MRT00033659

MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 ( IC 50 =0.9 µM for CK1δ) and CHK1 ( IC 50 =0.23 µM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation In Vitro MRT00033659 (5-40 µM; 48 hours) is sufficient to significantly reduce cell number of 5 µM. MRT00033659 (1-80 µM; 48 hours) induces substantial cell death from 5 µM. MRT00033659 (0.2-80 µM; 48 hours) induces a robust and sustained stabilisation of p53, MDM2 and p21 proteins, as well as E2F-1 destabilisation from 0.2 µM to 5 µM. MRT00033659 does not inhibit p38α MAPK. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: A375 cells Concentration: 5, 20, 40 µM Incubation Time: 48 hours Result: Significantly reduced cell number of 5 µM. Apoptosis AnalysisCell Line: A375 cells Concentration: 1, 5, 10, 20, 40, 80 µM Incubation Time: 48 hours Result: Induced substantial cell death from 5 µM. Western Blot AnalysisCell Line: A375 cells Concentration: 0.2, 1, 5, 10, 20, 40, 80 µM Incubation Time: 48 hours Result: Induced a robust and sustained stabilisation of p53, MDM2 and p21 proteins, as well as E2F-1 destabilisation from 0.2 µM to 5 µM. Form:Solid IC50& Target:CKIδ 0.9 μM (IC 50 ) Chk1 0.23 μM (IC 50 )

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