KMG-1068

KMG-1068 (compound 4a) (serial concentrations; 72 h) potently inhibits the proliferation of HEK293T, Jurkat and various solid tumor cell lines in a Cullin-RING ligase-dependent manner, with a GI₅₀ range of 0.2 μM to 0.8 μM in the absence of MLN4924^[1].
KMG-1068 (72 h) exerts antiproliferative effects on HEK293T cells in a CUL4-dependent manner, and the GI50 value rises by 4-fold in CUL4-knockdown cells relative to control cells, which verifies this regulatory relationship^[1].
KMG-1068 forms a ternary complex with CRBN and GSPT1 in HEK293T cells, with an EC₅₀ of 11.4 μM; it induces proximity-dependent interaction between CRBN and GSPT1/2 in Mia-paca2 cells^[1].
KMG-1068 (0-10 μM; 6 h) induces dose-dependent degradation of GSPT1 and GSPT2 in Jurkat cells, with DC₅₀ values of 126.7 nM and 42.2 nM, respectively; this degradation is proteasome-dependent^[1].
KMG-1068 (1 μM; 6 h) induces GSPT1 degradation in HEK293T cells, and this degradation effect relies on CUL4-containing Cullin-RING ligase complex^[1].
KMG-1068 (0-10 μM; 24 h) triggers GSPT1 degradation in MEF cells, and this degradation relies on binding to CRBN's tryptophan triad pocket; the effect is totally lost in cells with CRBN^W386A mutant^[1].

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