产品说明
应用
AA-CW236 has been used as an inhibitor of m6G DNA methyltransferase in mouse embryo fibroblasts.
包装
5, 25 mg in glass bottle
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).
基本信息
| 经验(实验)分子式 | C17H16ClF3N4O2 |
| 分子量 | 400.78 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | powder |
| 颜色 | white to beige |
| 溶解性 | DMSO: 25 mg/mL protein, clear |
| 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 |
安全信息
| 储存分类代码 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
