1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  2. HSP
  3. YM-1 tosylate

YM-1 tosylate 是稳定的和 MKT-077 类似物和具有口服活性的 Hsp70 抑制剂。YM-1 tosylate 诱导 HeLa 细胞死亡,上调 p53p21 的蛋白水平。

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YM-1 tosylate Chemical Structure

YM-1 tosylate Chemical Structure

CAS No. : 1427450-47-2

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

YM-1 tosylate is a stable MKT-077 (HY-15096) analog and an orally active Hsp70 inhibitor. YM-1 tosylate induces cell death of HeLa cells and up-regulates the level of p53 and p21 proteins[1][2].

IC50 & Target[1]

HSP70

3.2 μM (IC50)

体外研究
(In Vitro)

YM-1 tosylate 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) tosylate 激活 Hsp70 与未折叠底物的结合[1]
YM-1 (0.001-1000 μM) tosylate 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) tosylate 促进 nNOS 泛素化[1]
YM-1 (5 和 10 μM;24 和 48 小时) tosylate 诱导 HeLa 细胞死亡和 hTERT-RPE1 细胞生长停滞[2]
YM-1 (10 μM;48 小时) tosylate 上调 p53 和 p21,下调 FoxM1 和 survivin 的蛋白水平[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MCF7, MCF10A and MDA-MB-231
Concentration: 0-30 μM
Incubation Time: 72 h
Result: Inhibited viability with EC50s of 2.0 ± 0.2, 3.3 ± 0.3 and 5.2 ± 0.8 μM for MDA-MB-231, MCF10A and MCF7, respectively.
体内研究
(In Vivo)

YM-1 (1 mM;口服,持续 7 天) tosylate 通过激活 Hsp70 挽救果蝇中的 polyQ 毒性[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CD1 mice[1]
Dosage: 20 mg/kg
Administration: Intravenous injection (Pharmacokinetic Analysis)
Result: Initial pharmacokinetics of HSP70-IN-4 (Compound YM-01; 20 mg/kg; i.v.)[1]
hour plasma (ng/mL) brain (ng/g) kidney (ng/g)
0.16 359 0 74378
1 324 0 63231
Animal Model: UAS-hAR52Q flies with polyQ AR-induced dihydrotestosterone (DHT) phenotype[1]
Dosage: 1 mM
Administration: Oral administration; 1 mM, for 7 days
Result: Weakened the DHT-dependent eye degeneration phenotype and rescued DHT-dependent pupal toxicity of the polyQ AR.
分子量

553.72

Formula

C27H27N3O4S3

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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YM-1 tosylate
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HY-18406
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