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J2580 Sigma

L-JNKi 1 trifluoroacetate salt

≥98% (HPLC), solid

  • Empirical Formula (Hill Notation) C164H286N66O40 · xC2HF3O2

  • Molecular Weight 3822.44 (free base basis)

  •  MDL number MFCD12912420

  •  PubChem Substance ID 329815404

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Properties

Related Categories Cell Biology, Cell Signaling and Neuroscience, JNKs, c-Jun N-Terminal Kinase, Mitogen-Activated Protein Kinase (MAPK), Kinase/Phosphatase Biology, Serine/Threonine Kinase Activators,
InChI Key   OCVQPVVUPFPZLE-NWQCESEKSA-N
assay   ≥98% (HPLC)
form   powder
  solid
color   white
solubility   H2O: >1 mg/mL
storage temp.   −20°C

Description

Amino Acid Sequence

Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Pro-Pro-Arg-Pro-Lys-Arg-Pro-Thr-Thr-Leu-Asn-Leu-Phe-Pro-Gln-Val-Pro-Arg-Ser-Gln-Asp-NH2

Biochem/physiol Actions

The L-JNKi 1 and the protease resistant, all-D retro-inverso form, D-JNKi peptides represent the only potent inhibitors specific for JNK (JNK1, JNK2 and JNK3). Different from chemical inhibitors that directly affect kinase activity e.g. by competing with the ATP-binding site of the protein kinase, they rather inhibit the interaction between JNK and its substrate, resulting in a JNK K.O. phenotype. In contrast to pure diffusion they are actively transported into cells, where they remain until their proteolytic degradation. The c-Jun N-terminal kinases (JNK1, 2, 3), members of the mitogen-activated protein kinase (MAPK) superfamily, are activated by a wide variety of extracellular stimuli such as inflammatory cytokines, heat shock and ischemia.

Targets of JNKs are mostly transcription factors, including c-Jun, activating transcription factor(ATF) 2, and ETS-containing factors such as Elk1. Other targets having function regulated by JNK-mediated phosphorylation include insulin receptor substrate 1 and Bcl-2.

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