A cell-permeable, selective, and irreversible type 2 inhibitor of c-Jun N-terminal kinases (JNK) (IC50=4.67nM, 18.7nM, 980pM 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=486nM in HeLa cells, 338nM 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=92nM for V559D and 56nM for T670I) and RIOK2 (120nM). Does not show any significant inhibitory activity against various other kinases, including ERK, p38, Akt, MSK, and RSK. CAS No.: 1410880-22-6 Formula: C29H29N7O2 Molecular Weight: 507.6 Solubility: DMSO (100mg/ml, clear, yellowish solution) Storage and Stability: Lyophilized powder may be stored at -20C. Stable for 12 months at -20C. Reconstitute with sterile ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
Molecular Weight:
507.6
Purity:
97% (HPLC)
Form:
Supplied as a light beige powder.
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