Doramapimod
Cat. No.:YN350026
CAS No. :285983-48-4
产品名称: | Doramapimod |
CAS No.: | 285983-48-4 |
Chemical Name: | N-[3-(1,1-dimethylethyl)-1-(4-methylphenyl)-1H-pyrazol-5-yl]-N'-[4-[2-(4-morpholinyl)ethoxy]-1-naphthalenyl]-urea |
Synonyms: | 达马莫德; BIRB 796 |
分子量: | 527.66 |
分子式: | C₃₁H₃₇N₅O₃ |
SMILES: | O=C(NC1=CC(C(C)(C)C)=NN1C2=CC=C(C)C=C2)NC3=C4C=CC=CC4=C(OCCN5CCOCC5)C=C3 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | Doramapimod (BIRB 796) 是一种具有口服活性的,高效的p38 MAPK抑制剂,IC50值分别为 p38α=38 nM,p38β=65 nM,p38γ=200 nM,p38δ=520 nM。Doramapimod 对 p38 激酶具有皮摩尔亲和力 (Kd=0.1 nM)。Doramapimod 也抑制B-Raf和 Abl,IC50分别为 83 nM 和 14.6 μM。 |
IC50和靶点: | [{name:"p38α:38 nM (IC50)"},{name: "p38β:65 nM (IC50)"},{name: "p38δ:520 nM (IC50)"},{name: "p38γ:200 nM (IC50)"},{name: "B-Raf:83.4 nM (IC50)"},{name: "Abl:14600 nM (IC50)"},{name: "p38 MAP kinase:0.1 nM (Kd)"}] |
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Pargellis, C., Tong, L., and Churchill, L.Inhibition of p38 MAP kinase by utilizing a novel allosteric binding siteNat. Struct. Biol.9(4),268-272(2002)
Bain, J., Plater, L., Elliot, M., et al.The selectivity of protein kinase inhibitors: A further updateBiochem. J.408(3),297-315(2007)
Kuma, Y., Sabio, G., Bain, J., et al.BIRB796 inhibits all p38 MAPK isoforms in vitro and in vivoJ. Biol. Chem.280(20),19472-19479(2005)