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Doramapimod

产品编号 T6277 CAS 285983-48-4

别名: BIRB 796, 达马莫德, 度马莫德

Doramapimod 是一种具有口服活性的p38 MAPK 抑制剂，Kd 值为0.1nM。它也抑制B-Raf 和 Abl，IC50分别为 83 nM 和 14.6 μM。

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Doramapimod, CAS 285983-48-4

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参考文献

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产品描述	Doramapimod is a highly potent inhibitor of p38 MAPK (Kd: 0.1 nM), but weakly inhibits c-RAF, Fyn, Lck, ERK-1, SYK, IKK2, and ZAP-70.
靶点活性	p38 MAPK:0.1 nM (Kd, cell free)
体外活性	Doramapimod (BIRB796) is a highly potent inhibitor of p38 MAPK (Kd: 0.1 nM) that blocks TNFα release in LPS-stimulated THP-1 cells (IC50: 18 nM) [1]. BIRB796 also inhibits the activity and the activation of SAPK3/p38gamma. BIRB796 blocks the stress-induced phosphorylation of the scaffold protein SAP97 [2]. BIRB 796 inhibited Hsp27 phosphorylation induced by 17-AAG plus bortezomib, thereby enhancing cytotoxicity. In bone marrow stromal cells (BMSC), BIRB 796 inhibited phosphorylation of p38 MAPK and secretion of IL-6 and vascular endothelial growth factor triggered by either tumour necrosis factor-alpha or tumour growth factor-beta1. BIRB 796 also inhibited IL-6 secretion induced in BMSCs by adherence to MM cells, thereby inhibiting tumour cell proliferation [3].
体内活性	Systolic blood pressure of untreated dTGRs was 204 mm Hg, but partially reduced after BIRB796 (30 mg/kg per day) treatment (166 mm Hg), whereas Sprague-Dawley rats were normotensive. The beta-myosin heavy chain expression of BIRB796-treated hearts was significantly lower in BIRB796 compared with dTGRs. BIRB796 treatment significantly reduced cardiac fibrosis, connective tissue growth factor, tumor necrosis factor-alpha, interleukin-6, and macrophage infiltration [4].
激酶实验	Binding studies are conducted in a buffer containing 20 mM Bis-Tris Propane, pH 7.0, 2 mM EDTA, 0.01% (w/v) NaN3 and 0.15% (w/v) n-octylglucoside. Kinetic data for the association of SK&F 86002 to p38 MAP kinase is collected on a Kintech fluorescence detector system equipped with a stopped-flow controller. The data are fit simultaneously to an appropriate equation describing kinetic binding for a simple one-step binding mechanism. The data for the binding of the fluorescent analog of BIRB 796 is corrected for background fluorescence of unbound ligand. The exchange curve assays are run as two half-reactions using an SLM Aminco Bowman Series 2 Model SQ-340 fluorescence detector. In the first half-reaction, p38 MAP kinase and SK&F 86002 are preincubated for 3 min. In the second half-reaction, p38 MAP kinase is preincubated with Doramapimod for 60 min. A net dissociation of the fluoroprobe is observed for the first half-reaction, and a net association is observed for the second half-reaction. The raw data from both half reactions are fit simultaneously to an equation describing simple competitive inhibition. p38 is preactivated by treatment with constitutively active recombinant MKK6 (prepared by mutagenizing the two activation residues, Ser189 and Thr193, to Glu residues). Activated p38 is purified and used as a source of enzyme in a standard kinase activity assay monitoring the incorporation of radioactive phosphate into recombinant human MAPKAP k2. Cellular assays follow published procedures. Briefly, human THP.1 cells are stimulated with 1 μg/mL LPS, in the presence or absence of compound, followed by the determination of released TNF using a commercial ELISA kit [1].
细胞实验	Human embryonic kidney (HEK) 293 and HeLa cells were cultured in Dulbecco's modified Eagle's medium at 37 °C, supplemented with 10% fetal calf serum, 50 units of penicillin/ml, 50 μg/ml streptomycin, and 2 mM glutamine. Mouse embryonic fibroblasts were cultured as described previously, and C2C12 myoblasts were cultured. Cells were exposed to 0.5 M sorbitol for 30 min or 100 ng/ml EGF for 10 min and then lysed in buffer A (50 mM Tris-HCl, pH 7.5, 1 mM EGTA, 1 mM EDTA, 1 mM sodium orthovanadate, 10 mM sodium fluoride, 50 mM sodium β-glycerophosphate, 5 mM pyrophosphate, 0.27 M sucrose, 0.1 mM phenylmethylsulfonyl fluoride, 1% (v/v) Triton X-100) plus 0.1% (v/v) 2-mercaptoethanol and Complete proteinase inhibitor mixture from Roche Applied Science. Lysates were centrifuged at 18,000 × g for 5 min at 4 °C, and the supernatants were removed, quick-frozen in liquid nitrogen, and stored at –20 °C until use. When required, cells were preincubated for 1 h without or with 10 μM SB 203580 or 10 μM PD 184352 or with different concentrations of BIRB796 for the times indicated in the figures [2].
动物实验	We studied male transgenic dTGRs and age-matched nontransgenic Sprague–Dawley (SD) rats (MDC). Local authorities approved the studies, and American Physiological Society guidelines for animal care were followed. We performed 2 different protocols. In protocol 2, untreated dTGR (n=15), dTGR+BIRB796 (30 mg/kg per day in the diet for 3 weeks; n=11), and SD (n=8 each group) rats were analyzed. Systolic blood pressure was measured weekly by tail cuff. Twenty-four– hour urine samples were collected in metabolic cages from weeks 5 to 7. Serum was collected at week 7. Serum creatinine and cystatin C were measured by clinical routine assays. Urinary rat albumin was determined by enzyme-linked immunosorbent assay. The aim of protocol 2 was to focus on electrophysiological alterations and mortality. Untreated dTGR (n=10), dTGR+BIRB796 (n=10), and SD (n=10) rats were studied up to week 8. Cardiac magnetic field mapping (CMFM) was performed at week 7 under isoflurane anesthesia. Echocardiography was performed as described earlier [4].

别名	BIRB 796, 达马莫德, 度马莫德
分子量	527.66
分子式	C31H37N5O3
CAS No.	285983-48-4

存储

　|　Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

Ethanol: 26.4 mg/mL (50 mM)

DMSO: 52.8 mg/mL (100 mM)

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Pargellis C, et al. Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site. Nat Struct Biol, 2002, 9(4), 268-272. 2. Kuma Y, et al. BIRB796 inhibits all p38 MAPK isoforms in vitro and in vivo. J Biol Chem, 2005, 280(20), 19472-19479. 3. Yasui H, et al. BIRB 796 enhances cytotoxicity triggered by bortezomib, heat shock protein (Hsp) 90 inhibitor, and dexamethasone via inhibition of p38 mitogen-activated protein kinase/Hsp27 pathway in multiple myeloma cell lines and inhibits paracrine tumour growth. Br J Haematol. 2007 Feb;136(3):414-23. 4. Park JK, et al. p38 mitogen-activated protein kinase inhibition ameliorates angiotensin II-induced target organ damage. Hypertension. 2007 Mar;49(3):481-9. 5. Zhao L, Wang Y, Xu Y, et al. BIRB796, an Inhibitor of p38 Mitogen-Activated Protein Kinase, Inhibits Proliferation and Invasion in Glioblastoma Cells[J]. ACS Omega. 2021 6. Yuan F, Liu B, Xu Y, et al. TIPE3 is a regulator of cell apoptosis in glioblastoma[J]. Cancer letters. 2019 Apr 1;446:1-14.

文献引用

1. Yuan F, Liu B, Xu Y, et al. TIPE3 is a regulator of cell apoptosis in glioblastoma. Cancer Letters. 2019, 446: 1-14 2. Zhao L, Wang Y, Xu Y, et al. BIRB796, an Inhibitor of p38 Mitogen-Activated Protein Kinase, Inhibits Proliferation and Invasion in Glioblastoma Cells. ACS Omega. 2021 Apr 22;6(17):11466-11473. doi: 10.1021/acsomega.1c00521.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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配液计算器

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浓度

容积

分子量

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容积 (起始)

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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Doramapimod 285983-48-4 Autophagy MAPK Raf p38 MAPK Raf kinases BIRB-796 inhibit BIRB 796 达马莫德度马莫德 BIRB796 Inhibitor inhibitor

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Doramapimod

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