p38 MAP Kinase Inhibitor XX, MW108 - CAS 1628503-09-2 - Calbiochem

A cell-permeable, aminopyridazine derivative that acts as a highly selective, active site targeted, and stable inhibitor of neuronal p38 alpha MAP Kinase (K_i = 114 nM) and exhibit about 10-fold greater selectivity over casein kinase 1d (IC₅₀ >1 µM). Does not exhibit any significant inhibitory activity against a panel of 290 protein kinases. Exhibits desirable aqueous solubility and blood-brain barrier permeability. Binds to human p38 alpha with DFG-in conformation, but without inducing a glycine flip conformational change. Reduces lipopolysaccharide and TLR-ligand-induced overproduction of IL-1b (IC₅₀ = 610 nM). Also shown to ameliorate Aβ42-induced memory impairment and improve synaptic functions in mice (~ 5 mg/kg, i.p).

A cell-permeable, aminopyridazine derivative that acts as a highly selective, active site targeted, and stable inhibitor of neuronal p38 alpha MAP Kinase (K_i = 114 nM) and exhibit about 10-fold greater selectivity over casein kinase 1d (IC₅₀ >1 µM). Does not exhibit any significant inhibitory activity against a panel of 290 protein kinases. Exhibits desirable aqueous solubility and blood-brain barrier permeability. Binds to human p38 alpha with DFG-in conformation, but without inducing a glycine flip conformational change. Reduces lipopolysaccharide and TLR-ligand-induced overproduction of IL-1b (IC₅₀ = 610 nM). Also shown to ameliorate Aβ42-induced memory impairment and improve synaptic functions in mice (~ 5 mg/kg, i.p).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Cell permeable: yes

Primary Target
p38a MAPK

Reversible: yes

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

Watterson, D.M., et al. 2013.PLos One.8, e66226.

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

Toxicity: Standard Handling (A)