JNK 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).
JNK Inhibitor XVI, JNK-IN-8 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
Overview 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.
Declaration Licensed under pending patent from Dana-Farber Cancer Institute.
Application JNK 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).
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.