MD-4251

MD-4251 potently inhibits the growth of wild-type p53 acute leukemia cell lines RS4;11 (IC₅₀ = 1 nM), MV4;11 (IC₅₀ = 2 nM), and MOLM-13 (IC₅₀ = 2 nM), while showing minimal activity against the mutated p53 cell line RS4;11/IRMI2 (IC₅₀ > 1000 nM)^[1].
MD-4251 (≥3 nM; 2 h) degrades MDM2 in RS4;11 cells with a DC₅₀ of 0.2 nM and 96% maximal degradation within 2 h, while increasing p53 protein levels by over 6-fold at concentrations of 3 nM or higher^[1].
MD-4251 upregulates p53, DSC1, NBEA, and CASP14 protein levels in MV4;11 and MOLM-13 cells, with no detectable MDM2 depletion due to low baseline MDM2 expression^[1].
MD-4251 (0.03-300 nM; 2 h) potently degrades MDM2 with a DC₅₀ of 0.2 nM and D_max of 96% in RS4;11 cells after 2 h, accompanied by robust p53 upregulation, while showing minimal effects on other cereblon neo-substrates^[2].
MD-4251 (Serial dilutions; 4 days) inhibits RS4;11 cell growth with an IC₅₀ of 1 nM, and this activity is dependent on cereblon binding^[2].
MD-4251 (Serial dilutions; 4 days) inhibits MV4;11 cell growth with an IC₅₀ of 2 nM^[2].
MD-4251 (Serial dilutions; 4 days) inhibits MOLM-13 cell growth with an IC₅₀ of 2 nM^[2].
MD-4251 (3 nM; 2 h) upregulates p53 and three additional proteins (DSC1, NBEA, CASP14) in RS4;11 cells, with no protein depleted by more than 2-fold^[2].
MD-4251 exhibits excellent metabolic stability in liver microsomes and plasma from multiple species, with a half-life exceeding 60 min across all tested samples^[1].
MD-4251 (1 μM; Up to 60 min) demonstrates excellent microsomal and plasma stability (T_1/2 >60 min) in human, mouse, rat, dog, and monkey samples^[2].

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