Hotline:400-820-3792

Inhibitors?ScreeningLibraries?Proteins

www.MedChemE

Doramapimod(Standard)

Cat.No.:HY-10320R

CASNo.:285983-48-4

Synonyms:BIRB796(Standard)

分?式:C??H??N?O?

分?量:527.66

作?靶点:p38MAPK;Raf;Autophagy

作?通路:MAPK/ERKPathway;Autophagy

储存?式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

?物活性Doramapimod(Standard)是Doramapimod的分析标准品。本产品?于研究及分析应?。Doramapimod

(BIRB796)是?种具有?服活性的，?效的p38MAPK抑制剂，IC50值分别为p38α=38nM，p38β=65

nM，p38γ=200nM，p38δ=520nM。Doramapimod对p38激酶具有?摩尔亲和?(Kd=0.1nM)。

Doramapimod也抑制B-Raf和Abl，IC50分别为83nM和14.6μM[1][2]。

IC50TargetIC50:4nM(p38α),83nM(B-Raf)[1]

REFERENCES

[1].DietrichJ,etal.Thedesign,synthesis,andevaluationof8hybridDFG-outallosterickinaseinhibitors.BioorgMedChem.2010Aug

1;18(15):5738-48

[2].CicenasJ,etal.JNK,p38,ERK,andSGK1InhibitorsinCancer.Cancers(Basel).2017Dec21;10(1).pii:E1.

[3].KumaY,etal.BIRB796inhibitsallp38MAPKisoformsinvitroandinvivo.JBiolChem,2005,2