cell-macrophage

NHWD-870 是一种有效且特异性的 BET 家族溴结构域抑制剂，仅与 BRD2、BRD3、BRD4 (IC50 = 2.7 nM) 和 BRDT 结合。 NHWD-870 具有强大的抗肿瘤功效，并通过增加肿瘤细胞凋亡和抑制肿瘤增殖来抑制癌细胞-巨噬细胞相互作用。

Dexamethasone (Hexadecadrol) 是一种糖皮质激素受体激动剂和一种 IL 受体调节剂。Dexamethasone 具有抗炎和免疫抑制活性，可诱导自噬。Dexamethasone 抑制 LPS 诱导的巨噬细胞炎症反应。

Amiprilose (SM 1213) 具有抗炎活性，抑制多种过度增殖细胞类型的增殖。Amiprilose 诱导淋巴因子诱导的巨噬细胞激活，可用于研究类风湿性关节炎和银屑病。

Bestatin (Ubenimex) 是 CD13 (Aminopeptidase N) APN 和 leukotriene A4 hydrolase 抑制剂，可用于癌症研究。

Inosine pranobex (Delimmun) 是一种免疫增强剂，它是一种广谱抗病毒剂，用于 HIV 感染。

Cimifugin (Cimitin) 是中草药Saposhnikovia divaricate 的一种生物活性成分。它能够调节紧密连接减少上皮衍生的主动关键因子，对过敏性炎症产生抑制作用。

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.

G150 是高选择性h-cGAS 抑制剂，IC50值为 10.2 nM，用于抑制 dsDNA 引发的干扰素表达。

Golotimod (SCV 07) 是一种具有抗菌活性的二肽，具有免疫调节活性，能显著提高抗结核治疗的疗效，诱导胸腺和脾脏细胞增殖，调节巨噬细胞功能，抑制 STAT3 信号传导。Golotimod 可用于研究复发性生殖器单纯疱疹病毒 2 （HSV-2）感染和口腔黏膜炎。

SJ-C1044 是一种口服泛RAF抑制剂，具备免疫调节与抗肿瘤活性。该化合物能够有效抑制BRAF（野生型）、CRAF（野生型）及BRAF(V600E)，对应的IC50值为331 nM、257 nM及187 nM。它通过阻断kras激活及MEK-ERK路径的磷酸化作用来抑制肿瘤细胞增殖。此外，SJ-C1044 对VEGFR2、TIE2、CSF1R也显示出抑制效果，其IC50值分别是100 nM、23 nM和235 nM。通过抑制血管生成和调节巨噬细胞功能，SJ-C1044能改善肿瘤免疫微环境，适用于结直肠癌的研究。

PLD-IN-1（Compound 3r），作为一种有效的磷脂酶D（phospholipase D）抑制剂，其IC50为1.97 μM，能够通过调节肺癌细胞的免疫逃避机制来抑制肿瘤。该化合物能降低CD24、CD47和PD-L1的表达，并增强钙网络蛋白的表达，从而促进巨噬细胞吞噬癌细胞。此外，PLD-IN-1抑制多种肺癌细胞线的细胞活力，包括A549、HCC44、H460和HCC15，其IC50分别为18.44、22.31、24.85和21.45 μM。它还可以诱导A549细胞凋亡（apoptosis）并抑制细胞迁移，同时增强促炎性M1巨噬细胞水平并降低抗炎性M2巨噬细胞水平，展现出在小鼠模型中的抗肿瘤活性。

Lipid 16，一种可电离脂质，主要用于制备脂质纳米颗粒 (LNP)，进而递送mRNA及其他有效载荷。该脂质具有针对CD11bhi巨噬细胞群的强效细胞类型特异性，无需附加的靶向组分。

EP4 receptor antagonist 7 (Compound 14) 是一种针对前列腺素 E2 (PGE2) 的 EP4 受体亚型的拮抗剂，其IC50值为1.1 nM。在HEK293细胞中，它抑制PGE2诱导的β-阻滞蛋白的募集，IC50为0.9 nM。在RAW 264.7巨噬细胞中，EP4 receptor antagonist 7 能降低PGE2诱导的IL-4、Mrc1、Chil3、Cxcl1、Trem2和Arg1等mRNA的表达。在CT26小鼠结肠癌模型中，该化合物与抗PD-1抗体联合使用可抑制肿瘤生长并增加CD8+ T细胞对肿瘤的浸润。

AN0128 （CRM-0005）是一种具有抗炎活性的含硼抗菌剂，抑制 S. aureus，S. epidermidis，P. acnes，B. subtilis，通过抑制 p38 MAP 激酶信号转导途径抑制巨噬细胞系中促炎细胞因子的产生，可用于皮肤病的研究。

KGP94 是一种有效的、选择性的和竞争性的溶酶体内肽酶抑制剂。

D-Trimannuronic acid is an alginate oligomer that originates from seaweed. It can induce TNF-α secretion by mouse macrophage cell lines, making it valuable in pain and vascular dementia research [1][2][3].

Thiocarlide (isoxyl) is a thiourea derivative that was used in the 1960s to successfully treat tuberculosis (TB). It has considerable antimycobacterial activity in vitro and is effective against multi-drug resistant strains of Mycobacterium tuberculosis in the range of 1-10 µg ml. [1] [2] At concentrations of 10 µM, isoxyl inhibits the synthesis of M. bovis during six hours of exposure which is similar to isoniazid (INH) and ethionamide (ETH), two other predominant anti-tuberculosis drugs. Unlike INH and ETH, isoxyl also partially inhibits the synthesis of fatty acids. Isoxyl shows no acute toxicity against primary macrophage cell cultures as demonstrated by diminution of redox activity.[2]

Betamethasone 21-phosphate is a synthetic glucocorticoid.1It prevents increases in macrophage and eosinophil numbers in bronchoalveolar lavage fluid (BALF) and decreases in blood leukocyte numbers in a guinea pig model of parainfluenza-3 viral infection when administered at a dose of 8 mg/kg but does not prevent airway hyperresponsiveness after infection.2Betamethasone 21-phosphate inhibits cell infiltration into the aqueous humor in a rat model of endotoxin-induced uveitis when administered topically or subcutaneously at doses of 0.01-1% or 1 mg/kg, respectively.3It increases maximal lung pressure volume curves in fetal sheep when administered to pregnant ewes at 0.75 gestation at doses of 80 and 170 μg/kg.1Betamethasone 21-phosphate increases body weight, impairs learning and memory, increases anxiolytic behavior, and reduces hippocampal neurogenesis in CD-1 mice but reduces body weight and increases neurogenesis with no effect on anxiety in high-anxiety DBA/2 mice when administered at a dose of approximately 25 mg/kg per day in the drinking water for seven weeks.4Formulations containing betamethasone 12-phosphate and betamethasone acetate have been used in the treatment of severe allergic conditions and a variety of immune-related conditions. 1.Loehle, M., Schwab, M., Kadner, S., et al.Dose-response effects of betamethasone on maturation of the fetal sheep lungAm. J. Obstet. Gynecol.202(2)186.e181-186.e187(2010) 2.Leusink-Muis, A., Ten Broeke, R., Folkerts, G., et al.Betamethasone prevents virus-induced airway inflammation but not airway hyperresponsiveness in guinea pigsClin. Exp. Allergy29(Suppl. 2)82-85(1999) 3.Tsuji, F., Sawa, K., Kato, M., et al.The effects of betamethasone derivatives on endotoxin-induced uveitis in ratExp. Eye Res.64(1)31-36(1997) 4.Aiello, R., Crupi, R., Leo, A., et al.Long-term betamethasone 21-phosphate disodium treatment has distinct effects in CD1 and DBA/2 mice on animal behavior accompanied by opposite effects on neurogenesisBehav. Brain Res.278155-166(2015)

JC-171 is a selective NLRP3 inflammasome inhibitor, with an IC50 of 8.45 μM for inhibiting LPS ATP-induced interleukin-1β (IL-1β) release from J774A.1 macrophages[1]. JC-171 (0-100 μM) blocks NLRP3 inflammasome activation and IL-1β production in primary macrophages dose dependently[1]. Cell Viability Assay[1] Cell Line: J774A.1 murine macrophage cells JC-171 treatment delays the progression and reduces the severity of experimental autoimmune encephalomyelitis (EAE) in mouse[1]. Animal Model: Mice immunized subcutaneously with 200 μg Myelin oligodendrocyte glycoprotein (MOG) 35-55 peptide emulsified in Complete Freund's Adjuvant (CFA) on day 0 followed by injection of 200 ng of pertussis toxin. [1]. Chunqing Guo, et al. Development and Characterization of a Hydroxyl-Sulfonamide Analogue, 5-Chloro-N-[2-(4-hydroxysulfamoyl-phenyl)-ethyl]-2-methoxy-benzamide, as a Novel NLRP3 Inflammasome Inhibitor for Potential Treatment of Multiple Sclerosis. ACS Chem Neurosci. 2017 Oct 18;8(10):2194-2201.

Roquinimex (FCF89) 是一种喹啉衍生物免疫刺激剂，可增加 NK 细胞活性和巨噬细胞的细胞毒性，抑制血管生成并减少 TNF α 的分泌。

CCR4 antagonist 3-1 是一种具有较低活性的趋化因子受体 4 (CCR4) 拮抗剂，对 [125I]TARC (胸腺和活化调节趋化因子) 具有抑制作用，IC50 值为 1.7 μM。CCR4 antagonist 3-1 对放射标记的[125I]TARC和巨噬细胞来源的趋化因子(MDC) 与 CEM 细胞表面的CCR4 受体的结合有抑制作用， 并对 TARC 介导的 CEM 细胞的体外迁移有抑制作用，IC50 值为 6.4 μM。

MIF098 是一种巨噬细胞迁移抑制因子 (MIF) 拮抗剂。MIF098，抑制与 SLE 相关的肺动脉高压，抑制肺平滑肌细胞(PASMC)增殖和迁移。MIF098 可用于研究特发性肺动脉高压。

MIF-IN-6 (compound 2d) is an effective inhibitor of macrophage migration inhibitory factor (MIF), exhibiting an IC50 of 1.4 μM and a Ki value of 0.96 μM. MIF-IN-6 effectively reduces MIF-induced ERK phosphorylation and impedes A549 cell proliferation [1].

GGTI-2166 is a geranylgeranyl transferase I inhibitor. GGTI-2166 inhibit the pOC formation induced by RANKL or TNF-alpha in cultures of both mouse marrow-derived macrophage-colony-stimulating factor (M-CSF) dependent monocytes (MD cells) and the mouse monocyte cell line RAW 264.7 (RAW cells). GGTI-2166 inhibited TRAP activity induced by RANKL or TNF-alpha in both cell cultures and prevented the incorporation of [3H]all-trans geranylgeraniol into prenylated proteins in RAW cells.