CDK16 Inhibitor

Tambiciclib (GFH009, JSH-009) is an orally active, highly potent and selective CDK9 inhibitor (IC₅₀ = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over DYRK1A/B, and excellent selectivity over 468 kinases/mutants. Tambiciclib demonstrates potent in vitro and in vivo antileukemic efficacy in acute myeloid leukemia (AML) mouse models by inhibiting RNA Pol II phosphorylation, downregulating MCL1 and MYC, and inducing apoptosis. Tambiciclib can be used for AML research.

JSH-150 is a highly selective and potent CDK9 inhibitor with an IC₅₀ of 1 nM.

CDK16/CycY-IN-1 is a CDK16/CycY inhibitor (IC₅₀ = 125.2 nM) and also inhibits CDK6/CycD1, CDK9/CycT1, and CDK4/CycD3. CDK16/CycY-IN-1 exhibits anti-tumor cell proliferation activity, inhibits colony formation, migration, and p53 Ser315 phosphorylation, and induces S-phase cell cycle accumulation and apoptosis. CDK16/CycY-IN-1 shows anti-tumor activity in the H460 xenograft tumor model. CDK16/CycY-IN-1 can be used for research on non-small cell lung cancer (NSCLC).

Tambiciclib (GFH009, JSH-009) dimaleate is an orally active, highly potent and selective CDK9 inhibitor (IC₅₀ = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over DYRK1A/B, and excellent selectivity over 468 kinases/mutants. Tambiciclib dimaleate demonstrates potent in vitro and in vivo antileukemic efficacy in acute myeloid leukemia (AML) mouse models by inhibiting RNA Pol II phosphorylation, downregulating MCL1 and MYC, and inducing apoptosis. Tambiciclib dimaleate can be used for AML research.

JA397, a chemical probe, is a potent and selective inhibitor for the TAIRE family with cellular activity ranging from IC₅₀ values of 21 nM to 307 nM.

FLT3/ITD-IN-4 (Compound 16) is a selective FMS-like tyrosine kinase 3 internal tandem duplications (FLT3-ITD) inhibitor with an IC₅₀ of 2.3 nM. FLT3/ITD-IN-4 can be used for acute myeloid leukemia research.