285983-48-4|Doramapimod|Doramapimod, p38 MAPK inhibitor|Not available-范德生物科技公司

Doramapimod

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names：
Doramapimod, p38 MAPK inhibitor
CAS号：
285983-48-4
MDL Number： Not available
MF(分子式)： C31H37N5O3 MW(分子量)： 527.66
EINECS:Not available Reaxys Number:NA
Pubchem ID:156422 Brand:BIOFOUNT

应激激活的p38丝裂原激活蛋白激酶（MAPK）在调节促炎细胞因子（如肿瘤坏死因子和白细胞介素-1）的产生中起着关键作用。多拉莫德是p38 MAPK的高效抑制剂，Kd值为0.1 nM，阻断LPS刺激的THP-1细胞中的TNFα释放，IC50值为18 nM.1在10μM时，多拉马匹莫德在体外抑制JNK2α2，但在抑制p38 MAPK所需的低浓度下，它不影响细胞中JNK底物的磷酸化。

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中文别名	285983-48-4;达马莫德;多拉马匹莫德;p38MAPK抑制剂
英文别名	BIRB 796;BIRB796; BIRB-796;Doramapimod;p38 MAPK inhibitor;1kv2;S1574_Selleck;Kinome_2137
CAS号	285983-48-4
Inchi	InChI=1S/C31H37N5O3/c1-22-9-11-23(12-10-22)36-29(21-28(34-36)31(2,3)4)33-30(37)32-26-13-14-27(25-8-6-5-7-24(25)26)39-20-17-35-15-18-38-19-16-35/h5-14,21H,15-20H2,1-4H3,(H2,32,33,37)
InchiKey	MVCOAUNKQVWQHZ-UHFFFAOYSA-N
分子式 Formula	C31H37N5O3
分子量 Molecular Weight	527.66
溶解度Solubility
性状	Solid powder
储藏条件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

产品说明	多拉莫德是p38 MAPK的高效抑制剂，Kd值为0.1 nM，阻断LPS刺激的THP-1细胞中的TNFα释放，IC50值为18 nM.1在10μM时，多拉马匹莫德在体外抑制JNK2α2，但在抑制p38 MAPK所需的低浓度下，它不影响细胞中JNK底物的磷酸化。
Introduction	Doramapimod is a highly potent inhibitor of p38 MAPK with a Kd value of 0.1 nM that blocks TNFα release in LPS-stimulated THP-1 cells with an IC50 value of 18 nM.1 At 10 μM, doramapimod inhibits JNK2α
Application1
Application2
Application3

警示图
危险性	Warning
危险性警示
安全声明
安全防护
备注

[1]Dietrich J, Hulme C, Hurley LH. The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796. Bioorg Med Chem. 2010 Aug 1;18(15):5738-48. Epub 2010 Jun 4. PubMed PMID: 20621496.

[2]Joos H, Albrecht W, Laufer S, Brenner RE. Differential effects of p38MAP kinase inhibitors on the expression of inflammation-associated genes in primary, interleukin-1beta-stimulated human chondrocytes. Br J Pharmacol. 2010 Jul;160(5):1252-62. PubMed PMID: 20590617.

[3] Page TH, Brown A, Timms EM, Foxwell BM, Ray KP. p38 inhibitors suppress cytokine production in RA synovial membranes: Does variable inhibition of IL-6 production limit effectiveness in vivo? Arthritis Rheum. 2010 Jun 29. [Epub ahead of print] PubMed PMID: 20589681.

[4] Namboodiri HV, Bukhtiyarova M, Ramcharan J, Karpusas M, Lee Y, Springman EB. Analysis of imatinib and sorafenib binding to p38alpha compared with c-Abl and b-Raf provides structural insights for understanding the selectivity of inhibitors targeting the DFG-out form of protein kinases. Biochemistry. 2010 May 4;49(17):3611-8. PubMed PMID: 20337484.

[5] Chopra P, Kulkarni O, Gupta S, Bajpai M, Kanoje V, Banerjee M, Bansal V, Visaga S, Chatterjee M, Chaira T, Shirumalla RK, Verma AK, Dastidar SG, Sharma G, Ray A. Pharmacological profile of AW-814141, a novel, potent, selective and orally active inhibitor of p38 MAP kinase. Int Immunopharmacol. 2010 Apr;10(4):467-73. Epub 2010 Jan 20. PubMed PMID: 20093202.

6: Turpeinen T, Nieminen R, Moilanen E, Korhonen R. Mitogen-activated protein kinase phosphatase-1 negatively regulates the expression of interleukin-6, interleukin-8, and cyclooxygenase-2 in A549 human lung epithelial cells. J Pharmacol Exp Ther. 2010 Apr;333(1):310-8. Epub 2010 Jan 20. PubMed PMID: 20089808.7: Tecle H, Feru F, Liu H, Kuhn C, Rennie G, Morris M, Shao J, Cheng AC, Gikunju D, Miret J, Coli R, Xi SH, Clugston SL, Low S, Kazmirski S, Ding YH, Cao Q, Johnson TL, Deshmukh GD, DiNitto JP, Wu JC, English JM. The design, synthesis and potential utility of fluorescence probes that target DFG-out conformation of p38alpha for high throughput screening binding assay. Chem Biol Drug Des. 2009 Dec;74(6):547-59. Epub 2009 Oct 20. PubMed PMID: 19843080.8: Engstrom L, Pinzon-Ortiz MC, Li Y, Chen SC, Kinsley D, Nelissen R, Fine JS, Mihara K, Manfra D. Characterization of a murine keyhole limpet hemocyanin (KLH)-delayed-type hypersensitivity (DTH) model: role for p38 kinase. Int Immunopharmacol. 2009 Sep;9(10):1218-27. Epub 2009 Jul 16. PubMed PMID: 19616132.9: Han S, Mistry A, Chang JS, Cunningham D, Griffor M, Bonnette PC, Wang H, Chrunyk BA, Aspnes GE, Walker DP, Brosius AD, Buckbinder L. Structural characterization of proline-rich tyrosine kinase 2 (PYK2) reveals a unique (DFG-out) conformation and enables inhibitor design. J Biol Chem. 2009 May 8;284(19):13193-201. Epub 2009 Feb 25. PubMed PMID: 19244237; PubMed Central PMCID: PMC2676051.10: Genovese MC. Inhibition of p38: has the fat lady sung? Arthritis Rheum. 2009 Feb;60(2):317-20. PubMed PMID: 19180514.

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