Sulfopin

• CAT Number: I036826
• CAS Number: 2451481-08-4
• Molecular Formula: C11H20ClNO3S
• Molecular Weight: 281.80
• Purity: ≥95%
• Synonyms: 2-chloro-N-(2,2-dimethylpropyl)-N-(1,1-dioxothiolan-3-yl)acetamide
• InChI: InChI=1S/C11H20ClNO3S/c1-11(2,3)8-13(10(14)6-12)9-4-5-17(15,16)7-9/h9H,4-8H2,1-3H3
• InChIKey: NMHVAHHYKGXBMY-UHFFFAOYSA-N
• SMILES: CC(C)(C)CN(C1CCS(=O)(=O)C1)C(=O)CCl

Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors[1].
MDA-MB-468 cells show the most pronounced sensitivity to Sulfopin (1, 2.5 μM; 4-8 days)[1].
Sulfopin (2 μM, HEK293 cells; 48 hours) downregulates Myc transcription[1].
Sulfopin (1, 2.5 μM; PATU-8988T cells; 4 days) shows a small but significant reduction in the number of synthesis (S)-phase cells and a corresponding increase of growth 1 (G1)-phase cells[1].
Sulfopin (40 mg/kg; p.o.; QD/BID for 7 days) regresses neuroblastoma in mice[1].
Sulfopin (20-40 mg/kg; i.p.; daily for 27 days) inhibits pancreatic cancer progression in mice[1].
Sulfopin (25-100 μM) blocks neuroblastoma in zebrafish[1].

Reference

[1]. Dubiella C, et al. Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo. Nat Chem Biol. 2021;17(9):954-963.
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