YM-01 Tosylate

Names

[ Name ]:
YM-01 Tosylate

[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 4-methylbenzenesulfonate

Biological Activity

[Description]:

HSP70-IN-4 (Compound YM-01) is an Hsp70 inhibitor with an IC50 of 3.2 μM. HSP70-IN-4 is not BBB permeable[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> HSP

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

[Target]

HSP70:3.2 μM (IC50)

[In Vitro]

HSP70-IN-4 (Compound YM-01; 50 μM) 显著增强 Hsp70 与错误折叠蛋白的结合[1]。 HSP70-IN-4 (0-30 μM; 72 h) 抑制 MDA-MB-231、MCF10A 和 MCF7 的活性，EC50 分别为 2.0 ± 0.2、3.3 ± 0.3 和 5.2 ± 0.8 μM[1]。 HSP70-IN-4 在水中稳定 (室温下至少 8 小时)[1]。 HSP70-IN-4 在人肝微粒体中被快速代谢 (t1/2 值为 ~2-4 min)[1]。 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.

[In Vivo]

HSP70-IN-4 (Compound YM-01) 不能通过血脑屏障[1]。 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

[References]

[1]. Miyata Y, et al. Synthesis and initial evaluation of YM-08, a blood-brain barrier permeable derivative of the heat shock protein 70 (Hsp70) inhibitor MKT-077, which reduces tau levels. ACS Chem Neurosci. 2013 Jun 19;4(6):930-9.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₇H₂₇N₃O₄S₃

[ Molecular Weight ]:
553.72

[ Exact Mass ]:
553.116394

Related Compounds

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