产品说明
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 µM/YM-08, 3.2 µM/YM-01, and 6.4 µM/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 µM YM-08, MKT-077, or YM-01, respectively) and weaker anti-cancer activity (IC50 against MDA-MB-231/MCF10A/MCF7 in µM = 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 (Cmax = 4 µg/g; t1/2 = 6.8 h; AUCinf = 260 ng·h/g; 6.6 mg/kg via i.v.; 100 µL/mouse in 30% H2O/5% Cremophor/5% EtOH/60% PBS) with much reduced accumulation in kidney in 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 µM YM-08, MKT-077, or YM-01, respectively) and weaker anti-cancer activity (IC50 against MDA-MB-231/MCF10A/MCF7 in µM = 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
经验(实验)分子式 | C19H17N3OS2 |
分子量 | 367.49 |
产品性质
测定 | ≥99% (HPLC) |
质量水平 | 100 |
形式 | solid |
效能 | 0.6 μM IC50 |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze protect from light |
颜色 | orange |
溶解性 | DMSO: 50 mg/mL |
储存温度 | 2-8℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 2 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich