420175

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
• Empirical Formula (Hill Notation): C₂₂H₂₃NO₂
• CAS Number: 1354359-53-7
• Molecular Weight: 333.42
• MDL number: MFCD20926355
• UNSPSC Code: 12352200

Properties

• Assay: ≥97% (HPLC)
• Quality Level: 100
• 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

Description

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3