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Losmapimod (GSK-AHAB) 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。
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Losmapimod (GSK-AHAB) 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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 175 | 现货 | |
2 mg | ¥ 243 | 现货 | |
5 mg | ¥ 385 | 现货 | |
10 mg | ¥ 619 | 现货 | |
25 mg | ¥ 1,270 | 现货 | |
50 mg | ¥ 2,120 | 现货 | |
100 mg | ¥ 2,970 | 现货 | |
500 mg | ¥ 6,860 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 451 | 现货 |
产品描述 | Losmapimod (GSK-AHAB) (GW856553X; SB856553; GSK-AHAB) is a specific, potent, and orally active p38 MAPK inhibitor (pKi: 8.1/7.6 for p38α/β). |
靶点活性 | p38α:8.1(pKi), p38β:7.6(pKi) |
激酶实验 | 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. |
别名 | 洛批莫德, SB856553, GW856553X, GW856553, GSK-AHAB, 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 |
分子量 | 383.46 |
分子式 | C22H26FN3O2 |
CAS No. | 585543-15-3 |
Smiles | CC=1C(=CC(C(NC2CC2)=O)=CC1F)C3=CC=C(C(NCC(C)(C)C)=O)C=N3 |
密度 | 1.21 g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 39 mg/mL (101.7 mM) DMSO: 18.33 mg/mL (47.81 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
Ethanol
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