半岛bd体育手机客户端 说明
一般描述
A cell-permeable (Pappx 106= 9.38 and 7.91 cm/s, respectively, for "A-B" and "B-A" in Caco-2 permeability assay) and biologically stable (t1/2= 277.2 and 117.5 min., respectively, using human and mouse liver microsome preparation) tetrahydroquinoline-sulfonamide that enhances the donor PEP (phosphoenolpyruvate), but not the acceptor ADP, substrate affinity toward PK (pyruvate kinase) isoform PKM2 (Km= 0.4 vs. 1.9 mM with or without 10 ?M activator) and acts as a potent PKM2-selective activator (AC50= 90 nM using rhPKM2; ACmax= 88%), displaying much reduced activity toward PKL (≤25% at 57 ?M) and no effect toward PKM1 or PKR.
A cell-permeable and biologically stable (t1/2= 277.2 and 117.5 min., respectively, in human and mouse liver microsome preparation) tetrahydroquinoline-sulfonamide that enhances the donor PEP, but not the acceptor ADP, substrate affinity toward pyruvate kinase isoform PKM2 (Km= 0.4 vs. 1.9 mM with or without 10 ?M activator) and acts as a potent PKM2-selective activator (AC50= 90 nM using rhPKM2; ACmax= 88%), displaying much reduced activity toward PKL (≤25% at 57 ?M) and no effect toward PKM1 or PKR.
包装
25 mg in Glass bottle
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Walsh, M.J., et al. 2011.Bioorg. Med. Chem. Lett.21,6322.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
| 经验(实验)分子式 | C15H11ClF2N2O3S |
| 分子量 | 372.77 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | powder |
| manufacturer/tradename | Calbiochem? |
| 储存条件 | OK to freeze protect from light |
| 颜色 | white |
| 溶解性 | DMSO: 100 mg/mL, clear, colorless |
| 运输 | ambient |
| 储存温度 | 2-8℃ |
| SMILES string | FC1=CC2=C(CCC(N2)=O)C=C1S(NC3=CC=C(F)C(Cl)=C3)(=O)=O |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
Sigma-Aldrich
m.cnreagent.com
