signal-regulating

ASK1-IN-2 是一种口服有活性的凋亡信号调节激酶 1 抑制剂(IC50:32.8 nM)。它可用于研究溃疡性结肠炎。

TC ASK 10 是选择性的，口服有效的细胞凋亡信号调节激酶 1 抑制剂，IC50为 14 nM。它对其他代表性激酶的抑制活性低于 50％，除 ASK2之外 (IC50为 0.51 μM)。

GTP tritris 在细胞生理和化学过程中扮演多种关键角色，尤其在肌细胞分化及miRNA-肌肉调节因子的调控中起到增强作用。此外，它促进富含鸟苷及其衍生物的外泌体释放，并作为 RNA 合成的活化前体。在线粒体功能方面，GTP 通过协助蛋白质进入基质来启动肽合成，不仅助力甲酰甲硫氨酰-tRNA 与核糖体的结合，还推动多肽链的延长。它也作为磷酸盐及焦磷酸盐的载体，激活G蛋白信号转导路径，调节细胞的增殖与分化。GTP 的水解过程，特别是小 GTPases（如Ras与 Rho）的作用对于细胞的增殖和凋亡是必需的。同样，小 GTPase Rab 也是囊泡对接、融合与形成不可或缺的因素。GTP 不仅限于信号转导，还是 DNA 和 RNA 酶生物合成中的一个能量丰富的前体。

ASK1-IN-8 (Compound 35) 是一种口服活性的凋亡信号调节激酶 1 (ASK1) 抑制剂，其IC50值为1.8 nM。在小鼠肝损伤模型中，使用Acetaminophen诱导的实验显示，ASK1-IN-8 能显著降低血浆丙氨酸转氨酶 (ALT) 水平，从而发挥肝脏保护作用。该化合物适用于肝脏疾病相关领域的研究。

dASK1是一种选择性CRBN基于的凋亡信号调节激酶1 (ASK1) 的PROTAC靶向降解剂。它能够形成ASK1稳定的三元复合物，通过泛素-蛋白酶体途径快速并持久地降解ASK1，展现出强大的降解能力。dASK1可用于肝炎研究。

PtdIns-(3)-P1 (1,2-dipalmitoyl) (Compound 7) ammonium 是一种磷脂酰肌醇 3-磷酸衍生物。其能够与人类 EEA1 的 FYVE 结构域相结合，并在细胞信号转导和膜运输中发挥第二信使的作用。此外，磷脂酰肌醇 3-磷酸可通过调节中性粒细胞氧化酶复合物来刺激ROS的形成。

NQDI-1 (NQDI 1) 是一种凋亡信号调节激酶 1 抑制剂，Ki 为 500 nM，IC50为 3 μM。

Selonsertib (GS-4997) 是一种选择性的，具有生物口服可利用的凋亡信号调节激酶1 抑制剂，pIC50为 8.3。它具有潜在的抗炎、抗肿瘤和抗纤维化活性。

Quorum sensing is a regulatory process used by bacteria for controlling gene expression in response to increasing cell density.[1] This regulatory process manifests itself with a variety of phenotypes including biofilm formation and virulence factor production.[2] Coordinated gene expression is achieved by the production, release, and detection of small diffusible signal molecules called autoinducers. The N-acylated homoserine lactones (AHLs) comprise one such class of autoinducers, each of which generally consists of a fatty acid coupled with homoserine lactone (HSL). AHLs vary in acyl group length (C4-C18), in the substitution of C3 (hydrogen, hydroxyl, or oxo group) and in the presence or absence of one or more carbon-carbon double bonds in the fatty acid chain. These differences confer signal specificity through the affinity of transcriptional regulators of the LuxR family.[3] C16:1-Δ9-(L)-HSL is a long-chain AHL that functions as a quorum sensing signaling molecule in strains of S. meliloti.[4],[5],[6],[7] Regulating bacterial quorum sensing signaling can be used to inhibit pathogenesis and thus, represents a new approach to antimicrobial therapy in the treatment of infectious diseases.[8] Reference：[1]. González, J.E., and Keshavan, N.D. Messing with bacterial quorum sensing. Microbiol. Mol. Biol. Rev. 70(4), 859-875 (2006).[2]. Gould, T.A., Herman, J., Krank, J., et al. Specificity of acyl-homoserine lactone syntheses examined by mass spectrometry. J. Bacteriol. 188(2), 773-783 (2006).[3]. Penalver, C.G.N., Morin, D., Cantet, F., et al. Methylobacterium extorquens AM1 produces a novel type of acyl-homoserine lactone with a double unsaturated side chain under methylotrophic growth conditions. FEBS Lett. 580(2), 561-567 (2006).[4]. Teplitski, M., Eberhard, A., Gronquist, M.R., et al. Chemical identification of N-acyl homoserine lactone quorum-sensing signals produced by Sinorhizobium meliloti strains in defined medium. Archives of Microbiology 180, 494-497 (2003).[5]. Gao, M., Chen, H., Eberhard, A., et al. sinI- and expR-dependent quorum sensing in Sinorhizobium meliloti. Journal of Bacteriology 187(23), 7931-7944 (2005).[6]. Marketon, M.M., Glenn, S.A., Eberhard, A., et al. Quorum sensing controls exopolysaccharide production in Sinorhizobium meliloti. Journal of Bacteriology 185(1), 325-331 (2003).[7]. Marketon, M., Gronquist, M.R., Eberhard, A., et al. Characterization of the Sinorhizobium meliloti sinR/sinI locus and the production of novel N-Acyl homoserine lactones. Journal of Bacteriology 184(20), 5686-5695 (2002).[8]. Cegelski, L., Marshall, G.R., Eldridge, G.R., et al. The biology and future prospects of antivirulence therapies. Nat. Rev. Microbiol. 6(1), 17-27 (2008).

Quorum sensing is a regulatory process used by bacteria for controlling gene expression in response to increasing cell density. This regulatory process manifests itself with a variety of phenotypes including biofilm formation and virulence factor production. Coordinated gene expression is achieved by the production, release, and detection of small diffusible signal molecules called autoinducers. The N-acylated homoserine lactones (AHLs) comprise one such class of autoinducers, each of which generally consists of a fatty acid coupled with homoserine lactone (HSL). AHLs vary in acyl group length (C4-C18), in the substitution of C3 (hydrogen, hydroxyl, or oxo group) and in the presence or absence of one or more carbon-carbon double bonds in the fatty acid chain. These differences confer signal specificity through the affinity of transcriptional regulators of the LuxR family. C18:1-δ9 cis-(L)-HSL is a long-chain AHL that may have antimicrobial activity and thus, might be used to inhibit pathogenesis by regulating bacerial quorum sensing signaling.

Quorum sensing is a regulatory process used by bacteria for controlling gene expression in response to increasing cell density. This regulatory process manifests itself with a variety of phenotypes including biofilm formation and virulence factor production. Coordinated gene expression is achieved by the production, release, and detection of small diffusible signal molecules called autoinducers. The N-acylated homoserine lactones (AHLs) comprise one such class of autoinducers, each of which generally consists of a fatty acid coupled with homoserine lactone (HSL). AHLs vary in acyl group length (C4-C18), in the substitution of C3 (hydrogen, hydroxyl, or oxo group) and in the presence or absence of one or more carbon-carbon double bonds in the fatty acid chain. These differences confer signal specificity through the affinity of transcriptional regulators of the LuxR family. C14:1-δ9-cis-(L)-HSL is a long-chain AHL that functions as a signaling molecule in the quorum sensing of A. vitis. Regulating bacterial quorum sensing signaling can be used to inhibit pathogenesis and thus, represents a new approach to antimicrobial therpy in the treatment of infectious diseases.

Quorum sensing is a regulatory system used by bacteria for controlling gene expression in response to increasing cell density. This regulatory process manifests itself with a variety of phenotypes including biofilm formation and virulence factor production. Coordinated gene expression is achieved by the production, release, and detection of small diffusible signal molecules called autoinducers. The N-acylated homoserine lactones (AHLs) comprise one such class of autoinducers, each of which generally consists of a fatty acid coupled with homoserine lactone (HSL). Regulation of bacterial quorum sensing signaling systems to inhibit pathogenesis represents a new approach to antimicrobial therapy in the treatment of infectious diseases. AHLs vary in acyl group length (C4-C18), in the substitution of C3 (hydrogen, hydroxyl, or oxo group), and in the presence or absence of one or more carbon-carbon double bonds in the fatty acid chain. These differences confer signal specificity through the affinity of transcriptional regulators of the LuxR family. C11-HSL possesses a rare odd-numbered acyl carbon chain and may be a minor quorum-sensing signaling molecule in P. aeruginosa strains.

GS-444217 是一种可口服的选择性 ATP 竞争性凋亡信号调节激酶 1 抑制剂，IC50为 2.87 nM。

TRK-IN-16 (WO2012034091A1, compound X-21) is a highly effective TRK inhibitor, targeting protein kinases that are integral to regulating cell growth, differentiation, and various cellular signal transduction processes. This compound shows great potential for research in TRK-related diseases [1].

BPyO-34 is a novel apoptosis signal-regulating kinase 1 (ASK1) inhibitor with IC50 of 0.52μM in vitro in kinase assay.

Praeruptorin C 是白花前胡中的一种主要成分，是钙拮抗剂，pD2′值为 5.7。

Selonsertib, also known as GS-4997, is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. GS-4997 targets and binds to the catalytic kinase domain of ASK1 in an ATP-competitive manner, thereby preventing its phosphorylation and activation. GS-4997 prevents the production of inflammatory cytokines, down-regulates the expression of genes involved in fibrosis, suppresses excessive apoptosis and inhibits cellular proliferation.

cis-11-Methyl-2-dodecenoic acid 是群体感应 (QS) 信号分子，在微生物及真菌的细胞外通讯系统中扮演扩散信号因子(DSF)的角色。它参与调控多种细菌病原体的毒性及生物膜的生成。

JT21-25 (compound 9h) 作为一种高效的选择性凋亡信号调节激酶 1 (ASK1) 抑制剂，其 IC50 值为 5.1 nM。

ASK1-IN-6 (Compound 32) 是一种针对凋亡信号调节激酶 1 (ASK1) 的选择性抑制剂，具有 25 nM 的半抑制浓度 (IC50)。此化合物表现出良好的血脑屏障渗透性（大鼠动脉/静脉清除率为 1.6/56 L/h/kg，脑间隙非离子型药物分配系数 (Kp,uu) 为 0.46）。在阿尔茨海默症的 Tg4510 小鼠模型中，ASK1-IN-6 显示了其抗炎效果并有助于疾病的改善。

ASK1-IN-1 是一种凋亡信号调节激酶 1（SK1） 抑制剂，具有良好的效价 (细胞IC50=138 nM; BiochemicalIC50=21 nM)。ASK1-IN-1具有中枢神经系统渗透性。

1,2-Dioleoyl-sn-glycero-3-phospho-(1'-myo-inositol-5'-phosphate) ammonium是一种膜结合的信号分子，能调节细胞内的膜运输和信号转导。它可用于脂质体制备，以提高化合物的传递效率。此外，1,2-Dioleoyl-sn-glycero-3-phospho-(1'-myo-inositol-5'-phosphate) ammonium作为肌动蛋白细胞骨架的协调者，参与细胞形态和运动的调控。

1,2-Dioctanoyl-sn-glycero-3-phospho-(1'-myo-inositol-3',4',5'-trisphosphate) ammonium是一种重要的膜结合信号分子，能调控细胞的生长、代谢、增殖和存活。它在细胞生理过程中参与多条信号传导途径，对细胞内信号传递有显著影响。

Adenosine monophosphate-15N5,d12 (AMP-15N5,d12) dilithium 是一种氘代和15N标记的Adenosine monophosphate。它作为腺苷A1受体 (adenosine A1 receptor) 的激动剂，对HSV-1和HSV-2显示出显著的抗病毒活性。此外，Adenosine monophosphate 是调节能量稳态和信号转导的关键细胞代谢物。