDK9) via the proteasome pathway [1].

PROTAC CDK9 degrader-5 is a selective PROTAC that mediates degradation of CDK9 via the proteasome pathway, efficiently degrading CDK9 42 and CDK9 55 isoforms with DC50 values of 0.10 μM and 0.14 μM, respectively [1].

CDK9-IN-11 is a potent CDK9 inhibitor and serves as the ligand for the PROTAC CDK9 Degrader-1 [1].

PROTAC CDK9 degrader-4 is a potent and efficacious compound designed to degrade CDK9, a protein involved in transcription regulation, thereby modulating transcriptional activity by effectively targeting and reducing CDK9 levels.

CDK9/10/GSK3β-IN-1 is a kinase inhibitor (Flavopiridol analogue) that effectively inhibits HsGSK3β, HsCDK9/CyclinT, HsCDK5/p25 and HsCDK2/CyclinA with IC50 values of 59 nM, 64 nM, 1.093 μM and 1.725 μM, respectively. CDK9/10/GSK3β-IN-1 exhibited comparable or higher anti-cancer cell activity than Flavopiridol and showed high anti-proliferative activity against up to seven cancer cell lines in vitro.

PROTAC CDK9 degrader-6 is a specific PROTAC targeting CDK9 for degradation via the proteasome pathway, effectively degrading CDK9 with DC50 values of 0.10 μM and 0.14 μM for the CDK9 42 and CDK9 55 isoforms, respectively [1].

CDK9/CycT1-IN-93 is a highly specific, ATP-competitive inhibitor of CDK9/CycT1 with antiviral activity.

CDK9-IN-12 exhibits optimal CDK9 inhibitory activity with an IC50 value of 5.41 nM.

CDK9-IN-27 (Compound 6a), a CDK9 inhibitor with an IC50 of 0.424 μM, induces apoptosis and S-phase cell cycle arrest. It exhibits cytotoxicity against HepG2, HCT-116, and MCF-7 cell lines, with IC50 values ranging from 10.31 to 40.34 μM, rendering it applicable in cancer research [1].

CDK9-IN-19 is a selective and potent CDK9 inhibitor (IC50: 2.0 nM). CDK9-IN-19 exhibits good anti-proliferative activity in cancer cells, moderate pharmacokinetic properties and low hERG inhibition. CDK9-IN-19 significantly inhibited tumor growth in the MV4-11 xenograft mouse model. CDK9-IN-19 can be used in studies of acute myeloid leukemia (AML).

CDK9-IN-14 is a potent, high and low selective CDK9 inhibitor (IC50: 6.92 nM). CDK9-IN-14 is a strong inhibitor of MV-4-11 cells and in vivo tumour models with low toxicity and few side effects.

PROTAC FLT3/CDK9 degrader-1, a potent dual degrader of FLT3 and CDK9, effectively induces apoptosis and targets protein degradation of FLT3 and CDK9. This compound holds research potential for FLT3-ITD mutated AML [1].

CDK9-IN-13 is a potent and selective CDK inhibitor (IC50<3 nM). CDK9-IN-13 has a very short half-life in rodents.

CDK9-IN-1 is a novel, selective CDK9 inhibitor for the treatment of HIV infection [IC50: 39 nM for CDK9 CycT1].

CDK9-IN-15 is a potent small molecule CDK9 inhibitor, which can block the phosphorylation of positive transcription elongation factor b (P-TEFb) on the C-terminal region of RNA Poly-II by degradation and inhibition of CDK9, inhibit transcription, and rapidly reduce the level of intracellular mRNA, thereby causing apoptosis of tumor cells.

CDK9-IN-23 (Example 4) is a highly potent CDK9 inhibitor with an IC50 value below 20 nM [1].

CDK9-IN-25 (compound 4a), an imidazopyrazine derivative, functions as a CDK9 inhibitor with an IC50 of 0.24 μM. It also exhibits affinity for the main protease of COVID-19 and demonstrates antiviral activity against human coronavirus 229E, with an IC50 of 63.28 μM [1].

EGFR HER2 CDK9-IN-3 (Compound 10) is a potent inhibitor of EGFR (IC50:191.08 nM), HER2 (IC50:132.65 nM), and CDK9 (IC50:113.98 nM), demonstrating significant anti-tumor effects.

PROTAC CDK9 ligand-1, a CDK9 ligand, is used in the synthesis of PROTACs.

CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective inhibitor of the CDK9-Cyclin T1 protein-protein interaction (PPI), suppressing cell proliferation in TNBC MDA-MB-231 cells with an IC50 of 0.044 μM and inducing apoptosis. This compound diminishes CDK9 transcriptional activity and downregulates phosphorylation of RNA Pol II CTD ser2. In vivo, CDK9-Cyclin T1 PPI-IN-1 effectively impedes tumor growth in a TNBC 4T1 mouse model [1].

PROTAC CDK9 Degrader-1 is a selective degrader of cyclin-dependent kinase 9 (CDK9).

CDK9-IN-26, also known as compound 1, is a potent inhibitor of Cyclin-Dependent Kinase 9 (CDK9) with an IC50 value of 0.18 μM.[1]

PROTAC CDK9/CycT1 Degrader-2 inhibits CDK9 with an IC50 of 45 nM [1].

EGFR/HER2/CDK9-IN-2 are potent inhibitors of EGFR/HER2/CDK9, and they exhibited significant antitumor effects with IC50s of 145.35, 129.07 and 117.13 nM, respectively.

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[1].

CDK9-IN-18, a potent inhibitor of CDK9, blocks its phosphorylation, exhibits good anticancer activity, induces apoptosis, and has low cellular activity.

EGFR HER2 CDK9-IN-1 (Compound 4) is a potent inhibitor of EGFR, HER2, and CDK9, with IC50 values of 90.17 nM, 131.39 nM, and 67.04 nM, respectively, and exhibits significant anti-tumor effects.

CDK9-IN-29 (compound Z11) is a potent CDK9 inhibitor, demonstrating high kinase selectivity with an IC50 of 3.20 nM, effectively hindering cell proliferation and inducing apoptosis [1].

CDK-IN-9 (compound 24) is a potent inhibitor of CDK and acts on CDK2 E (IC50: 4 nM). It functions as a molecular gel that induces interaction between CDK12 and DDB1, and can dephosphorylate retinoblastoma protein and RNA polymerase II, thereby inducing apoptosis.

SY-5609 is a selective and noncovalent inhibitor of CDK7(KD = 0.065 nM) with antitumor activity and inhibits apoptosis.

SEL120-34A is a selective and ATP-competitive inhibitor of CDK8 with IC50s of 4.4 nM, 10.4 nM and 1070 nM for CDK8/CycC, CDK19/CycC and CDK9/cycT. SEL120-34A possesses antitumor activity.

PHA-767491 (CAY10572) is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively.

(S)-Enitociclib (VIP152) is a selective CDK9 inhibitor that induces complete regression of MYC+ lymphomas by inhibiting RNA polymerase II-mediated transcription of anti-apoptotic and pro-survival proteins.

GW297361 is a potent inhibitor of the cell cycle protein-dependent kinase Cdk1 and also inhibits the Pho85 signaling pathway.The IC50s of GW297361 on yeast Cdk1 and Pho85 were 20 nM and 400 nM, respectively.

(R)-Enitociclib, an enantiomer of BAY-1251152, is a CDK9 inhibitor with anticancer activity.

BUR1 is a selective BMP upregulator that acts by increasing the expression of Inhibitor of DNA binding 1 and inducing BMP2 and PTGS2 expression.

SEL120-34A HCl is a selective, orally available and ATP-competitive inhibitor of CDK8(CDK8/CycC and CDK19/CycC with IC50s of 4.4 nM and 10.4 nM , respectively), with antitumor activity.

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