CDK2-IN-12

CDK2-IN-12 (compound 10b) is a potent CDK2 inhibitor, with an IC50 of 11.6 μM. CDK2-IN-12 inhibits hCA (carbonic anhydrase) isoforms I, II, IX and XII, with KI values of 3534, 638.4, 44.3, and 48.8 nM. CDK2-IN-12 shows anticancer activity[1].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> CDK

Signaling Pathways >> Metabolic Enzyme/Protease >> Carbonic Anhydrase

CDK2:11.6 μM (IC50)

CDK9:>12.5 μM (IC50)

CDK2-IN-12 (compound 10b) exerts outstanding anti-proliferative activity against leukemia (CCRF-CEM, HL-60TB, K-562 and MOLT-4), non-small cell lung cancer (HOP-92), colon cancer (COLO 205, HCT-116 and SW-620), renal (ACHN) and breast (MDA-MB-468) cell lines with GI% (percentage growth inhibition) ranging from 80 to 100%[1]. CDK2-IN-12 displays much enhanced growth inhibitory activity, under normoxic and hypoxic conditions, against MDA-MB-468 (IC50 = 1.37 ± 0.07 and 3.03 ± 0.11 μM) than MCF-7 cells (IC50 = 6.80 ± 0.17 and 15.10 ± 0.82 μM)[1].

[1]. Said MA, et al. Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation. Eur J Med Chem. 2020 Mar 1;189:112019.