tnf-a-in-9

TNF-α-IN-9 是一种 NDM-1 inhibitor-3类似物，是一种 TNF-α 抑制剂。TNF-α-IN-9 显示低抑制活性。

MG-T-19是一种TIM-3抑制剂（KD=0.26 μM），显著抑制TIM-3与PtdSer、CEACAM1和Gal-9的相互作用，增加PBMCs中TNF-α和IFN-γ的产生，从而重新激活T细胞对肿瘤的攻击能力。

CU-T12-9 是特异性 TLR1 2激动剂，可激活先天免疫系统和适应性免疫系统。它选择性激活 TLR1 2 异二聚体，可通过促进 TLR1 和 TLR2 二聚而激活 NF-κB 信号，引起下游 TNF-α、IL-10 和 iNOS 增加。

PDE1-IN-9 (Compound 7a) 为磷酸二酯酶 1 (PDE1) 的选择性抑制剂，其可抑制PDE1C，IC50为11 nM。PDE1-IN-9 能降低IL-1β、IL-6、TNF-α 和 iNOS的mRNA表达，并抑制一氧化氮 (NO) 和活性氧 (ROS) 的产生。此外，该化合物在大鼠肝微粒体中显示出良好的代谢稳定性。

CB2 receptor agonist 9 (Compound 33) 是一种有效的口服大麻素受体 2 (CB2 receptor) 激动剂，EC50 为 16.2 nM。CB2 receptor agonist 9 能抑制 TNF-α、IL-1β 和 IL-6 的表达，并在 DDS 诱导的小鼠急性结肠炎模型中显示抗炎活性。

9(Z),11(E)-Conjugated linoleic acid is an isomer of linoleic acid that has been found in beef and milk fat.1It binds to peroxisome proliferator-activated receptor α (PPARα; IC50= 140 nM) and activates the receptor in a reporter assay using COS-1 cells expressing mouse PPARα when used at a concentration of 100 μM.29(Z),11(E)-Conjugated linoleic acid inhibits TNF-α-inducedGLUT4expression and increases insulin-stimulated glucose transport in 3T3-L1 adipocytes.3Dietary administration of 9(Z)11(E)-conjugated linoleic acid reduces serum fasting glucose, insulin, and triglyceride levels and decreases white adipose tissue macrophage infiltration inob obmice. It also increases body weight gain and body fat in weanling mice.4[Matreya, LLC. Catalog No. 1278] 1.Shultz, T.D., Chew, B.P., Seaman, W.R., et al.Inhibitory effect of conjugated dienoic derivatives of linoleic acid and β-carotene on the in vitro growth of human cancer cellsCancer Lett.63(2)125-133(1992) 2.Moya-Camarena, S.Y., Heuvel, J.P.V., Blanchard, S.G., et al.Conjugated linoleic acid is a potent naturally occurring ligand and activator of PPARαJ. Lipid Res.40(8)1426-1433(1999) 3.Moloney, F., Toomey, S., Noone, E., et al.Antidiabetic effects of cis-9, trans-11-conjugated linoleic acid may be mediated via anti-inflammatory effects in white adipose tissueDiabetes56(3)574-582(2007) 4.Pariza, M.W., Park, Y., and Cook, M.E.The biologically active isomers of conjugated linoleic acidProg. Lipid Res.40(4)283-298(2001)

MMP-9 inhibitor I is an inhibitor of matrix metalloproteinase-9 (MMP-9) that is selective over MMP-1 and MMP-13 (IC50s = 5, 1,050, and 113 nM, respectively). It also decreases the activity of TNF-α converting enzyme (TACE) in a dose-dependent manner (IC50 = 0.54 μM). MMP-9 inhibitor I decreases TNF-α secretion stimulated by LPS in BV-2 microglial cells when used at concentrations of 50 and 100 μM.

GSK-J4 Hydrochloride (GSK J4 HCl) 是 H3K27me3 me2 去甲基化酶 JMJD3 KDM6B 和 UTX KDM6A 双抑制剂，IC50分别为 8.6 和 6.6 μM。它是 GSK-J1 的乙酯衍生物，体外 IC50 值大于 50 μM。它抑制 LPS 诱导的人原代巨噬细胞产生 TNF-α，IC50值为 9 μM。

UCB-5307 是一种小分子化合物，可在体外抑制 TNFR1 信号转导和下游功能。 人 TNFα 的 KD 为 9 nM。 TNF 直接通过缓慢的结合动力学结合，KD = 6 nM。 UCB-5307 可以通过预制的 hTNF hTNFR1 复合物。

Glucocorticoid receptor modulator1 是一种高效且具有口服活性的 NF-κB 和 AP-1抑制剂，IC50分别为 9 nM 和 130 nM。Glucocorticoid receptor modulator1 可有效降低炎症因子 IL-6、IL-1β、TNF-α 的表达，可缓解小鼠皮炎。

3-Hydroxyxanthone (3-Hydroxy-xanthen-9-one) 是一种具有抗炎活性的氧杂蒽酮化合物。它能抑制人脐静脉内皮细胞（HUVEC）中NADPH催化的脂质过氧化，并且阻止TNF-α所诱导的ICAM-1表达。

PON-PC, an oxidized phospholipid with a 9-carbon fatty acyl chain ending in an aldehyde at the sn-2 position, arises from the oxidation of palmitoyl oleoyl phosphatidylcholine (POPC) or through interaction with ozone in pulmonary surfactant. It is found in oxidized LDL. At a 40 µM concentration, PON-PC diminishes the production of TNF-α, nitric oxide (NO), and NADP+ in primary mouse alveolar macrophages and lowers the bactericidal capability of RAW 264.7 cells. Additionally, levels of PON-PC increase in the bronchoalveolar lavage fluid (BALF) of mice exposed to cigarette smoke or in older mice.

TIC10g，作为TLR7和TLR9（Toll样受体7和9）的双重抑制剂，能够在小鼠巨噬细胞（IC50为14.5 μM和6.5 μM）及人类B淋巴细胞（IC50为7.69 μM和11.5 μM）中抑制由TLR7和TLR9介导的TNF-α释放。此外，TIC10g还能抑制NF-κB与MAPK的活化，显示出对系统性红斑狼疮和类风湿性关节炎的抗炎活性。