Bioactivity | PV1162 is a selective Chk2 inhibitor with an IC50 of 0.29 nM. PV1162 inhibits ATP binding to Chk2 by targeting the gatekeeper-dependent hydrophobic pocket, which is specific to Chk2 and located behind the ATP-binding site (adenine-binding region), thereby inhibiting the phosphorylation activity of Chk2. PV1162 holds potential application value in the field of cancer therapy[1]. |
CAS | 1093793-11-3 |
Formula | C21H24N6O2 |
Molar Mass | 392.45 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Lountos GT, et al. X-ray structures of checkpoint kinase 2 in complex with inhibitors that target its gatekeeper-dependent hydrophobic pocket. FEBS Lett. 2011 Oct 20;585(20):3245-9. |