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MilliporeSigma

SML1988

Sigma-Aldrich

TASIN-1 hydrochloride

≥98% (HPLC)

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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5 MG
$102.06
25 MG
$436.00

About This Item

Empirical Formula (Hill Notation):
C18H28N2O3S · HCl
CAS Number:
Molecular Weight:
388.95
UNSPSC Code:
12352200
NACRES:
NA.77

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$102.06

List Price$108.00Save 5%
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In StockDetails


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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

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This Item
PZ0362SML0853P3246
assay

≥98% (HPLC)

assay

≥95% (HPLC)

assay

≥98% (HPLC)

assay

~99% (HPLC)

form

powder

form

powder

form

powder

form

powder

storage temp.

2-8°C

storage temp.

room temp

storage temp.

2-8°C

storage temp.

-

solubility

H2O: 2 mg/mL, clear

solubility

H2O: 2 mg/mL, clear (warmed)

solubility

H2O: 1 mg/mL, clear (warmed)

solubility

H2O: >2.0 mg/mL

storage condition

desiccated, protect from light

storage condition

desiccated

storage condition

-

storage condition

-

color

white to beige

color

white to beige

color

white to beige

color

white

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_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Questions

  1. How is it recommended to reconstitute Tasin-1 (solvent and up to what concentration)? And does it need to be filter sterilised before use in cell-culture?

    1 answer
    1. This product may be reconstituted in water at 2 mg/mL. This is not a sterile product. Stock solutions would require sterile filtration prior to use in cell culture.

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