2762181-19-9
Chemical Structure
MS83
- CAS No.: 2762181-19-9
- Formula:C52H55ClN10O8S2
- Molecular Weight:1047.64
IUPAC Name: ethyl (S)-3-(7-(2-(2-(2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamido)acetamido)ethoxy)-1-methyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(4-methyl-3-(((R)-4-methyl-1,1-dioxido-3,4-dihydro-2H-benzo[b][1,4,5]oxathiazepin-2-yl)methyl)phenyl)propanoate
InChIKey: IELFRNBYIDDQHB-QZNHJORUSA-N
SMILES: O=S1(C2=CC=CC=C2O[C@H](C)CN1CC3=CC([C@@H](C4=CC(OCCNC(CNC(C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5)=O)=O)=C(N(C)N=N9)C9=C4)CC(OCC)=O)=CC=C3C)=O
Biological Activity: MS83 is a selective degrader of BRD4/BRD3 belonging to the PROTAC class. MS83 hijacks the KEAP1-dependent CUL3 ligase complex by binding to KEAP1 and forming a ternary complex with BRD4/BRD3. MS83 induces polyubiquitination and degradation of BRD4/BRD3 in a concentration-, time- and ubiquitin-proteasome system-dependent manner. MS83 inhibits c-MYC protein levels and suppresses the proliferation of triple-negative breast cancer cells[1].
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MS83 | MS83 is a selective degrader of BRD4/BRD3 belonging to the PROTAC class. MS83 hijacks the KEAP1-dependent CUL3 ligase complex by binding to KEAP1 and forming a ternary complex with BRD4/BRD3. MS83 induces polyubiquitination and degradation of BRD4/BRD3 in a concentration-, time- and ubiquitin-proteasome system-dependent manner. MS83 inhibits c-MYC protein levels and suppresses the proliferation of triple-negative breast cancer cells. | |||||||||||||||||||||
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