FMK 9a
产品说明书
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同义名 : | - |
| CAS号 : | 1955550-51-2 | |
| 货号 : | A723647 | |
| 分子式 : | C23H21FN2O3 | |
| 纯度 : | 98% | |
| 分子量 : | 392.42 | |
| MDL号 : | MFCD31382128 | |
| 存储条件： |
Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 200 mg/mL(509.65 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 | ATG4 or autophagins are a class of cytosolic cysteine proteases that cleave ATG8 family proteins. ATG4 plays essential roles in the formation and maturation of autophagosomes[2]. FMK 9a is a potent inhibitor of ATG4B and ATG4A with IC50 values of 0.23 and 0.36 μM, respectively. FMK 9a exhibits strong binding affinity for both full-length ATG4B and ATG4BC74S with KDs of 3.89 μM and 3.24 μM, respectively. In vitro, FMK 9a (1 μM) could almost entirely inhibit ATG4B activity in HeLa cells in a very short time. FMK 9a could efficiently accumulate LC3-II in dose-dependent manner both in HeLa and MEF cells. Meanwhile, FMK 9a also induced LC3-II accumulation in a time-dependent manner and showed the best effect at 6 hrs[3]. FMK 9a exhibits moderate solubility and high human and mouse liver microsome clearances of 13.9 and 70 mL/min/kg, respectively[2]. | ||
| 作用机制 | FMK 9a forms an irreversible covalent bond with the more reactive thiol group of Cys74 located at the catalytic site of ATG4B[2]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.55mL 0.51mL 0.25mL |
12.74mL 2.55mL 1.27mL |
25.48mL 5.10mL 2.55mL |
| 参考文献 |
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