Synonym: 1′-(4-Methoxyphenylsulfonyl)-4-methyl-1,4′-bipiperidine hydrochloride; 1,4′-Bipiperidine, 1′-[(4-methoxyphenyl)sulfonyl]-4-methyl-, hydrochloride; Truncated APC Selective INhibitor-1
CAS Number: 1678515-13-3
Empirical Formula (Hill Notation): C18H28N2O3S · HCl
Molecular Weight: 388.95
Linear Formula: C18H28N2O3S · HCl
Product Type: Chemical
| assay |
≥98% (HPLC) |
| color |
white to beige |
| form |
powder |
| InChI key |
TXDTUQPRRXNCLP-UHFFFAOYSA-N |
| SMILES string |
CC(CC1)CCN1C(CC2)CCN2S(C3=CC=C(OC)C=C3)(=O)=O.[H]Cl |
| solubility |
H2O: 2 mg/mL, clear |
| storage condition |
desiccated |
| |
protect from light |
| storage temp. |
2-8°C |
| Biochem/physiol Actions: |
EBP-dependent cholesterol synthesis inhibitor with selective cytotoxicity against colorectal cancer cells harboring APC truncations. |
| 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. |
| RIDADR |
NONH for all modes of transport |
| WGK Germany |
WGK 3 |
| Flash Point(F) |
Not applicable |
| Flash Point(C) |
Not applicable |
| Purity |
≥98% (HPLC) |
| Storage Temp. |
2-8°C |
| UNSPSC |
12352200 |
