5.05276

HSP70 Activator II, YM-08

• 別名: HSP70 Activator II, YM-08, (2Z,5E)-3-ethyl-5-(3-methylbenzo[d]thiazol-2(3H)-ylidene)-2-(pyridin-2-ylmethylene)thiazolidin-4-one, Heat Shock 70 kDa Protein Activator II, Hsp70 Chemical Co-Chaperone II, YM-08, YM08, YM8
• 実験式（ヒル表記法）: C₁₉H₁₇N₃OS₂
• CAS番号: 1427472-76-1
• 分子量: 367.49
• UNSPSCコード: 12352200
• PubChem Substance ID: 72201046
• NACRES: NA.77

特性

• アッセイ: ≥99% (HPLC)
• 品質水準: 100
• フォーム: solid
• 有効性: 0.6 μM IC₅₀
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: orange
• 溶解性: DMSO: 50 mg/mL
• 保管温度: 2-8°C
• SMILES記法: CCN1C(=CC2=CC=CC=N2)SC(=C3N(C4=CC=CC=C4S3)C)C1=O
• InChI: 1S/C19H17N3OS2/c1-3-22-16(12-13-8-6-7-11-20-13)25-17(18(22)23)19-21(2)14-9-4-5-10-15(14)24-19/h4-12H,3H2,1-2H3
• InChI Key: UYFLAORTCSDPFM-UHFFFAOYSA-N

詳細

詳細

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 (C_max = 4 µg/g; t_1/2 = 6.8 h; AUC_inf = 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.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
HSP70

Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 2
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable