p38-α mapk-in-5

p38-α MAPK-IN-5 是一种有效的 p38α抑制剂，对 p38α、p38 β、p38γ、p38δ 的 IC50分别为 0.1 nM、0.2 nM、944 nM、4100 nM。p38-α MAPK-IN-5 具有抗炎作用，并且具有用于哮喘和慢性阻塞性肺病 (COPD) 研究的潜力。

SR-318 是p38 MAPK 的选择性抑制剂，对 p38α，p38β 和 p38α β 的IC50分别为 5 nM，32 nM 和 6.11 μM。它有效抑制全血中TNF-α的释放，IC50为 283 nM。它显示出抗癌和抗炎活性。

Neochlorogenic acid (trans-5-O-Caffeoylquinic acid) 是在干果和其他植物中发现的一种多酚类天然产物，可抑制iNOS 和COX-2蛋白表达，抑制TNF-α和IL-1β产生，还抑制磷酸化的NF-κB p65和p38 MAPK 活化。

p38 MAPK inhibitor (IC50 = 0.38 μM). Inhibits the release of IL-1β and TNF-α in a peripheral blood mononuclear cell (PBMC) assay (IC50 values are 0.039 and 0.16 μM respectively). Laufer et al (2003) Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. J.Med.Chem. 46 3230 PMID:12852754 |Kammerer et al (2007) Pharmacokinetics of ML3403 ({4-[5-(4-fluorophenyl)-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-(1-phenylethyl)-amine), a 4-pyridinylimidazole-type p38 mitogen-activated protein kinase inhibitor. Drug Metab.Dispos. 35 875 PMID:17344341

Sauchinone 是一种从Saururus chinensis 中获得的非对映异构的木脂素。它通过抑制I-κBα磷酸化和p65核易位来抑制 LPS 诱导的 iNOS，TNF-α 和 COX-2 表达。它具有抗炎和抗氧化活性。

Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5 μM) inhibits the proliferation of KG-1a leukemia cells.3 1.Garvin, L.K., Green, N., Hu, Y., et al.Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: Synthesis and structure-activity relationshipsBioor. Med. Chem. Lett.15(23)5288-5292(2005) 2.Wang, X., and Studzinski, G.P.Expression of MAP3 kinase COT1 is up-regulated by 1,25-dihydroxyvitamin D3 in parallel with activated c-jun during differentiation of human myeloid leukemia cellsJ. Steroid. Biochem. Mol. Biol.121(1-2)395-398(2010) 3.Wang, X., Gocek, E., Novik, V., et al.Inhibition of Cot1/Tlp2 oncogene in AML cells reduces ERK5 activation and up-regulates p27Kip1 concomitant with enhancement of differentiation and cell cycle arrest induced by silibinin and 1,25-dihydroxyvitamin D3Cell Cycle9(22)4542-4551(2010)