TASIN-1 HYDROCHLORIDE

Code: SML1988-25MG D2-231

Biochem/physiol Actions

TASIN-1 (Truncated APC Selective INhibitor-1) targets EBP- (Emopamil-binding protein; D8-D7 sterol isomerase) dependent cholesterol biosynthesis and s...


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€372.67 25MG
€458.38 inc. VAT

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.

assay≥98% (HPLC)
colorwhite to beige
formpowder
SMILES stringCC(CC1)CCN1C(CC2)CCN2S(C3=CC=C(OC)C=C3)(=O)=O.[H]Cl
solubilityH2O: 2 mg/mL, clear
storage conditionprotect from light
storage temp.2-8°C
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