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Doramapimod
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Doramapimod
CAS No. : 285983-48-4
MCE 站:Doramapimod
产品活性: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。
研究领域:MAPK/ERK Pathway | Autophagy
作用靶点:p38 MAPK | Raf | Autophagy
In Vitro: Doramapimod (BIRB 796) is usually associated with inflammation because of its role in T-cell proliferation and cytokine production.
Doramapimod (BIRB 796) blocks the stress-induced phosphorylation of the scaffold protein SAP97, further establishing that this is a physiological substrate of SAPK3/p38γ. The binding of Doramapimod to the p38 MAPKs or JNK1/2 is impairing their phosphorylation by the upstream kinase MKK6 or MKK4.
In Vivo: The mean xenograft weigh of Doramapimod (BIRB 796) is lighter than control. The inhibition rate of Doramapimod is 1.93%.
The Doramapimod (BIRB 796) treatment slightly reduces blood pressure (166±7 mm Hg at week 7; P<0.05), whereas SD rats are normotensive (123±3 mm Hg). Despite the reduction in blood pressure, untreated and Doramapimod-treated dTGRs have similar heart weight and cardiac hypertrophy indices (heart-to-tibia ratio), which are significantly higher compare with nontransgenic SD rats (310±6 versus 307±6 versus 206±5 mg/cm, respectively; P<0.05).
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