BIRB 796 (Doramapimod)

BIRB 796 (Doramapimod)はp38αMAPKの高さ選択阻害剤、THP-1細胞に作用する時、EC50が18nMになる。

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BIRB 796 (Doramapimod) 化学構造
分子量: 527.66



Quality Control & MSDS


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情報 BIRB 796 (Doramapimod)はp38αMAPKの高さ選択阻害剤、THP-1細胞に作用する時、EC50が18nMになる。
目標 p38α MAPK
IC50 0.1 nM (Kd) [1]
In vitro試験 BIRB 796 shows no significant inhibition to ERK-1, SYK, IKK2β, ZAP-70, EGF receptor kinase, HER2, protein kinase A (PKA), PKC, PKC-α, PKC-β (I and II) and PKC-γ. BIRB 796 greatly improves binding affinity by forming a hydrogen bond between the morpholine oxygen and the ATP-binding domain of p38α. BIRB 796 represents one of the most potent and slowest dissociating inhibitors against human p38 MAP kinase now known. [1] BIRB 796 potently inhibits c-Raf-1 and Jnk2α2 with IC50 of 1.4 and 0.1 nM, respectively. [2] BIRB796 also inhibits the activity and the activation of SAPK3/p38γ at a higher concentration than it does in p38α. BIRB796 blocks the stress-induced phosphorylation of the scaffold protein SAP97, which is a physiological substrate of SAPK3/p38γ. BIRB796 blocks JNK1/2 activation and activity in HEK293 cells, while not inhibits the activation and activity of ERK1/ERK2 in Hela cells. Moreover, the binding of BIRB796 to the p38 MAPKs or JNK1/2 is impairing their phosphorylation by the upstream kinase MKK6 or MKK4 rather than enhancing their dephosphorylation. [3] BIRB 796 blocks baseline and bortezomib-triggered upregulation of p38 MAPK and Hsp27 phosphorylation, thereby enhancing cytotoxicity and caspase activation. BIRB 796 downregulates IL-6 and VEGF secretion in BMSCs triggered by TNF-α and TGF-β1. [4] BIRB-796 has a pyrazole scaffold that places a lipophilic t-butyl group into the lower selectivity site and a tolyl ring into the upper selectivity site. BIRB-796 also inhibits B-Raf and Abl with IC50 of 83 nM and 14.6 μM, respectively. [5]
In vivo試験 BIRB 796 (30 mg/kg) inhibits 84% of TNF-α in LPS-stimulated mice and demonstrates efficacy in a mouse model of established collagen-induced arthritis. [1] BIRB 796 has good pharmacokinetic performance even after oral administration in mice. [2]
臨床試験 Boehringer Ingelheim has announced the discontinuation of BIRB 796 R&D project in 2005.
特集 The first p38 MAPK inhibitor to be tested in a phase III clinical trial.

推薦された実験操作 (公開の文献だけ)

キナーゼアッセイ: [6]

Procedures for the THP-1 cellular assay for inhibition of LPS-stimulated TNF-α production THP-1 cells are preincubated in the presence and absence of BIRB 796 for 30 min. Cell mixture is stimulated with LPS (1 μg/mL final) and incubation continued overnight (18−24 hours) as above. Supernatant is analyzed for human TNF-α by a commercially available ELISA. Data are combined and analyzed by nonlinear regression using a three parameter logistic model to obtain an EC50 value. BIRB 796 is analyzed in each experiment and the 95% confidence intervals for the EC50 are between 16 and 22 nM.

動物実験: [2]

動物モデル Collagen-induced arthritis in female Balb/c mice
製剤 70% PEG400 (intravenous) or 100% PEG400 (oral)
投薬量 1 mg/kg (intravenous) or 10 mg/kg (oral)
管理 Intravenous injection or by oral



Download BIRB 796 (Doramapimod) SDF
分子量 527.66


CAS No. 285983-48-4
別名 N/A
溶解度 (25°C)
  • DMSO 106 mg/mL
  • 水 <1 mg/mL
  • エタノール 106 mg/mL
保管 2年 -20°C
6月-80°Cin DMSO
化学名 1-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)-3-(4-(2-morpholinoethoxy)naphthalen-1-yl)urea


カスタマーレビュー (1)

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Source BIRB 796 (Doramapimod) purchased from Selleck
Method Western blot
Cell Lines HEK293 cells
Concentrations 0.01-1 μM
Incubation Time 1 h
Results BIRB796 treatment resulted in a reduction of p38 phosphorylation in HEK293 cells.

製品表彰状 (7)

  • RNAi screen identifies MAPK14 as a druggable suppressor of human hematopoietic stem cell expansion. [Baudet A, et al. Blood 2012;119(26):6255-8]

    PubMed: 22555972
  • Novel function for the p38-MK2 signalling pathway in circulating CD1c+ (BDCA-1+) myeloid dendritic cells from healthy donors and advanced cancer patients; inhibition of p38 enhances IL-12 whilst suppressing IL-10. [Franks HA, et al. Int J Cancer 2013;134(3):575-86]

    PubMed: 23901045
  • Glucose induces autophagy under starvation conditions by a p38 MAPK-dependent pathway. [Moruno-Manchón JF, et al. Biochem J 2013;449(2):497-506]

    PubMed: 23116132
  • Blocking p38/ERK crosstalk affects colorectal cancer growth by inducing apoptosis in vitro and in preclinical mouse models. [Chiacchiera F, et al. Cancer Lett 2012;324(1):98-108]

    PubMed: 22579651
  • Joint inhibition of TOR and JNK pathways interacts to extend the lifespan of Brachionus manjavacas (Rotifera). [Snell TW, et al. Exp Gerontol 2014;10.1016/j.exger.2014.01.022]

    PubMed: 24486130
  • BIRB796, the Inhibitor of p38 Mitogen-Activated Protein Kinase, Enhances the Efficacy of Chemotherapeutic Agents in ABCB1 Overexpression Cells. [He D, et al. PLoS One 2013;8(1):e54181]

    PubMed: 23349819
  • p38 Mitogen-activated protein kinase and extracellular signal regulated kinase signaling pathways are not essential regulators of formyl peptide-stimulated p47(phox) activation in neutrophils. [Tsai YR, et al. Eur J Pharmacol 2013;701(1-3):96-105]

    PubMed: 23348708



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