SML1988

TASIN-1 hydrochloride

≥98% (HPLC)

• Synonym(s): 1′-(4-Methoxyphenylsulfonyl)-4-methyl-1,4′-bipiperidine hydrochloride, 1,4′-Bipiperidine, 1′-[(4-methoxyphenyl)sulfonyl]-4-methyl-, hydrochloride, Truncated APC Selective INhibitor-1
• Empirical Formula (Hill Notation): C₁₈H₂₈N₂O₃S · HCl
• CAS Number: 1678515-13-3
• Molecular Weight: 388.95
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Assay: ≥98% (HPLC)
• form: powder
• storage condition: desiccated; protect from light
• color: white to beige
• solubility: H₂O: 2 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: CC(CC1)CCN1C(CC2)CCN2S(C3=CC=C(OC)C=C3)(=O)=O.[H]Cl

Description

Biochem/physiol Actions

TASIN-1 (Truncated APC Selective INhibitor-1) targets EBP- (Emopamil-binding protein; D8-D7 sterol isomerase) dependent cholesterol biosynthesis and selectively induces cellular cholesterol depletion and apoptotic death in human colorectal cancer (CRC) cultures harboring APC truncations under lipid-deficient conditions (0.2% FCS or 2% lipoprotein-deficient serum; IC50 from 35 nM/HT29 to 4.9 μM/HT55 in 72 hrs) as a result of defective cholesterol homeostasis regulation, while exhibiting little cytotoxicity toward wild-type APC CRC cells or non-transformed human colonic and bronchial epithelial cells (IC50 >50 μM in 72 hrs). TASIN-1 intraperitoneal injection is efficacious against the growth of CRC tumors with trunctated APC using the genetically engineered CPC;Apc mice (20 mg/kg twice a week) and two xenograft murine models (DLD1 & HT29; 40 mg/kg twice daily) without apparent toxicity to the animals.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable