YM-01(YM-1)

Names

[ Name ]:
YM-01(YM-1)

[Synonym ]:
2-{(Z)-[(5E)-3-Ethyl-5-(3-methyl-1,3-benzothiazol-2(3H)-ylidene)-4-oxo-1,3-thiazolidin-2-ylidene]methyl}-1-methylpyridinium chloride
Pyridinium, 2-[(Z)-[(5E)-3-ethyl-5-(3-methyl-2(3H)-benzothiazolylidene)-4-oxo-2-thiazolidinylidene]methyl]-1-methyl-, chloride (1:1)
YM-1

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> HSP

Signaling Pathways >> Immunology/Inflammation >> NO Synthase

Signaling Pathways >> Cell Cycle/DNA Damage >> HSP

[In Vitro]

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: HeLa and hTERT-RPE1 cell lines Concentration: 10 μM Incubation Time: 48 hoursI Result: Increased the level of p53 and p21 and decreased the level of FoxM1 and survivin.

[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: 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.

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₀H₂₀ClN₃OS₂

[ Molecular Weight ]:
417.975

[ Exact Mass ]:
417.073639

[ Storage condition ]:
2-8°C

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Related Compounds

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