EMAIL THIS PAGE TO A FRIEND
SML1761 Sigma-Aldrich

AA-CW236

≥98% (HPLC)

Synonym: 4-(2-(5-(Chloromethyl)-4-(4-(trifluoromethoxy)phenyl)-1H-1,2,3-triazol-1-yl)ethyl)-3,5-dimethylisoxazole

  • CAS Number 1869921-96-9

  • Empirical Formula (Hill Notation) C17H16ClF3N4O2

  • Molecular Weight 400.78

Purchase

Properties

Related Categories A-AM, Apoptosis and Cell Cycle, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology,
assay   ≥98% (HPLC)
form   powder
color   white to beige
solubility   DMSO: 25 mg/mL protein, clear
storage temp.   2-8°C

Description

Packaging

5, 25 mg in glass bottle

Biochem/physiol Actions

AA-CW236 is a cell-permeable chloromethyl triazole (CMT) derivative that acts as a non-pseudosubstrate inhibitor against human O(6)-alkylguanine DNA methyltransferase (MGMT) by targeting MGMT active site Cys145 for covalent modification (KI = 24 nM, kinact = 0.03/min), displaying little affinity toward cysteines from other cellular proteins. AA-CW236 pretreatment (1 μM) effectively prevents MGMT from repairing DNA damage, causing significantly more upregulated O6-alkylguanine accumulation than the pseudosubstrate inhibitor Lomeguatrib (1 μM) when co-administered with the DNA-alkylating agent Temozolomide/TMZ (300 μM) in MCF-7 cells. Likewise, AA-CW236 is shown to boost TMZ toxicity in Caco-2 cultures (IC50 = 227 and 673 μM, respectively, with or without 3 μM AA-CW236 co-treatment).

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport

Documents

Certificate of Analysis

Protocols & Articles
Related Products

Technical Service:

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Bulk Ordering & Pricing:

Need larger quantities for your development, manufacturing or research applications?