CCT241533-DataSheet-生命科学试剂-MedChemExpress.pdf

Hotline: 400-820-3792 Inhibitors • Screening Libraries • Proteins www.MedChemE CCT241533 Cat. No.: HY-14715 CAS No.: 1262849-73-9 分⼦式: C₂₃H₂₇FN₄O₄ 分⼦量: 442.48 作⽤靶点: Checkpoint Kinase (Chk) 作⽤通路: Cell Cycle/DNA Damage 储存⽅式: Please store the product under the recommended conditions in the Certificate of Analysis. BIOLOGICAL ACTIVITY ⽣物活性 CCT241533 是有效，选择性的 CHK2 抑制剂，IC50 和 Ki 分别为 3 nM 和 1.16 nM [1]。 IC50 Target Chk2 Chk1 Chk2 3 nM (IC50) 245 nM (IC50) 1.16 nM (Ki) 体外研究 CCT241533 hydrochloride inhibits CHK2 with an IC50 of 3 nM and shows minimal cross reactivity against a panel of kinases at 1 μM. X-ray crystallography confirms that CCT241533 binds to CHK2 in the ATP pocket. CCT241533 blocks CHK2 activity in human tumor cell lines in response to DNA damage, as demonstrated by inhibition of CHK2 autophosphorylation at S516, band-shift mobility changes and HDMX degradation. CCT241533 does not potentiate the cytotoxicity of a selection of genotoxic agents in several cell lines. However, CCT241533 significantly potentiates the cytotoxicity of two structurally distinct PARP inhibitors. Clear induction of t