il 20

Anti-IL-20 Antibody 是靶向 IL-20 的人源化抗体。

Anti-IL-12 p70 Antibody (20C2) 为来源于大鼠的IgG1, κ 嵌合抗体，专门针对IL-12p70(人源)。其同型对照抗体为 RatIgG1kappa, Isotype Control。

Anti-Mouse IL-6 Antibody (MP5-20F3) 是一种大鼠来源的抗小鼠IL-6 的 IgG1, κ 抗体抑制剂。

NMI 8739 (n-docosahexaenoyl dopamine) 是 D2 自身受体的激动剂。 NMI 8739 减少 NO 的产生并引起 CCL-20、MCP-1 和 IL-6 释放的浓度依赖性抑制。

PAT-048 is an effective and selective autotaxin inhibitor. PAT-048 reduces dermal fibrosis in vivo. PAT-048 also inhibits IL-6 mRNA expression but displays no effect on autotaxin protein and pulmonary lysophosphatidic acid (LPA) production in the lung fibrosis model. PAT-048 has an IC50 and IC90 of 20 nM and 200 nM for autotaxin in mouse plasma.

Immuno modulator-1 (compound 22) 在hPBMC中抑制TNFα和IL-2的分泌，IC50为4.7 nM和26 nM。同时，该化合物对hERG钾通道具阻断活性，3 μM浓度时抑制率达20%。

Y-320 是一种免疫调节剂，能阻碍IL-15刺激CD4 T 细胞后的IL-17的产生，IC50=20~60 nM。

Ginsenoside Rh1 (Sanchinoside B2) 是人参的一种主要成分，具有抗炎作用，抑制PPAR-γ，TNF-α，IL-6和IL-1β的表达。

Mizoribineprodrug-2 trifluoroacetate (compound 20) 为一种口服活性的前体药物,属于Mizoribine (氨基酸偶联).此化合物有效抑制IL-2的生成.

Potent inhibitor of NF-κB activation (IC50 = 85 nM); decreases IκBα phosphorylation. Attenuates LPS-induced nitric oxide production and expression of TNF-α, IL-6 and MCP. Suppresses proliferation of HeLa and HCT116 cells. Anti-inflammatory and antitumor. Hu et al (2007) Regulation of c-Src nonreceptor tyrosine kinase activity by bengamide A through inhibition of methionine aminopeptidases. Chem.Biol. 14 764 PMID:17656313 |Johnson et al (2012) Myxobacteria versus sponge-derived alkaloids: the bengamide family identified as potent immune modulating agents by scrutiny of LC-MS ELSD libraries. Bioorg.Med.Chem. 20 4348 PMID:22705020 |Kinder et al (2001) Synthesis and antitumor activity of ester-modified analogues of bengamide B. J.Med.Chem. 44 3692 PMID:11606134

Reslizumab (Sch 55700) 是一种人源化免疫球蛋白 G （IgG）4 κ 单克隆抗体，可与人白细胞介素 5 结合，从而减少嗜酸性粒细胞的产生和存活。Reslizumab 可改善肺功能，可诱导嗜酸性粒细胞的产生和成熟减少，可用于研究哮喘。

Limaprost (17α,20-dimethyl-δ2-PGE1) 是PGE1类似物，也是口服具有活性的血管舒张剂。它能够增加血流量以及减少血小板聚集。它具有抗心绞痛的功能，可用于疼痛的缓解，以及用于研究缺血性症状。

Tiger17是一种环状肽，属于tigerinin-RC1和tigerinin-RC2的衍生物，这两种化合物是在螃蟹吃蛙（F. cancrivora）皮肤分泌物中发现的抗微生物肽。在5至20µg/ml的浓度范围内使用时，Tiger17能增加HaCaT角质形成细胞和人类皮肤成纤维细胞的增殖，并且在20µg/ml的浓度下增加HaCaT细胞的迁移。此外，Tiger17还能增加RAW 264.7巨噬细胞的招募及其TGF-β1和IL-6的分泌。在全层皮肤创伤的小鼠模型中，局部应用20µg/ml的Tiger17能加速伤口闭合和重新上皮化的速度。

β-Defensin-3 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts. It inhibits the growth of the periodontopathogenic and cariogenic bacteria F. nucleatum, S. mutans, S. sobrinus, S. salivarius, and L. casei (MICs = 12.5-100 mg/l). It also inhibits the growth of S. aureus, S. pyogenes, P. aeruginosa, E. coli, and C. albicans. β-Defensin-3 stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes when used at a concentration of 30 μg/ml. It also stimulates calcium mobilization, migration, and proliferation of keratinocytes when used at concentrations of 30, 5, and 20 μg/ml, respectively. β-Defensin-3 induces IL-31 production by human peripheral blood-derived mast cells in vitro when used at a concentration of 10 μg/ml and by rat mast cells in vivo following a 500 ng intradermal dose.

Streptochlorin is a bacterial metabolite originally isolated from Streptomyces sp. SF2583 that has diverse biological activities, including antiangiogenic, antiproliferative, and anti-allergic properties. It inhibits TNF-α-induced NF-κB transcriptional activity and decreases proliferation of human umbilical vein endothelial cells (HUVECs) when used at concentrations ranging from 5 to 20 μM. Streptochlorin (12 μg/ml) decreases viability of, as well as induces apoptosis and increases the production of reactive oxygen species (ROS) in, Hep3B human hepatocellular carcinoma cells. It does not induce cytotoxicity in RBL-2H3 mast cells at concentrations up to 100 μM. Streptochlorin prevents degranulation in antigen-stimulated mast cells, as well as inhibits Syk kinase and the Src family kinases LYN and Fyn and reduces the secretion of TNF-α and IL-4 induced by dinitrophenyl-human serum album (DNP-HSA) in RBL-2H3 mast cells. It also decreases swelling and reduces scratching behavior in a mouse model of allergic dermatitis induced by dinitrofluorobenzene (DNFB).

Lup-20(29)-en-3-yl acetate 是 Lupeol 的衍生物，通过下调 TNF-α、IL-1β、MCP-1、COX-2、VEGF 和颗粒酶 B 来抑制类风湿性关节炎的进展。

Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM. Benpyrine tightly binds to TNF-α and blocks its interaction with TNFR1, with an IC50 value of 0.109 μM. Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research[1]. Benpyrine (5-20 μM; 14 hours; RAW264.7 cells) pretreatment results in a dose-dependent decrease in the phosphorylation of IκBα in RAW264.7 cells (stimulated with 10 ng mL TNF-α or 1 μg mL LPS). Benpyrine abolishes the TNF-α-induced nuclear translocation of NF-κB p65 in RAW264.7 cells[1].Benpyrine only blocks cell death induced by TNF-αWT and Y119A, and increases the cell survival rate up to 80%. Benpyrine does not obviously affect L57A- and Y59L-induced cytotoxicity in L929 cells[1]. Benpyrine (25-50 mg kg; oral gavage; daily; for 2 weeks; Balb c mice) treatment significantly relieves the symptoms of collagen-induced arthritis. Benpyrine dose-dependently decreases the levels of proinflammatory cytokines, such as IFN-γ, IL-1β and IL-6, and increases the concentration of the anti-inflammatory cytokine IL-10[1].Endotoxemia murine model shows that Benpyrine (25 mg kg) could attenuate TNF-α-induced inflammation, thereby reducing liver and lung injury[1]. [1]. Weiguang Sun, et al. Discovery of an Orally Active Small Molecule TNF-α Inhibitor. J Med Chem. 2020 Jul 15.

(±)19(20)-EDP ethanolamide is an ω-3 endocannabinoid epoxide and cannabinoid (CB) receptor agonist (EC50s = 108 and 280 nM for CB1 and CB2, respectively). It is produced through direct epoxygenation of docosahexaenoyl ethanolamide by cytochrome P450 (CYP) epoxygenases. (±)19(20)-EDP ethanolamide (25 μM) reduces the viability of 143B metastatic osteosarcoma cells. It decreases the production of IL-6 and increases the production of IL-10 when used at concentrations ranging from 2.5 to 10 μM in BV-2 microglia stimulated by LPS and decreases LPS-induced cytotoxicity when used at concentrations ranging from 5 to 10 μM. It also decreases nitrite production when used at a concentration of 7.5 μM, an effect that can be partially reversed by the CB2 receptor antagonist AM630 and the PPARγ antagonist GW 9662 . (±)19(20)-EDP ethanolamide induces vasodilation of isolated preconstricted bovine coronary arteries (ED50 = 1.9 μM) and reduces tube formation by human microvascular endothelial cells (HMVECs) in a Matrigel assay.

(R)-MLT-985 (compound 11) 是一种 MALT1 蛋白酶的有效抑制剂 (IC50: 3 nM)。(R)-MLT-985 在 Jurkat 细胞中对 MALT1 依赖性 IL-2 的 IC50 值为 20 nM。(R)-MLT-985 对 ABC-DLBCL 细胞中的生长和异常 CARD11 BCL10 MALT1 复合物信号传导具有抑制作用。

SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR).1 It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1 in RAW 264.7 cells. SR 1903 (20 mg kg twice per day) reduces severity score in a mouse model of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity.References1. Chang, M.R., Ciesla, A., Strutzenberg, T.S., et al. Unique polypharmacology nuclear receptor modulator blocks inflammatory signaling pathways. ACS Chem. Biol. 14(5), 1051-1062 (2019). SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR).1 It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1 in RAW 264.7 cells. SR 1903 (20 mg kg twice per day) reduces severity score in a mouse model of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity. References1. Chang, M.R., Ciesla, A., Strutzenberg, T.S., et al. Unique polypharmacology nuclear receptor modulator blocks inflammatory signaling pathways. ACS Chem. Biol. 14(5), 1051-1062 (2019).

(20R)-Protopanaxadiol ((20R)-Protopanaxdiol) 是黑参中20(R)-人参皂甙 Rg3的一种三萜皂苷代谢物。它抑制幽门螺杆菌的生长，有抗肿瘤活性和细胞毒性。

Fletikumab (NNC0109-0012) 是一种针对 IL-20 的单克隆抗体，常当作 IL-20 抑制剂使用。Fletikumab 可用于研究类风湿关节炎和银屑病。

IRBP1-20（1-20）是IRBP的一个十二肽片段，亦称视黄醇结合蛋白3，负责运输视锥细胞中的视黄醇和视黄醛至视网膜色素上皮，参与色素再生。在携带H-2b等位基因型的C57BL/6小鼠中，IRBP1-20用于诱导自身免疫性葡萄膜视网膜炎。IRBP1-20（3 µM）能增加初级小鼠脾淋巴细胞分泌IL-4、IL-5和IL-6的水平。用IRBP1-20免疫并再次挑战，可增加IFN-γ缺乏小鼠的耳部肿胀、眼部血管炎症、免疫细胞浸润和视锥细胞层损伤，以及视网膜脱落。

NLRP3-IN-20（compound 11）是一款口服活性的NLRP3炎症小体抑制剂，其抑制IL-1β分泌的IC50值为25 nM。该化合物展现出卓越的药代动力学性质，并在非酒精性脂肪性肝炎、致命性感染性休克以及结肠炎模型中证明了其显著疗效。