CDK9 Inhibitor

VCC972839:01 is an inhibitor for cyclin dependent kinase (CDK9), with IC₅₀ of 7 nM. VCC972839:01 inhibits the cell viability of SCLC cells in nanomolar levels. VCC972839:01 induces apoptosis through an intrinsic pathway. VCC972839:01 exhibits antitumor activity in mouse model.

BLINK15 is a BBB-penetrant CDK5 inhibitor. BLINK15 lowers CDK5 activity for both complexes CDK5/p35 (IC₅₀ = 29.34 nM) and CDK5/p25 (IC₅₀ = 12.08 nM). BLINK15 offers anti-diabetic and neuroprotective benefits. BLINK15 lowers blood glucose, enhances cognition, and reduces neurodegeneration in T2D mice.

CDK9-IN-41 is a potent CDK9, EGFR, HER2, and COX-2 kinases inhibitor with IC₅₀s of 192.81 nM, 254.03 nM, 238.81 nM, and 775 nM. COX-2-IN-18 exhibits remarkable antitumor activity against leukemia cancer cells, colon cancer cells, melanoma cells, ovarian cells and breast cells.

SY-5102 is a potent, selective, and orally active cyclin-dependent kinase (CDK7) inhibitor with a K_d value of 0.03 nM. SY-5102 occupies the ATP-binding pocket of CDK7 via non-covalent binding to inhibit CDK7 activity, and downregulates its phosphorylation of cyclin CDK and RNA polymerase II. SY-5102 inhibits cancer cell proliferation, and induces tumor growth inhibition and regression. SY-5102 can be used in research related to triple-negative breast cancer.

ZLWT-37 is a potent, orally active CDKs inhibitor with IC₅₀ values of 0.002 μM and 0.054 μM against CDK9 and CDK2, respectively. ZLWT-37 induces apoptosis and arrests the cell cycle in the G2/M phase in HCT116 cells.

CDK7/9-IN-1 is a cyclin-dependent kinases 7/9 (CDK7/9) inhibitor. CDK7/9-IN-1 selectively inhibits CDK7 over CDK9. CDK7/9-IN-1 inhibits CDK7 with IC₅₀s of 0.0656 μM and 0.00574 μM without pre-incubation and after 3 hours pre-incubation, respectively. CDK7/9-IN-1 inhibits CDK9 with an IC₅₀ of 2.14 μM after 3 hours pre-incubation. CDK7/9-IN-1 can be used for the research of cancer.

CDK12-IN-4, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC₅₀ of 0.641 μM at high ATP (2 mM). CDK12-IN-4 has no effect on CDK2/Cyclin E (IC₅₀>20 μM) and CDK9/Cyclin T1 (IC₅₀>20 μM) at high ATP (2 mM) (WO2021116178A1).

CDK12-IN-9 is a potent and selective CDK12 inhibitor with an IC₅₀ of 2.2 nM. CDK12-IN-9 inhibits pSER2 (a downstream marker of CDK12/13 activity). CDK12-IN-9 can be used for the research of cancer.

CDK2-IN-28 (compound 22) is a CDK2 inhibitor with good selectivity and cellular effects against other CDKs. CDK2-IN-28 has anti-proliferative effects on MKN1 cells (EC50: 0.31 μM).

CDK9-IN-44 (Compound 7) is a selective CDK9 inhibitor (IC₅₀=7.6 μM). CDK9-IN-44 inhibits CDK9/cyclin T1 kinase activity, blocking transcriptional elongation, reducing the expression of pro-cancer proteins (such as MCL1, c-MYC), and inducing tumor cell apoptosis. CDK9-IN-44 is promising for research of glioblastoma (GBM) and central nervous system (CNS) disorders.

PROTAC CDK9 degrader-8 is a CDK9 PROTAC degrader that recruits cereblon. PROTAC CDK9 degrader-8 inhibits the growth of acute myeloid leukemia cells by inducing the degradation of CDK9 protein. PROTAC CDK9 degrader-8 can be used in studies related to CDK9-targeted degradation and acute myeloid leukemia.

CDK9-IN-32 (compound 006-3) is a CDK9 inhibitor.

CLZX-205 (compound C-7) is a selective inhibitor of CDK9, with the IC₅₀ of 2.9 nM. CLZX-205 plays an important role in cancer research.

CDK9-IN-23 (Example 4) is a CDK9 inhibitor with an IC₅₀ of <20 nM.

CDK-IN-9 (compound 24) is a potent CDK inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC₅₀ values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclin K and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNA polymerase II.

PROTAC CDK9 degrader-5 is a PROTAC targeting to CDK9 sepcifically. PROTAC CDK9 degrader-5 mediates CDK9 degradation via the proteasome. PROTAC CDK9 degrader-5 degrades CDK9 with DC₅₀s of 0.10 μM and 0.14 μM for the CDK9₄₂ and CDK9₅₅ isoforms, respectively.

CDK9/EZH2-IN-2 is a potent dual CDK9 and EZH2 inhibitor with an IC₅₀ of 8.9 nM against EZH2. CDK9/EZH2-IN-2 inhibits anti-apoptotic proteins and induces DNA damage by blocking the activity of CDK9 and EZH2, ultimately leading to tumor cell apoptosis. CDK9/EZH2-IN-2 can be used for research on diffuse large B-cell lymphoma.

HS-36 is a highly selective and orally active dual inhibitor of CDK4 and CDK9 with IC₅₀ values of 18.9 and 4.2 nM respectively. HS-36 exhibits nanomolar-level potent activity against various cancer cells, inducing G0/G1 phase arrest and promoting cell apoptosis. HS-36 efficiently inhibits tumor growth in a mouse model of MV-4-11 tumors. HS-36 can be used for the study of acute myeloid leukemia.

CDK6/9-IN-2 is a highly active dual inhibitor of CDK6 (IC₅₀ = 15 nM) and CDK9 (IC₅₀ = 22 nM). CDK6/9-IN-2 is selective for CDK2, CDK8, and CDK11. CDK6/9-IN-2 inhibits the proliferation of HaCaT cells induced by IFN-γ/TNF-α and suppresses the STAT3 pathway and the expression of inflammatory factors. CDK6/9-IN-2 can alleviate psoriatic dermatitis and is useful in psoriasis research.

LS-Q2 is a highly selective CDK4/9 inhibitor with IC₅₀ values of 1.4 nM and 6.2 nM. LS-Q2 inhibits cancer cells proliferation, induces G2/M phase arrest, apoptosis and reduces pSer2 RNA polymerase II expression. LS-Q2 interacts synergistically with BET and Bcl-2 inhibitors to drive antitumor activity. LS-Q2 can be used for the research of cancer, such as malignant solid tumors.