5.05276

HSP70 Activator II, YM-08

• 동의어(들): 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
• 실험식(Hill 표기법): C₁₉H₁₇N₃OS₂
• CAS Number: 1427472-76-1
• Molecular Weight: 367.49
• UNSPSC 코드: 12352200
• PubChem Substance ID: 72201046
• NACRES: NA.77

속성

• 분석: ≥99% (HPLC)
• Quality Level: 100
• 형태: solid
• 효능: 0.6 μM IC₅₀
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: orange
• solubility: DMSO: 50 mg/mL
• 저장 온도: 2-8°C
• SMILES string: CCN1C(=CC2=CC=CC=N2)SC(=C3N(C4=CC=CC=C4S3)C)C1=O

설명

일반 설명

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.

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).

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
HSP70

Reversible: yes

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

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

기타 정보

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

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable