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AA-CW236
产品别名
1869921-96-9
AA-CW236
4-(2-(5-(Chloromethyl)-4-(4-(trifluoromethoxy)phenyl)-1H-1,2,3-triazol-1-yl)ethyl)-3,5-dimethylisoxazole
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C17H16ClF3N4O2 |
| Molecular weight | 400.78 |
| Application【应用】 | AA-CW236 has been used as an inhibitor of m6G DNA methyltransferase in mouse embryo fibroblasts. |
| Biochem/physiol Actions【生化/生理作用】 | 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). |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 25 mg/mL protein, clear |
| storage temp.【储存温度】 | 2-8℃ |
| SMILES string | CC1=C(CCN2N=NC(C3=CC=C(OC(F)(F)F)C=C3)=C2CCl)C(C)=NO1 |
| packaging【包装】 | 5, 25 mg in glass bottle |
安全信息
| Storage Class Code【储存分类代码】 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
