SML1988
TASIN-1 hydrochloride
≥98% (HPLC), EBP-dpendent cholesterol synthesis inhibitor, powder
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
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About This Item
Empirical Formula (Hill Notation):
C18H28N2O3S · HCl
CAS Number:
Molecular Weight:
388.95
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
desiccated, protect from light
Product Name
TASIN-1 hydrochloride, ≥98% (HPLC)
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
InChI key
TXDTUQPRRXNCLP-UHFFFAOYSA-N
Biochem/physiol Actions
EBP-dependent cholesterol synthesis inhibitor with selective cytotoxicity against colorectal cancer cells harboring APC truncations.
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.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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