tnfr1

Infliximab 属于单克隆抗体，是一种抑制 TNF-α 的人鼠嵌合单克隆抗体，可阻止 TNF-α与 TNFR1 和 TNFR2 的相互作用。Infliximab 可以用于治疗克罗恩病和类风湿性关节炎。

Anti-TNFR1 CD120a TNFRSF1A Antibody (9Z795) 是一种靶向人 TNFR1 CD120a TNFRSF1A 的单克隆抗体，是一种 Rabbit IgG 抗体。

Anti-TNFR2 CD120b TNFR1B Antibody (6I44) 是一种靶向小鼠 TNFR2 CD120b TNFR1B 的单克隆抗体，是一种 Rabbit IgG 抗体。

JNJ525 is an inhibitor of TNFα. JNJ525 inhibits protein function via an aggregation-based mechanism. JNJ525 prevents the formation of TNFα complexes with TNFR1 and TNFR2, the apparent IC50 values for the inhibition of complex formation are 1.2 ± 0.2 μM an

TNF-α-IN-2是一种有效和具有口服活性的TNFα抑制剂，通过在结合时扭曲TNFα三聚体，使其与TNFR1结合时信号传导异常，可用于研究类风湿关节炎。

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.

TBK1 IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1 IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR[1]. TBK1 IKKε-IN-4 (Compound II; 96 hours; A549 andHCC44 cells) treatmentdisplays selective toxicity in TBK1-dependent cancer cell lines (IC50 of ~ 4.2 μM for H441 cells and IC50 of ~0.4 μM for A549 cells)[1].TBK1 IKKε-IN-4 (Compound II; 0-2 μM; 30 minutes; HCC44 cells) treatment inhibits the AKT activity[1].TBK1 IKKε-IN-4 (Compound II) inhibits LPS-induced expression of IFNβ (IC50 =62 nM), and the IFNβ target genes IP10 (IC50 =78 nM) and Mx1 (IC50=20 nM). TBK1 IKKε-IN-4 effectively blocksTLR3-dependent IRF3 nuclear translocation in cells with an IC50 under 100 nM, but does not impair TNFR1-dependent p65 NFκB nuclear translocation with doses as high as 20 μM[1]. [1]. Ou YH, et al. TBK1 directly engages Akt PKB survival signaling to support oncogenic transformation. Mol Cell. 2011 Feb 18;41(4):458-70.

GSK717 是 NOD2(核苷酸结合寡聚结构域 2) 的选择性抑制剂。它抑制壁酰二肽 (MDP) 诱导的 NOD2 介导的信号转导，抑制 MDP 刺激的 HEK293 hNOD2 细胞分泌 IL-8 (IC50为 400 nM)。

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。

UCB-6876 is a novel inhibitor of TNF signalling by stabilising an asymmetric form of the trimer, displaying a concentration-dependent response curve and selectivity over the TNFR1 extracellular domain and control proteins.

UCB-6786 is a novel inhibitor of TNF signalling by stabilising an asymmetric form of the trimer, displaying a concentration-dependent response curve and selectivity over the TNFR1 extracellular domain and control proteins.

Atrosab 是一种人源化靶向 TNFR1的 IgG1 类抗体，抑制 TNF 介导的细胞凋亡，可用于研究炎症和神经退行性疾病。

Atrosimab (ATM-001) 是 Fv-Fc1κ 融合蛋白，能够与人TNFR1强效结合，EC50值为 0.37 nM， 并且有效抑制 TNF 诱导的 TNFR1 激活。Atrosimab 被认为在慢性炎症性疾病的研究中具有潜力。