Doramapimod | CAS:285983-48-4

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Name:Doramapimod; BIRB 796
Cat. No. :CS-0219
CAS No. :285983-48-4
Formula:C31H37N5O3
M. Wt. : 527.66
Solubility:10 mM in DMSO

Doramapimod is a highly potent p38α inhibitor with an IC50 of 4 nM, also inhibits B-Raf with an IC50 of 83 nM and Abl with an IC50 of 14.6 μM. IC50 & Target: IC50: 4 nM (p38α), 83 nM (B-Raf)[1]In Vitro: Doramapimod (BIRB 796) is a highly potent inhibitor of p38α, a serine/threonine mitogen activated protein kinase (MAPK) that is usually associated with inflammation because of its role in T-cell proliferation and cytokine production[1]. Doramapimod (BIRB 796) is a picomolar inhibitor of human p38 MAP kinase[2]. HEK293 cells are incubated with different concentrations of Doramapimod (BIRB 796) for 30 min or 2 h prior to stimulation with sorbitol (an osmotic shock) and examined the activation of MAPKAP-K2 by measuring its activity. MAPKAP-K2 activation is inhibited in these cells in a time-dependent manner with an apparent IC50 of 30 nM after 30 min or 8 nM after 2 h of preincubation with Doramapimod[3].In Vivo: The mean xenograft weigh of Doramapimod (BIRB 796) plus Paclitaxel group (1.14±0.48 g) is lighter than control, Doramapimod or Paclitaxel group (1.84±0.61, 1.80±0.62 and 1.65±0.29 g) (P[4]. The Doramapimod (BIRB 796) treatment slightly reduces blood pressure (166±7 mm Hg at week 7; P[5].

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