mcp 2

Anti-Mouse Rat Human CCL2 MCP-1 Antibody (2H5) 是一种来自美国仓鼠的 IgG, κ 抗体抑制剂，针对小鼠、大鼠和人体的 CCL2 MCP-1。

Bindarit 是单核细胞趋化蛋白MCP-1 CCL2，MCP-3 CCL7和MCP-2 CCL8的选择性抑制剂，具有抗炎作用。Bindarit 对 p65 和 p65 p50 诱导的 MCP-1 启动子激活具有特异性抑制作用，对其它测试的活化启动子没有影响。

Licochalcone B 是从Glycyrrhiza inflate 根中提取的。它能够抑制淀粉样蛋白 β 自聚集作用 (IC50=2.16 μM) ，分解预先形成的 Aβ42原纤维，并通过螯合金属离子抑制金属诱导的 Aβ42聚集。

Berberrubine chloride (9-Berberoline Chloride) 是一种黄连素的有效代谢物，能够改善动物模型中溃疡性结肠炎的症状。

Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8 9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9, activates the proprotein form of caspase-1 independent of the inflammasome adaptor ASC[2]. Talabostat competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26 DPP-IV, and there is a high-affinity interaction with the catalytic site due to the formation of a complex between Ser630 624 and the boron of talabostat[3]. Talabostat can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system. In WEHI 164 fibrosarcoma and EL4 and A20 2J lymphoma models, PT-100 causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostat treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells[3]. Talabostat treated mice show significant less fibrosis and FAP expression is reduced. Upon PT100 treatment, significant differences in the MMP-12, MIP-1α, and MCP-3 mRNA expression levels in the lungs are also observed. Treatment with PT100 in this murine model of pulmonary fibrosis has an anti-fibro-proliferative effect and increases macrophage activation[4]. [1]. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. [2]. Okondo MC, et al. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat Chem Biol. 2017 Jan;13(1):46-53. [3]. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. [4]. Egger C, et al. Effects of the fibroblast activation protein inhibitor, PT100, in a murine model of pulmonary fibrosis. Eur J Pharmacol. 2017 Aug 15;809:64-72.

GPR183 antagonist-2 (化合物 32) 是一种选择性GPR183拮抗剂，水溶性好，药代动力学特性优异。该化合物能剂量依赖性地减轻胶原诱导的关节炎(CIA)小鼠模型中的爪子和关节肿胀，并显著抑制促炎细胞因子(MCP-1，MMPs 和 VEGF)的基因表达。GPR183 antagonist-2 适用于自身免疫性疾病的研究。

Lupeol acetate（乙酸羽扇醇酯）是Lupeol（羽扇醇酯）的衍生物，具有抗癌，抗炎，抗糖尿病，抗蛇毒，抗生育作用，具有口服活性。能够下调炎症细胞因子（TNF-α、IL-1β、MCP-1、COX-2、VEGF、granzyme B）从而抑制类风湿关节炎。对Hep-3B和A549细胞有细胞毒性。

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。

22(S)-hydroxy Cholesterol is a synthetic oxysterol and a modulator of the liver X receptor (LXR). [1] t prevents monocyte chemoattractant protein 1 (MCP-1) expression induced by the LXR agonist GW 3965 in primary hepatocytes and downregulates mRNA expression of the LXR target genes CD36, ACSL1, and SCD-1 in human myotubes. It decreases triacylglycerol and diacylglycerol synthesis from labeled palmitate and acetate, respectively, in human myoblasts by 50% when used at a concentration of 10 uM. 22(S)-hydroxy Cholesterol also reduces fatty acid synthase (FAS) reporter activity through an LXR response element in the promoter region in COS-1 cells transfected with RXRα and LXRα and decreases the expression of MCP-1 and CCR2 in a mouse model of chronic ethanol consumption.[1] [2] Dietary supplementation of 22(S)-hydroxy cholesterol (30 mg kg per day) leads to less body weight gain and lower liver triacylglycerol levels in rats when fed either a regular chow or high-fat diet as well as prevents an increase in plasma triacylglycerol levels resulting from a high-fat diet.[3]

CCR2 antagonist 4 (Teijin compound 1) 是高效的、特异性的CCR2拮抗剂，对 CCR2b 的IC50为 180 nM，抑制 MCP-1 诱导的趋化作用的 IC50为 24 nM。

GSK-3β inhibitor 17 (16, 32, 64 µM) 在 HK-2 细胞急性肾损伤 (AKI) 模型中，对剂量敏感地抑制由顺铂引起的 p-p65 和 KIM-1 蛋白表达。在同样的模型中，使用 32 µM 浓度的 GSK-3β inhibitor 17 可以减少顺铂诱导的 TNF-α、IL-1β、IL-6 和 MCP-1 mRNA 的表达水平。

SB297006 是一种CCR3拮抗剂，IC50为39 nM。它能够显著抑制 CCL11 处理的神经祖细胞的增殖和神经球形成。