Potent, selective, ATP competitive JNK inhibitor (IC 50 values are 150, 220 and 70 nM for hJNK1,2 and 3 respectively). Reduces cell adhesion and migration in cancer cells. anti-ischemic effects in vivo .
Storage Temp
Store at -20°C,Desiccated
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of mitogen-activated protein kinase 10
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
Store at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months.
product description：
A cell-permeable pyrimidinyl compound that displays anti-inflammatory properties. Acts as a potent, reversible, and ATP-competitive inhibitor of c-Jun N-terminal kinase (JNK, IC50 = 150, 220, and 70 nM for hJNK1, hJNK2, and hJNK3, respectively) with a 10- to 100-fold greater selectivity over a panel of 25 other commonly studied kinases (IC50 typically in the range of 1-10 µM or no effect at 10 µM). Its in vivo efficacy has been demonstrated in gerbils, mice, and rats via oral, i.v., or i.p. administration.
Biochemical mechanism:
Cell permeable: yes
Product competes with ATP.
Primary Target
hJNK 1, hJNK 2, hJNK 3
Reversible: yes
Target IC50: 150, 220, and 70 nM for hJNK1, hJNK2, and hJNK3, respectively
Associated Targets(Human)
MAPK10TchemMitogen-activated protein kinase 10 (1 Activities)
1.Gaillard P, Jeanclaude-Etter I, Ardissone V, Arkinstall S, Cambet Y, Camps M, Chabert C, Church D, Cirillo R, Gretener D et al.. (2005) Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase.. J Med Chem, 48 (14):(4596-607). [PMID:15999997]
2.Ivshina MP et al.. (2022) CPEB1 regulates the inflammatory immune response, phagocytosis, and alternative polyadenylation in microglia.. Glia, 70 (10):(1850-1863). [PMID:35635122]
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B2318670