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5.05276

HSP70 Activator II, YM-08

Name: HSP70 Activator II, YM-08
Brand: MM

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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About This Item

Empirical Formula (Hill Notation):

C₁₉H₁₇N₃OS₂

CAS Number:

1427472-76-1

Molecular Weight:

367.49

UNSPSC Code:

12352200

NACRES:

NA.77

PubChem Substance ID:

72201046

Assay:

≥99% (HPLC)

Form:

solid

Quality level:

100

Storage condition:

OK to freeze, protect from light

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Properties

assay

≥99% (HPLC)

Quality Level

100

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

Description

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 (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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
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