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Merck
CN

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:
1678515-13-3
Molecular Weight:
388.95
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

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Product Name

TASIN-1 hydrochloride, ≥98% (HPLC)

InChI key

TXDTUQPRRXNCLP-UHFFFAOYSA-N

SMILES string

CC(CC1)CCN1C(CC2)CCN2S(C3=CC=C(OC)C=C3)(=O)=O.[H]Cl

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

Related Categories

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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Certificates of Analysis (COA)

Lot/Batch Number
0000420538
0000420537
0000420537
0000420538
0000385458

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Lu Zhang et al.
Science translational medicine, 8(361), 361ra140-361ra140 (2016-11-01)
Mutations in the adenomatous polyposis coli (APC) gene are common in colorectal cancer (CRC), and more than 90% of those mutations generate stable truncated gene products. We describe a chemical screen using normal human colonic epithelial cells (HCECs) and a

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