synthase

Phenylbutazone (Butazolidine) 是是非甾体类抗炎药，前列腺素 H 合酶过氧化物酶的还原辅助因子，可诱导肌肉盲样蛋白 1 表达，有用于强直性脊柱炎的研究潜力。

FIN56 是一种铁死亡特异性诱导剂，能结合并激活角鲨烯合酶，可通过诱导 GPX4 降解来诱导铁死亡。

AT56 是口服有活性的脂钙蛋白型前列腺素 D 合酶 (L-PGDS) 选择性抑制剂，其IC50=95 μM，Ki=75 μM。它能够特异性地抑制L-PGDS 催化的 PGD2介导的嗜睡或疼痛反应。

yGsy2p-IN-1 是酵母糖原合酶 2 抑制剂。它是竞争性人类糖原合酶 1 抑制剂(IC50:2.75 µM)，对野生型 hGYS1 的Ki=为 1.31 µM。它是吡唑抑制剂，可用于糖原储存疾病的研究。

PF-04802367是 GSK-3高选择性抑制剂，对 GSK-3β酶的 IC50为 2.1 nM。它抑制两种 GSK-3 亚型（GSK-3α和GSK-3β）效果差不多，IC50值分别为 10.0 和 9.0 nM。它具有理想的中枢神经系统特性和效力。

Orlistat (Tetrahydrolipstatin) 是一种脂肪酶 (lipase) 抑制剂，也是一种脂肪酸合成酶 (FASN) 抑制剂。Orlistat 具有促减肥的作用。

ML406 是一种小分子探针，通过抑制M.tuberculosisBioA(DAPA 合酶) 显示出抗结核活性，IC50为 30 nM。

G140 是选择性环状GMP-AMP 合酶抑制剂，具有抗炎活性，对 h-cGAS 和 m-cGAS 的IC50值分别为 14.0 和 442 nM。

ATP synthase inhibitor 1 是 F1 FO-ATP 合酶复合物 c 亚基的有效抑制剂，抑制线粒体通透性转换孔的开放。

ATP synthase inhibitor3（compound PT6）作为一种分枝杆菌F-ATP合酶抑制剂（IC50=0.788 μM），显示出口服活性。此化合物能有效抑制体外Mycobacterium tuberculosis H37Rv菌株（ATCC-27294）的生长，并在IC50值达30 μM时显著降低细胞内ATP水平。

S.pombe lumazine synthase-IN-1 is an inhibitor of lumazine synthases with Ki values of 243 μM and 9.6 μM for Schizosaccharomyces pombe and Mycobacterium tuberculosis lumazine synthases, respectively[1]. [1]. Arindam Talukdar, et al. Discovery and Development of a Small Molecule Library With Lumazine Synthase Inhibitory Activity. J Org Chem. 2009 Aug 7;74(15):5123-34.

Polyketide synthase 13-IN-3 (compound 41) is a potent inhibitor of polyketide synthase 13, demonstrating a minimum inhibitory concentration (MIC) range of 0.0625-0.125 μg mL against the M. tuberculosis strain H37Rv.

Polyketide synthase 13-IN-1 (compound 32) is a polyketide synthase 13 inhibitor.

Phospho-Glycogen Synthase Peptide-2, a substrate for glycogen synthase kinase-3 (GSK-3), serves as a peptide substrate effective in the affinity purification of protein-serine kinases.

Chitin synthase inhibitor 2 (compound 2b) is a highly potent inhibitor of chitin synthase, with an IC50 value of 0.09 mM and a K i value of 0.12 mM. This compound exhibits antimicrobial activities in vitro and demonstrates synergistic or additive effects when combined with fluconazole or polyoxin B [1].

Chitin synthase inhibitor 3 (compound 2d) 是一种高效的chitin synthase抑制剂，具有0.16 mM的IC50值，并对candida albicans显示出1 μg mL的MIC，表现出抗真菌活性。

Polyketide synthase 13-IN-2 (comp 42) is a potent inhibitor of polyketide synthase 13 in Mycobacterium tuberculosis. It demonstrates a minimum inhibitory concentration (MIC) of 0.25 μg mL [1].

Glucosylceramide synthase-IN-3 (compound BZ1) is a highly potent, brain-penetrant, and orally active inhibitor of glucosylceramide synthase (GCS), exhibiting an IC50 value of 16 nM for human GCS. This compound, designated as Glucosylceramide synthase-IN-3, finds potential applications in Gaucher's disease research [1] [2].

ATP synthase inhibitor2 是一个铜绿假单胞菌 (PA)ATP synthase 抑制剂 (IC50=10 μg mL)，在 128 μg mL 时可完全抑制铜绿假单胞菌 (PA) 的 ATP 合成活性。

GlcN-6-P Synthase-IN-1 (Compound 4d) is a potent inhibitor of Glucosamine-6-phosphate (GlcN-6-P) synthase, with an IC50 of 3.47 μM. This compound demonstrates remarkable antimicrobial activity and exhibits excellent penetration in the central nervous system. Additionally, GlcN-6-P Synthase-IN-1 is capable of inhibiting cytochrome P450, specifically the CYP3A4 isoform [1].

Chitin synthase inhibitor 1 是有效的、选择性的几丁质合酶 (CHS) 抑制剂，IC50值为0.12 mM。Chitin synthase inhibitor 1 强效抑制耐药真菌变体。

Chitin synthase inhibitor 8 是一种 chitin synthase (CHS) 抑制剂，具有广谱抗真菌作用，能够用于真菌感染相关研究。

Chitin synthase inhibitor 7 (compound 9c) 是一种 chitin synthase (CHS) 的有效抑制剂 (IC50: 0.37 nM)。Chitin synthase inhibitor 7 对耐药真菌具有广谱抗真菌作用。Chitin synthase inhibitor 7 能够用于研究真菌感染。

Glucosylceramide synthase-IN-2 (compound T-690) 是一种有效的、具有血脑屏障通透性的、口服具有活力的 glucosylceramide synthase (GCS) 抑制剂，作用于人 GCS (IC50: 15 nM) 和小鼠 GCS (IC50: 190 nM)。Glucosylceramide synthase-IN-2 能够非竞争性抑制 C8 神经酰胺和 UDP 葡萄糖。Glucosylceramide synthase-IN-2 能够用于研究戈谢病。