il 18

hydrocotarnine 是 Cbl 的抑制剂。

Remibrutinib 是有效的、口服具有活力的 bruton tyrosine kinase 抑制剂 (IC50:1 nM)，在血液中抑制 BTK 活性的 IC50的值为 0.23 μM。它具有研究慢性荨麻疹的潜力。

JNJ-54175446 (JNJ-5446) 是一种具有中枢神经系统渗透性和选择性的 P2X7 受体拮抗剂，可减弱小胶质细胞 IL-1β IL-18 的释放，可用于研究抑郁症。

Lyn peptide inhibitor acetate(222018-18-0 free base) 是一种有效的细胞渗透性 Lyn 偶联 IL-5 受体信号通路抑制剂，同时保持其他信号完整。它阻断 Lyn 活化并抑制 Lyn 酪氨酸激酶与 IL-3 GM-CSF IL-5 受体的 βc 亚基的结合。它可用于哮喘、过敏和其他嗜酸性粒细胞疾病的研究。

HEI3090作为一种P2X7R激活剂，能够通过促进树突状细胞表达P2X7R来产生IL-18，从而激发肿瘤内的自然杀伤细胞和CD4T细胞释放IFN-γ，引导持续的抗肿瘤反应。该化合物还可以用来增强αPD-1治疗在非小细胞肺癌 (NSCLC) 中的效果。

Butyrolactone Ia 是一种NO生成的抑制剂，IC50为18 μM。它可抑制LPS诱导的iNOS和炎症细胞因子IL-1β的mRNA表达。在HeLa细胞中，Butyrolactone Ia 调节自噬 (autophagy)，并展现出免疫抑制活性。

Ac-YVAD-CMK (Ac-Tyr-Val-Ala-Asp-CMK) 是一种选择性的、不可逆的Caspase-1抑制剂，并能抑制焦亡作用、IL-1β和IL-18。Ac-YVAD-CMK 显示出神经保护和抗炎的能力。

Nrf2 activator 18 (Compound 11a) 是一种口服有效的Keap1 Nrf2 HO-1信号通路激活剂，能够促进Nrf2的核转移并增强抗氧化功能。Nrf2 activator 18 能抑制IL-6的释放，IC50为4.816 μM。在小鼠PM2.5引起的肺损伤模型中，该化合物表现出抗炎活性。

NSC80734 是一种 IL-18 抑制剂，它能阻止 hIL-18 与节肢动物病毒 IL-18BP 的结合，并抑制 IL-18 诱导的 IFN-γ 产生。

Mizoribine prodrug-1 (compound 18) 为一种酯基前体化合物,具备口服活性,并可抑制IL-2的产生.

PDE4-IN-18 (compound 1l) 作为PDE4抑制剂 (IC50=1.55 μM),展现了显著的抗炎效果.该化合物通过减少免疫细胞的过度浸润和肠膜形成,以及显著降低滑膜组织内如TNF-α和IL-6等促炎细胞因子的mRNA水平,有效抑制炎症.PDE4-IN-18 主要用于类风湿性关节炎和银屑病的相关研究.

(±)17(18)-EpETE-Ethanolamide, an ω-3 endocannabinoid epoxide, originates from eicosapentaenoic ethanolamide (EPEA) through cytochrome P450 (CYP) epoxygenases action and is decomposed by soluble epoxide hydrolase (sEH) and fatty acid amide hydrolase (FA, AH). Its endogenous synthesis occurs in LPS-stimulated and EPEA-supplemented BV-2 microglia cells, a process inhibited by the CYP inhibitor ketoconazole. This compound mitigates IL-6 and nitrite levels while enhancing IL-10 production following LPS exposure in BV-2 microglia. At a dose of 50 µM, it prevents platelet aggregation caused by arachidonic acid but not that triggered by ADP, collagen, or ristocetin. Additionally, it facilitates the dilation of constricted bovine coronary arteries (ED50= 1.1 µM) and blocks VEGF-driven tubulogenesis in human microvascular endothelial cells (HMVECs).

QS-21, an immunostimulatory saponin, is a powerful vaccine adjuvant that stimulates both Th2 humoral and Th1 cell-mediated immune responses by interacting with antigen presenting cells (APCs) and T cells. Additionally, QS-21 activates the NLRP3 inflammasome, leading to the release of cytokines IL-1β and IL-18, which are dependent on caspase-1.

JT002为口服活性的NLRP3炎性体抑制剂，能够抑制NLRP3依赖性促炎细胞因子（如IL-1β、IL-1α、IL-18）的生成以及细胞焦亡（pyroptosis），阻断NLRP3炎性体复合物的形成。此外，JT002可有效减少小鼠气道高反应性，并降低气道中中性粒细胞的聚集。

Camoteskimab (AVTX-007)为全人源、高亲和力抗IL-18单克隆抗体，展现于自身炎症性疾病研究潜力，包括成人斯蒂尔病(AOSD)。

C6 L-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides., C6 L-threo Ceramide is cytotoxic to U937 cells in vitro (IC50 = 18 μM). It is metabolically inactive and, unlike C6 L-erythro ceramide , C6 L-threo ceramide cannot be converted to C6 glucosylceramide by ceramide glucosyltransferase. C6 L-threo Ceramide enhances IL-4 production induced by phorbol 12-myristate 13-acetate in EL4 T cells when used at a concentration of 10 μM.

Pralnacasan inhibits proinflammatory cytokines IL-18, IL-1β , and IFN-γ. Pralnacasan is an effective, non-peptide, and orally active interleukin-1β converting enzyme inhibitor (Ki: 1.4 nM). Pralnacasan has the potential for osteoarthritis and rheumatoid a

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.

C6 D-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides., C6 D-threo Ceramide is cytotoxic to U937 cells in vitro (IC50 = 18 μM). It is metabolically inactive and, unlike C6 L-erythro ceramide , C6 D-threo ceramide cannot be converted to C6 glucosylceramide by ceramide glucosyltransferase. C6 D-threo Ceramide promotes survival of isolated rat spinal neurons when used at concentrations up to 2.5 μM but induces cell death at concentrations greater than 5 μM. It enhances IL-4 production induced by phorbol 12-myristate 13-acetate in EL4 T cells when used at a concentration of 10 μM.

IMMH001, also known as SYL930, is an orally active compound that exhibits potent selectivity as an agonist for the S1P1 receptor, which is the sphingosine-1-phosphate receptor 1. This compound effectively reduces the levels of various chemokines and proinflammatory cytokines, such as IL-1β, IL-5, IL-18, IP10, CCL3, and CCL5. IMMH001 finds utility in research focused on rheumatoid arthritis (RA) [1] [2].

Soyacerebroside II exhibits ionophoretic activity for Ca2+ ion. Soyacerebrosides I and II have modulating the cellular immune response effects, they show obvious inhibitory activity on IL-18 secretion in human peripheral blood mononuclear cells (PBMC).

C18 Phytoceramide (t18:0 18:0) (Cer(t18:0 18:0)) is a bioactive sphingolipid found in S. cerevisiae, wheat grains, and the stratum corneum layer of mammalian epidermis. Cer(t18:0 18:0) is composed of a phytosphingosine backbone amine-linked to a C18 fatty acid chain. Cer(t18:0 18:0) has a role in regulation of apoptosis, cell differentiation, proliferation of smooth muscle cells, and inhibition of the mitochondrial respiratory chain. It also inhibits expression of the allergic cytokines IL-4, TNF-α, and transcription factors c-Jun and NF-κB in histone-stimulated murine skin tissue. Formulations containing cer(t18:0 18:0) have been used used in cosmetics as a skin protectants as they reduce water loss to prevent epidermal dehydration and irritation.

TLR9-IN-18 is a potent and selective TLR9 antagonist. TLR9-IN-18 suppresses the production of the proinflammatory cytokine IL-6 in a CpG-induced mouse model.

P2X7 receptor antagonist-4（Compound 14a）是一种选择性P2X7R拮抗剂，其对人类和小鼠P2X7R的IC50值分别为64.7 nM和10.1 nM。该化合物能有效抑制NLRP3炎性体的激活，并在脓毒症模型小鼠中减少肾损伤，降低caspase-1、gasdermin D、IL-1β和IL-18的表达。