2375564-54-6
Chemical Structure
PROTAC SMARCA2/4 degrader-27
- CAS No.: 2375564-54-6
- Formula:C49H58FN9O6S
- Molecular Weight:920.10
InChIKey: UTZVLJZPTDCKCT-XBPZXCMESA-N
SMILES: O=C(C1(CC1)F)N[C@@H](C(C)(C)C)C(N2[C@@H](C[C@H](C2)O)C(NCC3=C(C=C(C4=C(C)N=CS4)C=C3)OCCC5=CC=C(C=C5)CN6CCN(C7=C(N)N=NC(C8=C(C=CC=C8)O)=C7)CC6)=O)=O
Biological Activity: PROTAC SMARCA2/4 degrader-27 is a VHL-recruiting PROTAC degrader targeting SMARCA2 and SMARCA4, derived from structure-guided modification of PROTAC SMARCA2/4 degrader-28 (HY-162835). PROTAC SMARCA2/4-degrader-27 forms a cooperative ternary complex with CRL2VHL E3 ligase to induce ubiquitination and degradation. PROTAC SMARCA2/4-degrader-27 induces a novel protein-protein interaction between VHL and SMARCA2/SMARCA4, thereby stabilizing ternary complex formation and promoting proteasomal degradation of target proteins. PROTAC SMARCA2/4-degrader-27 exhibits enhanced cell permeability and stronger ternary complex formation ability, leading to improved degradation activity. PROTAC SMARCA2/4-degrader-27 can be used in cancer-related research[1].
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PROTAC SMARCA2/4 degrader-27 | PROTAC SMARCA2/4 degrader-27 is a VHL-recruiting PROTAC degrader targeting SMARCA2 and SMARCA4, derived from structure-guided modification of PROTAC SMARCA2/4 degrader-28 (HY-162835). PROTAC SMARCA2/4-degrader-27 forms a cooperative ternary complex with CRL2VHL E3 ligase to induce ubiquitination and degradation. PROTAC SMARCA2/4-degrader-27 induces a novel protein-protein interaction between VHL and SMARCA2/SMARCA4, thereby stabilizing ternary complex formation and promoting proteasomal degradation of target proteins. PROTAC SMARCA2/4-degrader-27 exhibits enhanced cell permeability and stronger ternary complex formation ability, leading to improved degradation activity. PROTAC SMARCA2/4-degrader-27 can be used in cancer-related research. | |||||||||||||||||||||
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