MS143 

MS143 is a potent PROTAC AKT degrader (DC₅₀=46 nM and GI₅₀=0.8 μM in PC3 cells). MS143 induces rapid and robust AKT degradation in a concentration- and time-dependent manner via hijacking the ubiquitin-proteasome system. MS143 can suppress cancer cell growth (Pink: AKT ligand (HY-15431); Blue: E3 ligase ligand (HY-125845); Black: linker)^[1].

AKT

MS143 (1 nM-10 μM; 24 hours) induces T-AKT degradation with a concentration-dependent manner in PC3 cells^[1].
MS143 (0.1-10 μM;14 days, replenish every 2 days) effectively inhibits colony formation in BT474 cells^[1].
MS143 (1 μM; 24 hours) promotes AKT degradation in an E3 ligase- and UPS-dependent manner^[1].
MS143 (1 nM-10 μM) can inhibit the cell growth of PC3 cells (GI₅₀=0.8 nM) and MDA-MB-468 cells (GI₅₀=1.0 nM)^[1].

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

MS143 (75 mg/kg; i.p., 22 days) drastically inhibits the tumor growth by 92%, also substantially degrades T-AKT and P-AKT, and effectively inhibits the downstream signaling (PRAS40 phosphorylation) in xenograft mice^[1].
Pharmacokinetic Parameters of MS143 in male Swiss Albino mice^[1].

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

1121.87

C₅₉H₈₁ClN₁₂O₆S

2376137-41-4

O=C(N1[C@@H](C[C@H](C1)O)C(NCC2=CC=C(C3=C(N=CS3)C)C=C2)=O)[C@H](C(C)(C)C)NC(CCCCCCCCCCC(N(CC4)CCN4CC[C@@H](C5=CC=C(C=C5)Cl)NC(C6(CCN(CC6)C7=C8C(NC=C8)=NC=N7)N)=O)=O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Yu X, et al. Discovery of Potent, Selective, and In Vivo Efficacious AKT Kinase Protein Degraders via Structure-Activity Relationship Studies. J Med Chem. 2022;65(4):3644-3666.  [Content Brief]