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420150 JNK Inhibitor XVI, JNK-IN-8 - Calbiochem

420150
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Panoramica

Replacement Information

Tabella delle specifiche principali

Empirical FormulaCAS #
C₂₉H₂₉N₇O₂ 1410880-22-6

Products

Numero di catalogoConfezionamento Qtà/conf
420150-10MG Bottiglia di vetro 10 mg
Description
OverviewA cell-permeable, selective, and irreversible type 2 inhibitor of c-Jun N-terminal kinases (JNK) (IC50 = 4.67 nM, 18.7 nM, 980 pM for JNK1, JNK2, and JNK3, respectively). Forms a covalent adduct with the conserved cysteine residue (Cys116 in JNK1) and binds to JNK in an extended type 2 conformation. Blocks the phosphorylation of c-Jun in cells (EC50 = 486 nM in HeLa cells; 338 nM in A375 cells). Exhibits greater cellular specificity for JNK when compared to 40 other kinases screened using a cell-based assay. Shows weaker binding to KIT mutants (IC50 = 92 nM for V559D and 56 nM for T670I) and RIOK2 (120 nM). Does not show any significant inhibitory activity against various other kinases, including ERK, p38, Akt, MSK, and RSK.
Catalogue Number420150
Brand Family Calbiochem®
Synonyms(E)-3-(4-(dimethylamino)but-2-enamido)-N-(3-methyl-4-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide
References
ReferencesZhang, T., et al. 2011. Chem. Biol. 19, 140
Product Information
CAS number1410880-22-6
DeclarationLicensed under pending patent from Dana-Farber Cancer Institute.
FormLight yellow to yellow powder
Hill FormulaC₂₉H₂₉N₇O₂
Chemical formulaC₂₉H₂₉N₇O₂
ReversibleN
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
ApplicationJNK Inhibitor XVI, JNK-IN-8, CAS 1410880-22-6, is a cell-permeable, selective, irreversible type 2 inhibitor of c-Jun kinases (IC50 = 4.67 nM, 18.7 nM, 980 pM for JNK1, 2 & 3, respectively).
Biological Information
Primary TargetJNK1, JNK2, JNK3
Purity≥97% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

JNK Inhibitor XVI, JNK-IN-8 - Calbiochem MSDS

Titolo

Scheda di sicurezza (MSDS) 

JNK Inhibitor XVI, JNK-IN-8 - Calbiochem Certificati d'Analisi

TitoloNumero di lotto
420150

Riferimenti bibliografici

Panoramica delle referenze
Zhang, T., et al. 2011. Chem. Biol. 19, 140
Scheda tecnica

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-October-2016 JSW
Synonyms(E)-3-(4-(dimethylamino)but-2-enamido)-N-(3-methyl-4-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide
DescriptionA cell-permeable, selective, and irreversible type 2 inhibitor of c-Jun N-terminal kinases (JNK) (IC50 = 4.67 nM, 18.7 nM, 980 pM for JNK1, JNK2, and JNK3, respectively). Forms a covalent adduct with the conserved cysteine residue (Cys116 in JNK1) and binds to JNK in an extended type 2 conformation. Blocks the phosphorylation of c-Jun in cells (EC50 = 486 nM in HeLa cells; 338 nM in A375 cells). Exhibits greater cellular specificity for JNK when compared to 40 other kinases screened using a cell-based assay. Shows weaker binding to KIT mutants (IC50 = 92 nM for V559D and 56 nM for T670I) and RIOK2 (120 nM). Does not show any significant inhibitory activity against various other kinases, including ERK, p38, Akt, MSK, and RSK.
FormLight yellow to yellow powder
Intert gas (Yes/No) Packaged under inert gas
CAS number1410880-22-6
Chemical formulaC₂₉H₂₉N₇O₂
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (100 mg/ml; clear, yellowish solution)
Storage +2°C to +8°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesZhang, T., et al. 2011. Chem. Biol. 19, 140