Synonyms: 1'-(4-Methoxyphenylsulfonyl)-4-methyl-1,4'-bipiperidine hydrochloride; 1,4'-Bipiperidine, 1'-[(4-methoxyphenyl)sulfonyl]-4-methyl-, hydrochloride; Truncated APC Selective INhibitor-1
Molecular Formula: C18H28N2O3S · HCl
Molecular Weight: 388.95
Linear Structural Formula: C18H28N2O3S · HCl
Purity: >=98% (HPLC)
Storage: 2-8C
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 muM/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 muM 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.