JAK1/CDK7-IN-1

JAK1/CDK7-IN-1 (Compound 11) (24 h) potently inhibits the proliferation of MCF-7, MDA-MB-231, and PC-3 cancer cells with IC₅₀ values of 2.85, 4.61, and 7.69 µM respectively, and demonstrates selective toxicity toward cancer cells over normal WI-38 cells^[1].
JAK1/CDK7-IN-1 potently inhibits JAK1 enzyme activity in MCF-7, MDA-MB-231, and PC-3 cells with IC₅₀ values of 0.017, 0.01, and 0.10 µM respectively^[1].
JAK1/CDK7-IN-1 inhibits CDK7 enzyme activity by 80.7% in MCF-7 cells, 68.1% in MDA-MB-231 cells, and 83.4% in PC-3 cells^[1].
JAK1/CDK7-IN-1 upregulates apoptosis-associated caspase levels in cancer cells, with 4.60-, 3.03-, and 2.69-fold increases in caspase-1, -3, and -9 respectively in MDA-MB-231 cells, a 3.50-fold increase in caspase-1 in PC-3 cells, and 2.87- and 1.08-fold increases in caspase-1 and -9 respectively in MCF-7 cells^[1].
JAK1/CDK7-IN-1 induces G₂/M phase cell cycle arrest and pre-G₁ apoptosis in MCF-7 cells, increasing G₂/M phase cells to 35.03% and pre-G₁ phase cells to 20.68%^[1].
JAK1/CDK7-IN-1 significantly induces apoptosis and necrosis in MCF-7 cells, increasing total apoptosis to 10.92% and necrosis to 3.47%^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.