Other grades of this product :
| AA-CW236 Basic information |
| Product Name: | AA-CW236 | | Synonyms: | AA-CW236;AA-CW236
(AA-CW-236;1H-1,2,3-Triazole, 5-(chloromethyl)-1-[2-(3,5-dimethyl-4-isoxazolyl)ethyl]-4-[4-(trifluoromethoxy)phenyl]-;AA-CW236 >=98% (HPLC) | | CAS: | 1869921-96-9 | | MF: | C17H16ClF3N4O2 | | MW: | 400.78 | | EINECS: | | Product Categories: | | Mol File: | 1869921-96-9.mol |
| AA-CW236 Chemical Properties |
| storage temp. | 2-8°C | | form | powder | | color | white to beige |
| AA-CW236 Usage And Synthesis |
| 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). |
| AA-CW236 Preparation Products And Raw materials |
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