il 22

AZD-0284 是核受体 (RORγ) 的选择性反向激动剂。它对呼吸道疾病及斑块型寻常型银屑病具有潜在的应用价值。

SB225002 是一种有效的选择性 CXCR2 拮抗剂，抑制白介素 IL-8 与 CXCR2 的结合，IC50为 22 nM。

GSK2981278 (ROR gama modulator 1) 是 RORγ的选择性反向激动剂。它能够抑制 il17启动子的激活，并且干扰 RORγ-DNA 结合。

TF-S14 是一种 RORγt 的反向激动剂，它通过结合 RORγt 并抑制其活性来减少 Th17 细胞相关细胞因子的产生，包括 IL-17A、IL-21 和 IL-22。TF-S14 可用于研究自身免疫疾病和同种异体移植中的排斥反应。

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%。

p38 MAPK inhibitor IV is an ATP-competitive inhibitor of p38 MAP kinases with IC50 values of 0.13, 0.55, 5.47, and 8.63 μM for p38α, p38β, p38x, and p38δ, respectively, in vitro.[1] It also inhibits LPS-induced TNF-α and IL-1β cytokine production (IC50s = 22 and 44 nM, respectively) in human peripheral blood mononuclear cells.

IRAK4-IN-22 是选择性的、口服具有活力的、强效的 IRAK4 抑制剂，能够作用于 IRAK4 (IC50: 3 nM) 和 TAK1 (IC50: 17 nM)。IRAK4-IN-21 对 IL-23 的产生表现出有效的抑制作用，其 IC50值为0.10 μM。IRAK4-IN-21 能够用于研究自身免疫性疾病，如斑块状银屑病和银屑病关节炎。

RORγt Inverse agonist 10 is a highly potent and orally bioavailable compound that acts as an antagonist for the retinoic acid receptor-related orphan nuclear receptor gamma t (RORγt). With an IC50 of 51 nM, it effectively inhibits the activity of RORγt, a prominent transcription factor involved in the regulation of genes associated with the pathogenesis of psoriasis, including IL-17A, IL-22, and IL-23R.

Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat (ITF2357) suppresses total LPS-induced IL-1β production robustly compared with the reduction by ITF3056. At 25, 50, and 100 nM, Givinostat reduced IL-1β secretion more than 70%. Givinostat (ITF-2357) suppresses the production of IL-6 in PBMCs stimulated with TLR agonists as well as the combination of IL-12 plus IL-18. IL-6 secretion decreases to 50% at 50 nM Givinostat, but at 100 and 200 nM, there is no reduction[1]. As shown by the CCK-8 assay, Givinostat (ITF-2357) inhibits JS-1 cell proliferation in a concentration-dependent manner. Treatment with Givinostat ≥500 nM is associated with significant inhibition of JS-1 cell proliferation (P<0.01). Also, the cell inhibition rate significantly differs between the group cotreated with Givinostat ≥250 nM plus LPS and the group without LPS treatment (same Givinostat concentration) (P<0.05)[2]. Givinostat (ITF2357) at 10 mg kg is used as a positive control and, as expected, reduced serum TNFα by 60%. Strikingly, pretreatment of ITF3056 starting at 0.1 mg kg significantly reduces the circulating TNFα by nearly 90%. To achieve a significant increase in serum IL-1β production, a higher dose of LPS is injected (10 mg kg), and blood is collected after 4 h. Similarly, when pretreated with lower doses of Givinostat (ITF-2357) (1 or 5 mg kg), there is a 22% reduction for 1 mg kg and 40% for 5 mg kg[1]. [1]. Li S, et al. Specific inhibition of histone deacetylase 8 reduces gene expression and production of proinflammatory cytokines in vitro and in vivo. J Biol Chem. 2015 Jan 23;290(4):2368-78. [2]. Wang YG, et al. Givinostat inhibition of hepatic stellate cell proliferation and protein acetylation. World J Gastroenterol. 2015 Jul 21;21(27):8326-39. [3]. Leoni F, et al. The histone deacetylase inhibitor ITF2357 reduces production of pro-inflammatory cytokines in vitro and systemic inflammation in vivo. Mol Med. 2005 Jan-Dec;11(1-12):1-15.

NF(N-Me)GA(N-Me)IL是一种改性的生物活性肽，对应于人胰岛淀粉样蛋白多肽hIAPP中的22至27氨基酸片段（NFGAIL），其G24和I26的酰胺键经N-甲基化处理。引入N-甲基基团使得原本促进淀粉样蛋白形成及具细胞毒性的序列变为不促进淀粉样蛋白形成和无细胞毒性。此肽可高亲和力结合至全长hIAPP，并有效抑制其纤维化过程。

Ac2-26 ammonium是一种 Annexin-A1 （AnxA1） N 末端衍生肽，具有抗炎活性，通过调节 IL-22 IL-22R1 STAT3 信号传导和 eNOS 通路减轻小鼠肝缺血再灌注损伤。

IL-6-IN-1 (Compound 22) 抑制 IL-6 的释放，IC50 为 1.065 μM，在 LPS 诱发的小鼠急性肺损伤模型中显示抗炎活性。

Vunakizumab 是一种靶向 IL-17A 的人源化 IgGκ 单克隆抗体，常与白细胞介素 22 链接形成 Vunakizumab-IL22 来研究流感病毒引起的肺免疫损伤。Vunakizumab 可用于研究银屑病关节炎，通过与IL-17A结合发挥作用。

Fezakinumab 是一种有效的白细胞介素 22 (IL-22) 单克隆抗体。Fezakinumab 可用于研究银屑病、类风湿性关节炎和特应性皮炎等免疫系统疾病和炎症相关疾病。

Eflepedocokin alfa 是一种具有潜在细胞保护活性的重组融合蛋白。Eflepedocokin alfa 由人的IL-22与人的IgG2-Fc 结构域融合组成。Eflepedocokin alfa 可激活IL-22 IL-22R 介导的信号转导通路以及STAT3。Eflepedocokin alfa 在免疫反应和细菌感染、增强肠道屏障功能、肠道免疫和组织修复方面发挥作用。

Efmarodocokin alfa为人IL-22与IgG4可结晶片段的融合蛋白，具有激活IL-22信号的功能。该化学物质主要用于重症COVID-19肺炎的研究。

RORγ-IN-2 (Compound 22) 是一种有效的 RORγ 抑制剂，其对 hRORγ 的 Ki 值为 16.6 nM。RORγ-IN-2 可应用于研究 IL-17 依赖的自身免疫性疾病。