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420175

Sigma-Aldrich

Cancer Hydrolase KIAA1363 Inhibitor, JW480

Synonym(s):

Cancer Hydrolase KIAA1363 Inhibitor, JW480, 2ʹ-Isopropylphenyl-2-(2-naphthyl)ethylcarbamate, AADACL1 Inhibitor, Arylacetamide Deacetylase-Like 1 Inhibitor, NCEH1 Inhibitor, Neutral Cholesterol Ester Hydrolase 1 Inhibitor

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About This Item

Empirical Formula (Hill Notation):
C22H23NO2
CAS Number:
Molecular Weight:
333.42
MDL number:
UNSPSC Code:
12352200

assay

≥97% (HPLC)

Quality Level

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 50 mg/mL, clear, colorless

shipped in

ambient

storage temp.

2-8°C

SMILES string

O=C(OC1=CC=CC=C1C(C)C)NCCC2=CC3=C(C=C2)C=CC=C3

InChI

1S/C22H23NO2/c1-16(2)20-9-5-6-10-21(20)25-22(24)23-14-13-17-11-12-18-7-3-4-8-19(18)15-17/h3-12,15-16H,13-14H2,1-2H3,(H,23,24)

InChI key

PCNJGBMWAZRVEA-UHFFFAOYSA-N

General description

A membrane-permeable carbamate that acts as a highly potent and selective inhibitor against the 2-acetyl MAGE (monoakylglycerol ether) hydrolase KIAA1363/AADACL1 of both human (IC50 = 12 nM; PC3 cell lysate) and murine (IC50 = 20 nM; mouse brain membrane homogenate) origin, presumably via covalent/irreversible carbamoylation of enzyme active site nucleophilic serine, with no significant effect toward other PC3 or murine brain serine hydrolase activities, including HSL, FAAH, and AChE. Readily crosses blood-brain barrier in mice (complete inhibition of brain KIAA1363 in 4 h after single i.p. or o.g./oral gavage dose of 5 mg/kg and 20 mg/kg, respectively). Reported to inhibit the survival of PC3 prostate cancer cells in cultures in vitro (by 34%; 48 h; 1 µM) and suppress PC3-derived tumor growth in mice in vivo (by 56% on day 33; 80 mg/kg/day; o.g.). Also inhibits blood carboxylesterase.
A membrane-permeable, highly potent and selective inhibitor against the 2-acetyl MAGE (monoakylglycerol ether) hydrolase KIAA1363/AADACL1 of both human (IC50 = 12 nM; PC3 lysate) and murine (IC50 = 20 nM; brain membrane samples) origin, with no significant effect toward other PC3 or murine brain serine hydrolase activities, including HSL, FAAH, and AChE. Readily crosses blood-brain barrier in mice and effectively suppresses PC3-derived tumor growth in mice in vivo (by 56% on day 33; 80 mg/kg/day; o.g.). Also inhibits blood carboxylesterase.

Packaging

Packaged under inert gas

Warning

Toxicity: Regulatory Review (Z)

Other Notes

Chang, J.W., et al. 2011. Chem. Biol.18, 476.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3


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