AA-CW236 Property

Boiling point:

535.0±60.0 °C(Predicted)

Density 

1.43±0.1 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: 25mg/mL protein, clear

form 

powder

pka

-0.37±0.10(Predicted)

color 

white to beige

Hazard and Precautionary Statements (GHS)

AA-CW236 Chemical Properties,Usage,Production

Uses

AA-CW236 has been used as an inhibitor of m6G DNA methyltransferase in mouse embryo fibroblasts.

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).