effector

CK-666 是一种肌动蛋白相关蛋白 Arp2 3 复合物的细胞渗透性抑制剂。 它与 Arp2 3 复合物结合，稳定复合物的非活性状态，阻止 Arp2 和 Arp3 亚基进入活化的丝状短节距构象。

BAI1 是一种选择性凋亡因子BAX 变构抑制剂。它结合 BAX 并变构抑制其激活，具有潜力研究 BAX 依赖性细胞死亡介导的疾病。

Psora 4 (5-(4-Phenylbutoxy)psoralen) 是一种具有选择性和高效性的 Kv1.3 阻断剂，是热量限制模拟物，具有免疫抑制活性，可增强神经祖细胞的分化和成熟。

3-Hydroxykynurenamine, also known as 3-Hydroxy-L-kynurenamine or 3-HKA, is a biogenic amine produced via an alternative pathway of tryptophan metabolism. In vitro, 3-HKA has an anti-inflammatory profile by inhibiting the IFN-γ mediated STAT1 NF-κΒ pathway in both mouse and human dendritic cells (DCs) with a consequent decrease in the release of pro-inflammatory chemokines and cytokines, most notably TNF, IL-6, and IL12p70. 3-HKA has protective effects in an experimental mouse model of psoriasis by decreasing skin thickness, erythema, scaling and fissuring, reducing TNF, IL-1β, IFN-γ, and IL-17 production, and inhibiting generation of effector CD8+ T cells. Similarly, in a mouse model of nephrotoxic nephritis, besides reducing inflammatory cytokines, 3-HKA improves proteinuria and serum urea nitrogen, overall ameliorating immune-mediated glomerulonephritis and renal dysfunction.This compound is unstable in powder form and other related salt forms are recommended.

Acetylcholine iodide (Acetylcolina) 是一种在中枢和外周神经系统中常见的神经递质。

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.

RBC8是一种特异性 GTP 酶 RalA RalB 抑制剂，通过抑制 Ral 与其效应物 RALBP1 的结合，对 GTP 酶 RhoA 和 Ras 没有抑制作用。

RMC-6291 是一种可口服且具有高效性的 KRASG12C(ON) 抑制剂，具有抗癌抗肿瘤活性，通过空间阻断 RAS 效应子结合来发挥作用。RMC-6291 阻断 ERK 信号传导，促使 KRASG12C 突变 H358 细胞凋亡。

A-9758 is a RORγ ligand and a selective RORγt inverse agonist (IC50: 5 nM) and exhibits robust potency against IL-17A release. It is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 drive

AS2863619 free base enables the conversion of antigen-specific effector memory T cells into Foxp3+ regulatory T (Treg) cells. It is a potent, orally active CDK8 and CDK19 inhibitor (IC50s: 0.61 nM and 4.28 nM). STAT5 activation enhanced by AS2863619 free base inhibition of CDK8 19, which consequently activates the Foxp3 gene.

JI051 具有抗肿瘤作用，能够与癌症相关蛋白伴侣 prohibitin 2 (PHB2) 相互作用，通过抑制 Notch 下游效应基因 Hes1 转录来促使细胞周期停滞，抑制HEK293 细胞和胰腺癌细胞增殖。

PRN694 shows extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo. PRN694 is an irreversible, highly selective, and effective covalent interleukin-2-inducible T-cell kinase (ITK) and resting ly

6BrW is an analog of tryptophan effector.

L-5-BromoTryptophan (5-BrW) 是色氨酸(Trp) 效应物的类似物，可抑制血红蛋白 S 的凝胶化。

AM-001，作为Epac1的非竞争性抑制剂，能有效阻断培养细胞中Epac1下游效应子Rap1的激活，常用于心脏病相关的研究领域。

PF-07265028 是一种HPK1抑制剂，其IC50为17 nM。在进行了体内药代动力学研究后，PF-07265028在小鼠和猴子体内表现出适中的清除率、终端半衰期、分布容积及口服生物利用度。PF-07265028定位、结合并抑制Hpk1的活性，进而阻断Hpk1介导的信号传导途径，防止Hpk1介导的免疫抑制，包括阻止T细胞受体（TCR）信号的抑制、效应T细胞的抑制、破坏异常的细胞因子表达，并消除免疫抑制性肿瘤微环境（TME）。这可能激活针对肿瘤细胞的细胞毒性T淋巴细胞（CTL）介导的免疫反应。Hpk1主要在造血细胞中表达，是TCR信号和T、B细胞激活的负向调节因子。

Y-30141与广泛使用的ROCK 抑制剂Y-27632关系密切。该化合物通过竞争性结合到催化位点，抑制了ROCK-I与ROCK-II的激酶活性，其对ROCK激酶的亲和力比对其他Rho效应器激酶高出20至30倍。此外，Y-30141的抑制机制和作用谱也已进行了研究。

Acetylcholine bromide 是乙酰胆碱的溴化物盐。它是一种神经递质，存在于神经肌肉接头、自主神经节、副交感神经效应器接头、交感神经效应器接头的一个子集以及中枢神经系统的许多部位。

Lipid C2 是一种可电离阳离子脂质，广泛用于形成用于体内递送mRNA的脂质纳米颗粒 (LNP)。含有 Lipid C2 并封装mRNA报告基因的LNP在小鼠中选择性集聚于肝脏和脾脏，而不在心脏、肺或肾脏中积累。携带编码Epstein-Barr病毒 (EBV) 蛋白潜伏膜蛋白 2 (LMP-2) 的mRNA的LNP，与抗程序性细胞死亡蛋白 1 (PD-1) 抗体联用，可缩小肿瘤体积，逆转T细胞耗竭，提高CT26小鼠EBV感染结肠癌模型中脾脏中CD3+CD8+中心T细胞和CD3+CD8+效应记忆T细胞的比例，并降低表达Pd-1的CD3+T细胞的比例。

Adenanthin, a natural inhibitor of thiol-dependent antioxidant enzymes, impairs the effector functions of human natural killer cells.

RBC10 抑制 Ral 与其效应物 RALBP1 的结合，以及抑制 Ral 介导的鼠胚胎成纤维细胞的细胞扩散和人类癌细胞系的非贴壁依赖性生长。

RBC6 is an inhibitor of the binding of Ral to its effector RALBP1.

Dexbrompheniramine is an antihistamine with anticholinergic properties. It is used to treat allergic diseases such as hay fever or urticaria. It can compete with histamine for H1 receptor sites on effector cells of the gastrointestinal tract, blood vessel

L 35 is kind of a negative effector of hemoglobin.