MS5033

MS5033 (2 μM; 12 h) induces formation of the AKT-MS5033-CRBN ternary complex in E. coli-expressing HEK 293T cells, as measured by EGFP-based BiFC fluorescence^[1].
MS5033 (2 μM; 12 h) induces formation of the AKT-MS5033-mutant CRBN ternary complex in mEAEC-expressing HEK 293T cells, as measured by EGFP-based BiFC fluorescence, without causing degradation of the reporter's AKT fusion protein^[1].
MS5033 (2 μM; 24 h) induces degradation of the NLuc-AKT fusion protein in LALC-expressing HEK 293T cells, as measured by Western blotting, with residual protein levels at 0.45-fold of the DMSO control^[1].
MS5033 (Compound 35) binds with high affinity to AKT1 and AKT3, and moderate affinity to AKT2 purified protein isoforms, with K_d values of 4.8 nM, 22 nM, and 160 nM, respectively^[3].
MS5033 (Compound 62) inhibits purified AKT1, AKT2, and AKT3 kinases with IC₅₀ values of 798 nM, 90 nM, and 544 nM, respectively^[2].
MS5033 (30 nM-10 μM; 4-24 h) induces potent, time- and concentration-dependent, VHL- and ubiquitin-proteasome system-dependent AKT degradation in SW620 KRAS^G12C mutant colorectal cancer cells with a DC₅₀ of 23 nM^[2].
MS5033 (100 nM-1 μM) effectively induces AKT degradation in KRAS/BRAF mutant cancer cells (Colo205, HT-29, SKMEL 239, PANC-1) at 1 μM, with complete degradation in PANC-1 cells at 100 nM, and modest activity in Mia PaCa-2 cells^[2].
MS5033 (1 μM; 18 h) acts as a selective AKT degrader in SW620 KRAS^G12D colorectal cancer cells, significantly reducing AKT1 and AKT2 protein levels with no substantial off-target degradation^[2].
MS5033 effectively inhibits colony formation in PC3 PI3K/PTEN pathway mutant prostate cancer cells with potency comparable to related AKT PROTACs^[2].
MS5033 (1-10 μM; 24 h) induces robust AKT degradation and downstream signaling inhibition in BT474 human breast cancer cells^[3].
MS5033 (1 μM; 24 h) induces concentration-dependent AKT degradation in PC3 human prostate cancer cells with a DC₅₀ of 430 nM, acting via a cereblon (CRBN)- and ubiquitin-proteasome system (UPS)-dependent mechanism, and reaches maximum degradation^[3].
MS5033 (3-5 days) inhibits proliferation of PC3 human prostate cancer cells with a GI₅₀ of 10.8 μM and MDA-MB-468 human triple-negative breast cancer cells with a GI₅₀ of 4.8 μM^[3].
MS5033 inhibits proliferation of SW620 KRAS^G12C mutant colorectal cancer cells with a GI₅₀ of 3.1 μM, induces apoptosis, and suppresses colony formation, with activity dependent on AKT degradation^[2].

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