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 ; Blue: E3 ligase ligand (HY-125845) ; Black: linker).
Product Specifications
CAS Number
2376137-41-4
UNSPSC
12352005
Target
Akt; PROTACs
Type
Reference compound
Related Pathways
PI3K/Akt/mTOR; PROTAC
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/ms143.html
Solubility
10 mM in DMSO
Smiles
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
Molecular Formula
C59H81ClN12O6S
Molecular Weight
1121.87
References & Citations
[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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
Frequently Asked Questions
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