LosmaPimod 是一种可口服的特异性 p38 MAPK 抑制剂，抑制 p38α 和 p38β 的pKi值分别为 8.1 和 7.6。

Losmapimod (GW856553X; SB856553; GSK-AHAB) is a specific, potent, and orally active p38 MAPK inhibitor (pKi: 8.1/7.6 for p38α/β).

DNA binding assays: All reactions are performed in black non-binding polystyrene 384-well plates with reaction volumes of 30–100 μL. Purified DNA strand exchange proteins and chemical compounds are pre-incubated at room temperature for 5 minutes; they are then further incubated at 37°C for 30 min with 100 nM of ssDNA substrate, consisting of a 45-mer poly-dT tagged with Alexa 488 at the 5' terminus (synthesized and purified by Integrated DNA Technologies). Reactions are performed in 20 mM HEPES pH 7.5, 10 mM MgCl2, 0.25 μM BSA, 2% glycerol, 30 mM NaCl, 4% DMSO and 2 mM ATP. Some conditions included DTT or TCEP (tris(2-carboxyethyl)phosphine) as indicated. DNA binding is measured as a function of fluorescence polarization (FP) with a Safire2 plate reader, using the following settings: excitation 470±5 nM, emission 530±5 nM, 10 reads/well, Z height and G factor auto-calibrated from control wells. Displayed error bars represent standard deviation. For experiments involving a titration of protein concentrations, data are fit to an equation that accounts for the cooperative nature by which recombinase proteins bind DNA. For experiments involving a titration of RI-1, protein concentrations are selected to give an ～80% saturation of the FP signal in the absence of RI-1.

585543-15-3

C22H26FN3O2

383.467

6-[5-(环丙基氨基甲酰基)-3-氟-2-甲基苯基]-N-(2,2-二甲基丙基)吡啶-3-甲酰胺;SB856553;GW856553X;GSK-AHAB;洛批莫德;GW856553

H2O:<1 mgml
Ethanol:39 mg/mL (101.7 mM)
DMSO:71 mg/mL (185.2 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years