5.05276
HSP70 Activator II, YM-08
Synonym(s):
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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| Size/SKU | Availability | Price |
|---|---|---|
10 mg | 0 left in stock | $309.00 |
About This Item
Empirical Formula (Hill Notation):
C19H17N3OS2
CAS Number:
Molecular Weight:
367.49
UNSPSC Code:
12352200
NACRES:
NA.77
PubChem Substance ID:
Assay:
≥99% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
assay
≥99% (HPLC)
Quality Segment
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
SMILES string
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
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
HSP70
HSP70
Reversible: yes
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.
Other Notes
Miyata, Y., et al. 2013. ACS Chem. Neurosci.4, 930.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
WGK
WGK 2
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
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