HSP70 Activator II, YM-08-Calbiochem

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一般描述

A cell-permeable, neutrally charged, pyridinium-to-pyridine substituted YM-01 (Cat. No. 500615) and MKT-077 structural analog that exhibits higher HSP70-binding affinity than its cationic pyridinium counterparts (IC₅₀= 0.61 ?M/YM-08, 3.2 ?M/YM-01, and 6.4 ?M/MKT-077, respectively, in competitive binding assays using human Hsc70/HSPA8), but reduced tau degradation-promoting potency in cultures (% degradation of p-tau/total tau/24 h = 42/64, 88/89, and 81/80 in HeLaC3 with 30 ?M YM-08, MKT-077, or YM-01, respectively) and weaker anti-cancer activity (IC₅₀against MDA-MB-231/MCF10A/MCF7 in ?M = 1.4/3.0/2,2/MKT-077, 2.0/3.3/5.2/YM-01, and 8.5/7.8/10.5/YM-08 with 72 h compound treatment). However, only YM-08, but not YM-01 or MKT-077, exhibits detectable blood-brain-barrier permeability in mice (C_max= 4 ?g/g;t_1/2= 6.8 h;AUC_inf= 260 ng·h/g; 6.6 mg/kg via i.v.; 100 ?L/mouse in 30% H₂O/5% Cremophor/5% EtOH/60% PBS) with much reduced accumulation in kidneyin vivo.
A cell-permeable, neutrally charged, pyridinium-to-pyridine substituted YM-01 (Cat. No. 500615) and MKT-077 structural analog that exhibits higher HSP70-binding affinity, but reduced tau degradation-promoting potency in cultures (% degradation of p-tau/total tau = 42/64, 88/89, and 81/80 in HeLaC3 with 30 ?M YM-08, MKT-077, or YM-01, respectively) and weaker anti-cancer activity (IC₅₀against MDA-MB-231/MCF10A/MCF7 in ?M = 1.4/3.0/2,2/MKT-077, 2.0/3.3/5.2/YM-01, and 8.5/7.8/10.5/YM-08 in 72 h).

生化/生理作用

Cell permeable: yes
Primary Target
HSP70
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Miyata, Y., et al. 2013.ACS Chem. Neurosci.4,930.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

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安全信息