Description
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.
Product information
CAS Number: 2451481-08-4
Molecular Weight: 281.80
Formula: C11H20ClNO3S
Chemical Name: 2-chloro-N-(2,2-dimethylpropyl)-N-(1,1-dioxo-1λ⁶-thiolan-3-yl)acetamide
Smiles: CC(C)(C)CN(C1CS(=O)(=O)CC1)C(=O)CCl
InChiKey: NMHVAHHYKGXBMY-UHFFFAOYSA-N
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
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (354.86 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
MDA-MB-468 cells show the most pronounced sensitivity to Sulfopin (1, 2.5 μM; 4-8 days). Sulfopin (2 μM, HEK293 cells; 48 hours) downregulates Myc transcription. 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.
In Vivo:
Sulfopin (40 mg/kg; p.o.; QD/BID for 7 days) regresses neuroblastoma in mice. Sulfopin (20-40 mg/kg; i.p.; daily for 27 days) inhibits pancreatic cancer progression in mice. Sulfopin (25-100 μM) blocks neuroblastoma in zebrafish.
Products are for research use only. Not for human use.
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