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
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この商品について
実験式（ヒル表記法）:
C19H17N3OS2
CAS番号:
分子量:
367.49
UNSPSC Code:
12352200
NACRES:
NA.77
PubChem Substance ID:
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
SMILES string
CCN1C(=CC2=CC=CC=N2)SC(=C3N(C4=CC=CC=C4S3)C)C1=O
assay
≥99% (HPLC)
form
solid
potency
0.6 μM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
orange
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Cell permeable: yes
Primary Target
HSP70
HSP70
Reversible: yes
Disclaimer
Toxicity: Standard Handling (A)
General description
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.
Other Notes
Miyata, Y., et al. 2013. ACS Chem. Neurosci.4, 930.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
保管分類
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
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