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420150-M

JNK Inhibitor XVI, JNK-IN-8

Name: JNK Inhibitor XVI, JNK-IN-8
Brand: MM

The JNK Inhibitor XVI, JNK-IN-8 controls the biological activity of JNK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

JNK Inhibitor XVI, JNK-IN-8, (E)-3-(4-(dimethylamino)but-2-enamido)-N-(3-methyl-4-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide

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About This Item

Empirical Formula (Hill Notation):

C₂₉H₂₉N₇O₂

CAS Number:

1410880-22-6

Molecular Weight:

507.59

UNSPSC Code:

12352200

MDL number:

MFCD22124890

Assay:

≥97% (HPLC)

Form:

powder

Storage condition:

OK to freeze, protect from light

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Properties

assay

≥97% (HPLC)

form

powder

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, protect from light

color

light yellow to yellow

solubility

DMSO: 100 mg/mL, clear, yellow

storage temp.

2-8°C

InChI

1S/C29H29N7O2/c1-20-17-24(11-12-25(20)34-29-31-15-13-26(35-29)22-8-5-14-30-19-22)33-28(38)21-7-4-9-23(18-21)32-27(37)10-6-16-36(2)3/h4-15,17-19H,16H2,1-3H3,(H,32,37)(H,33,38)(H,31,34,35)/b10-6+

InChI key

GJFCSAPFHAXMSF-UXBLZVDNSA-N

Description

General description

A 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.

Biochem/physiol Actions

Primary Target
JNK1, JNK2, JNK3

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Zhang, T., et al. 2011. Chem. Biol.19, 140

Legal Information

Licensed under pending patent from Dana-Farber Cancer Institute.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c