TH-257
产品说明书
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同义名 : | - |
| CAS号 : | 2244678-29-1 | |
| 货号 : | A1193405 | |
| 分子式 : | C24H26N2O3S | |
| 纯度 : | 99% | |
| 分子量 : | 422.54 | |
| MDL号 : | MFCD31697753 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 250 mg/mL(591.66 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
| 生物活性 | |||
|---|---|---|---|
| 描述 | LIM kinase (LIMK) 1 and 2 are cytoplasmic tyrosine-like kinases involved in various physiological processes related to viral infection, tumor progression and metastasis. TH 257 is a potent inhibitor of both LIMK1 and 2 with IC50 values of 84 and 39nM, respectively[1]. In live cell NanoBRET assay, TH-257 exhibited an inhibitory effect against ectopically expressed full-length LIMK1 and 2 with IC50 values of 250 and 150nM, respectively. TH 257 showed no significant activity against the wider kinome that has been observed in the KINOMEscan assay at 1μM[1]. | ||
| 作用机制 | TH 257 is a potent, allosteric inhibitor of LIMK1/2 and can be used as a chemical probe for these enzymes. It targets a binding pocket induced by an αC and DFG-out conformation[1]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.37mL 0.47mL 0.24mL |
11.83mL 2.37mL 1.18mL |
23.67mL 4.73mL 2.37mL |
| 参考文献 |
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