autoimmune disease

HS-243 是 IRAK-4 和 IRAK-1 的抑制剂，IC50 分别为 20 和 24 nM。 HS-243 显示出抗炎和抗癌活性。

ML604440 是一种特异性的、有效的、细胞可渗透的蛋白酶体 β1i (LMP2) 亚基抑制剂，能够破坏 MHC I 类细胞表面表达，IL-6 分泌以及 naïve T helper 向 17 T helper 细胞的分化。它可以改善实验性结肠炎和 EAE 疾病。

STM2457 是一种 RNA 甲基转移酶 METTL3 的抑制剂 (IC50=16.9 nM)，具有选择性和口服活性。STM2457 可用于急性髓系白血病 (AML) 的研究。

NIBR189是 EBI2（GPR183）小分子拮抗剂(IC50:11 nM)。

ML-178 是一种二氯苯，是鞘氨醇-1-磷酸受体4（S1PR4）的强效选择性激动剂，EC50 为 46 nM，在25 μM 的浓度下对其他 S1P 受体没有影响。

Ciamexon (Ciamexone) 是一种新型的免疫调节剂，在自身免疫性疾病的实验模型中具有良好的效果，几乎没有显示出细胞毒性。Ciamexon 可用于研究内分泌眼病和糖尿病，在短时间给药后眼科疾病得到轻微改善。

MCC950 (CP-456773) 是NLRP3的选择性抑制剂，能够作用于BMDMs(IC50:7.5 nM) 和 HMDMs(IC50:8.1 nM)。

Tapinarof (Benvitimod) 是一种从发光杆菌中提取的天然产物，可消除炎症。它是芳烃受体 (AhR) 激动剂，EC50为 13 nM。

Cletoquine 是 Hydroxychloroquine 的主要活性代谢物。 Cletoquine 具有对抗基孔肯雅病毒 (CHIKV) 的能力。 Cletoquine 具有抗疟作用，并具有治疗自身免疫性疾病的潜力。

Cletoquine oxalate (Desethylhydroxychloroquine oxalate) is a major active metabolite of Hydroxychloroquine. Cletoquine has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune disea

HPN-01 (IKK inhibitor XII) 是一种选择性的 IKK 抑制剂，抑制 IKK-α、IKK-β 和 IKK-ε。HPN-01 可在自身免疫性脑脊髓炎模型中降低疾病的严重程度，减轻免疫失衡，延长小鼠的寿命，可用于研究免疫类疾病。

Nrf2 activator-12 (compound 10v) 在实验性自身免疫性脑脊髓炎小鼠模型中有效启动Nrf2 (EC50=83.5 nM)，显示出优异的药物属性，能逆转疾病的进展并减轻脱髓鞘现象。

ERAP1-IN-3 (compound 13) 是一种强效的内质网氨基肽酶 1 ERAP1 抑制剂，其 pIC50 值为 8.6。ERAP1-IN-3 有望用于癌症免疫和自身免疫性疾病的研究。

ARN-6039 is an orally available inverse agonist of RORγ for Autoimmune Neuroinflammatory Demyelinating Disease. The activity of ARN-6039 against RORγ was demonstrated in a RORγ-activated IL-17A Prom LUCPorter assay in HEK 293 cells (360 nM) and in IL-17 r

L-Mevalonic acid ((S)-Mevalonic acid) 是胆固醇的远源前体，是甲羟戊酸途径的代谢产物，可用于研究自身免疫性疾病、动脉粥样硬化和阿尔茨海默病。

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.

KZR-616, a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. KZR-616 has the potential for the research of multiple autoimmune diseases[1][2]. KZR-616 also inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM). KZR-616 maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells. KZR-616 (250 nM) shows a comparable cytokine inhibition profile peripheral blood mononuclear cells (PBMC)[1].KZR-616 is an immunoproteasome-selective inhibitor identified based on the optimization of ONX-0914 and PR-924 [3]. KZR-616 (5 mg/kg; i.v.; dosing was repeated on days 6, 8, 11, and 13) shows efficacy in the anticollagen antibody induced arthritis (CAIA) model[1]. [1]. Johnson HWB, et al. Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpholinoacetamido)propanamido)propenamide). J Med Chem. 2018 Dec 27;61(24):11127-11143. [2]. Muchamuel T, et al. FRI0296 Kzr-616, a selective inhibitor of the immunoproteasome, blocks the disease progression in multiple models of systemic lupus erythematosus (SLE). Annals of the Rheumatic Diseases 2018;77:685. [3]. Xi J, et al. Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases. Eur J Med Chem. 2019;182:111646.

AcylCoA:cholesterol acyltransferase (ACAT) is an intracellular cholesteryl ester synthase tied closely to the absorption of dietary cholesterol. Oleyl analide (OA) is a weak inhibitor of acylCoA:cholesterol acyltransferase (ACAT) with an IC50 of 26 μM. OA and the related glyceride dioleoyl phenylamino propane 1,2-diol have been linked to a syndrome of eosinophilia, excessive T-cell activation, and elevated interleukin-4 (IL-4), soluble IL-2R, and IL-5. The clinical consequences are an acute pulmonary inflammatory reaction followed by chronic neuropathy, myalgia, and autoimmune connective tissue disease, generally referred to as toxic oil syndrome (TOS). Aniline-denatured cooking oil is a source of OA associated with TOS.

TLR7 8-IN-1 是一种来自专利 WO2019220390（化合物 2b）的结晶 TLR7 TLR8 抑制剂，是一种用于自身免疫疾病研究的有价值的化合物。

Esculentoside A 是一种三萜皂苷，从商陆根部分离得到。它在具有抗炎活性，对环氧合酶-2 具有选择性抑制活性。它通过抑制NF-κB 和丝裂原活化蛋白激酶信号通路抑制 LPS 诱导的急性肺损伤中的炎症反应。

BMS-986143 是一种口服有效的、可逆的BTK 抑制剂，IC50为 0.26 nM，具有自身免疫性疾病的研究潜力。BMS-986143 还抑制 TEC、BLK、BMX、TXK FGR、YES1、ITK，IC50分别为 3 nM、5 nM、7 nM、10 nM、15 nM、19 nM、21 nM。

Amdizalisib is a PI3K inhibitor and used for the research of inflammatory disease, autoimmune disease or cancer.

TR-14035 (MDK-1191) 是一种具有口服活性的 α4β7 α4β1整合素双重抑制剂，对 α4β7和 α4β1作用的 IC50值分别为 7 和 87 nM，可用于炎症和自体免疫疾病的研究。

SSAO inhibitor-2 (Compound 1) 可用于动脉粥样硬化、糖尿病及其并发症、肥胖、中风、慢性肾病、视网膜病变、慢性阻塞性肺病 (COPD)、自身免疫性疾病、多发性硬化等的研究。SSAO inhibitor-2 是氨基脲敏感性胺氧化酶 (SSAO) 抑制剂，其对人 SSAO 和 MAO-A 的IC50分别为 <10 nM 和 10-100 μM。