420150-M

JNK Inhibitor XVI, JNK-IN-8

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

• 別名: 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
• 実験式（ヒル表記法）: C₂₉H₂₉N₇O₂
• CAS番号: 1410880-22-6
• 分子量: 507.59
• MDL番号: MFCD22124890
• UNSPSCコード: 12352200

特性

• アッセイ: ≥97% (HPLC)
• フォーム: powder
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: light yellow to yellow
• 溶解性: DMSO: 100 mg/mL, clear, yellow
• 保管温度: 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

詳細

詳細

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.

生物化学的／生理学的作用

Primary Target
JNK1, JNK2, JNK3

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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

法的情報

Licensed under pending patent from Dana-Farber Cancer Institute.

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable