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178506 ERK Kinase Kinase 5 Inhibitor - CAS 1005775-56-3 - Calbiochem

178506
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Overview

Replacement Information

Products

Catalogue NumberPackaging Qty/Pack
178506-10MG Glass bottle 10 mg
Description
OverviewA cell-permeable imidazopyridine compound that acts as a potent, ATP-binding site-targeting ASK1/MEKK5-selective inhibitor (IC50 = 14 and 500 nM, respectively, against ASK1 and ASK2/MEKK6), while exhibiting much reduced or no activity toward a panel of 195 other kinases. Shown to inhibit STZ- (1 mM; Cat. No. 572201) induced JNK and p38 phosphorylation in INS-1 pancreatic β cells (IC50 <300 nM) and be orally available in rats in vivo.
Catalogue Number178506
Brand Family Calbiochem®
SynonymsN-(6-(1H-Imidazol-1-yl)imidazo[1,2-a]pyridin-2-yl)-4-tert-butylbenzamide, 2HCl, N-(6-(1H-Imidazol-1-yl)imidazo[1,2-a]pyridin-2-yl)-4-(2-methyl-2-propanyl)benzamide, 2HCl, 4-tert-Butyl-N-(6-(1H-imidazol-1-yl)imidazo(1,2-a)pyridin-2-yl)benzamide, 2HCl, Apoptosis Signal-Regulating Kinase 1 Inhibitor, ASK-1 Inhibitor, MAP Kinase Kinase Kinase 5 Inhibitor, MAP3K5 Inhibitor, MAPKKK5 Inhibitor, MEKK5 Inhibitor
References
ReferencesTerao, Y., et al. 2012. Bioorg. Med. Chem. Lett. 22, 7326.
Product Information
CAS number1005775-56-3
FormWhite powder
Hill FormulaC₂₁H₂₁N₅O • 2HCl
Chemical formulaC₂₁H₂₁N₅O • 2HCl
Hygroscopic Hygroscopic
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetASK1/MEKK5
Primary Target IC<sub>50</sub>14 and 500 nM, respectively, against ASK1 and ASK2/MEKK6
Purity≥99% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

References

Reference overview
Terao, Y., et al. 2012. Bioorg. Med. Chem. Lett. 22, 7326.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision12-September-2013 JSW
SynonymsN-(6-(1H-Imidazol-1-yl)imidazo[1,2-a]pyridin-2-yl)-4-tert-butylbenzamide, 2HCl, N-(6-(1H-Imidazol-1-yl)imidazo[1,2-a]pyridin-2-yl)-4-(2-methyl-2-propanyl)benzamide, 2HCl, 4-tert-Butyl-N-(6-(1H-imidazol-1-yl)imidazo(1,2-a)pyridin-2-yl)benzamide, 2HCl, Apoptosis Signal-Regulating Kinase 1 Inhibitor, ASK-1 Inhibitor, MAP Kinase Kinase Kinase 5 Inhibitor, MAP3K5 Inhibitor, MAPKKK5 Inhibitor, MEKK5 Inhibitor
DescriptionA cell-permeable imidazopyridine compound that acts as a potent, ATP-binding site-targeting ASK1/MEKK5-selective inhibitor (IC50 = 14 and 500 nM, respectively, against ASK1 and ASK2/MEKK6), while exhibiting much reduced or no activity toward a panel of 195 other kinases, including MEKK1,TAK1, ERK1, JNK1, and p38α (IC50 >10 µM). Shown to inhibit STZ- (1 mM; Cat. No. 572201) induced JNK and p38 phosphorylation in INS-1 pancreatic β cells in a dose-dependent manner (IC50 <300 nM) and be orally available in rats in vivo (AUC0-8h = 275.4 ng·h/mL; 1 mg/kg p.o.).
FormWhite powder
Intert gas (Yes/No) Packaged under inert gas
CAS number1005775-56-3
Chemical formulaC₂₁H₂₁N₅O • 2HCl
Structure formulaStructure formula
Purity≥99% by HPLC
SolubilityDMSO (100 mg/ml) or H₂O (40 mg/ml)
Storage -20°C
Hygroscopic
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesTerao, Y., et al. 2012. Bioorg. Med. Chem. Lett. 22, 7326.