2768610-97-3
Chemical Structure
MS41
- No. CAS: 2768610-97-3
- Formula:C56H70N8O9S
- Molecular Weight:1031.27
InChIKey: XPICNVKPGAOVBF-VCNVHFLLSA-N
SMILES: CC1=C(SC=N1)C2=CC=C(C=C2)[C@@H](NC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(CCCCCCCCCNC(C4=CC=C5CC[C@H](C5=C4)NC(C6=NOC(C7=CC(O)=C(C=C7)C(N(C)C)=O)=C6)=O)=O)=O)=O)O)=O)C
Biological Activity: MS41 is a selective ENL PROTAC degrader with DC50 values of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat) and 26.58 nM (KASUMI1), respectively. MS41 recruits the VHL E3 ubiquitin ligase, induces ubiquitination and degradation of ENL (including mutant ENL carrying mutations in the YEATS domain), and reduces the chromatin occupancy of ENL-associated transcription elongation complexes. MS41 induces G1 phase cell cycle arrest and Apoptosis. MS41 inhibits leukemia progression in xenograft models. MS41 can be used in research related to mixed lineage leukemia-rearranged leukemia and Wilms tumor[1].
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MS41 | 98.97% | MS41 is a selective ENL PROTAC degrader with DC50 values of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat) and 26.58 nM (KASUMI1), respectively. MS41 recruits the VHL E3 ubiquitin ligase, induces ubiquitination and degradation of ENL (including mutant ENL carrying mutations in the YEATS domain), and reduces the chromatin occupancy of ENL-associated transcription elongation complexes. MS41 induces G1 phase cell cycle arrest and Apoptosis. MS41 inhibits leukemia progression in xenograft models. MS41 can be used in research related to mixed lineage leukemia-rearranged leukemia and Wilms tumor. | ||||||||||||||||||||
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Keywords
