| Bioactivity | YM-1 is a stable and soluble MKT-077 (HY-15096) analog and an orally active Hsp70 inhibitor. YM-1 induces cell death of HeLa cells and up-regulates the level of p53 and p21 proteins[1][2]. |
| Invitro | YM-1 促进 Nnos 成熟过程中依赖 Hsp70 的步骤，阻断部分与 ATP 的结合[1]。YM-1 (0-200 μM) 激活 Hsp70 与未折叠底物的结合[1]。YM-1 (0.001-1000 μM) 将 Hsp70 转化为紧密亲和构象，与 Hsp70 结合的 IC50 值为 8.2 μM[1]。YM-1 (0，0.1，0.5 和 1 μM；24 小时) 促进 nNOS 泛素化[1]。YM-1 (5 和 10 μM；24 和 48 小时) 诱导 HeLa 细胞死亡和 hTERT-RPE1 细胞生长停滞[2]YM-1 (10 μM；48 小时) 上调 p53 和 p21，下调 FoxM1 和 survivin 的蛋白水平[2]。 Western Blot Analysis[2] Cell Line: |
| In Vivo | YM-1 (1 mM；口服，持续 7 天) 通过激活 Hsp70 挽救果蝇中的 polyQ 毒性[1]。 Animal Model: |
| Name | YM-1 |
| CAS | 409086-68-6 |
| Formula | C20H20ClN3OS2 |
| Molar Mass | 417.98 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Wang AM, et al. Activation of Hsp70 reduces neurotoxicity by promoting polyglutamine protein degradation. Nat Chem Biol. 2013 Feb;9(2):112-8. [2]. Khondoker Md Zulfiker Rahman, et al. Effect of an Inhibitor of HSP70, YM-1, on Hikeshi Knockout Cells. Thermal Medicine. 2017, 33(4):129-134. |