3033586-04-5
Chemical Structure
SMD-1087
- CAS No.: 3033586-04-5
- Formula:C56H68ClN7O5S
- Molecular Weight:986.70
InChIKey: VHTCCGAJVGXIRY-RZMWLZPDSA-N
SMILES: C[C@H](NC([C@@H]1C[C@H](CN1C([C@@H](NC([C@@H]2CC[C@H](CC2)CN3CCC(CC3)C4=CC(N5C6=C7C(Cl)=CC=C6)=C(C=C4)C8(CCCCC8)C5=NC7=O)=O)C(C)(C)C)=O)O)=O)C9=CC=C(C=C9)C%10=C(C)N=CS%10
Biological Activity: SMD-1087 is a VHL-recruiting SMARCA2 PROTAC degrader with a DC50 of 8 nM. SMD-1087 induces ubiquitination and degradation of SMARCA2 via the proteasome pathway. SMD-1087 reduces PBRM1 protein levels, inhibits the growth of SMARCA4-deficient cancer cells, and suppresses tumor growth in mouse xenograft models. SMD-1087 can be used for research on SMARCA4-deficient human cancers, including lung cancer and melanoma[1][2].
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SMD-1087 | SMD-1087 is a VHL-recruiting SMARCA2 PROTAC degrader with a DC50 of 8 nM. SMD-1087 induces ubiquitination and degradation of SMARCA2 via the proteasome pathway. SMD-1087 reduces PBRM1 protein levels, inhibits the growth of SMARCA4-deficient cancer cells, and suppresses tumor growth in mouse xenograft models. SMD-1087 can be used for research on SMARCA4-deficient human cancers, including lung cancer and melanoma. | |||||||||||||||||||||
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References
- [1]. Yang L, et al. Discovery of SMD-3236: A Potent, Highly Selective and Efficacious SMARCA2 Degrader for the Treatment of SMARC4-Deficient Human Cancers. Journal of medicinal chemistry. 2025 Jan 23;68(2):1155-1178. [Content Brief]
- [2]. Leng L, et al. Discovery of High-Affinity SMARCA2/4 Bromodomain Ligands and Development of Potent and Exceptionally Selective SMARCA2 PROTAC Degraders. Journal of medicinal chemistry. 2025 Jan 23;68(2):1113-1133. [Content Brief]
