serine hydrolase

PAL-4刺激 LYPLAL1 的活性, 一种特征不佳的丝氨酸水解酶，与人类代谢特征具有复杂的遗传联系。

JW 480 是一种有效的丝氨酸水解酶 KIAA1363选择性抑制剂。

AA38-3 (1-Piperidinecarboxylic acid, 4-nitrophenyl ester) 是丝氨酸水解酶抑制剂，能够抑制三种 SHs：ABHD6，ABHD11 和 FAAH。

AA26-9 是广谱丝氨酸水解酶的高效抑制剂。它的靶点包括丝氨酸肽酶、酰胺酶、脂肪酶、酯酶和硫酯酶。在永生化 T 细胞系，检测到它对 40+ 丝氨酸水解酶中的 1 3 有抑制作用。

ABC99是 wnt 脱酰基酶的一种选择性不可逆抑制剂。ABC99抑制 NOTUM（IC50:13 nM）。它还显示了对丝氨酸水解酶家族的优良选择性。

LY2183240 是大麻素摄取阻滞剂。它是内源性大麻素降解酶脂肪酸酰胺水解酶的有效共价抑制剂。它抑制脂肪酸酰胺水解酶 (FAAH) 活性，IC50 为12.4 nM。它也抑制其他几种脑丝氨酸水解酶，对 MAG 脂肪酶、bh6 和 KIAA1363 的 IC50分别为 5.3、0.09 和 8.2 nM。

WWL 154 是一种丝氨酸水解酶 (SH) 和脂肪酸酰胺水解酶 FAAH-4 抑制剂。

Serine Hydrolase inhibitor-21（化合物8）为一种抑制丝氨酸水解酶的吡啶类化合物，其对BuChE的Ki值为429 nM，有望用于阿尔茨海默病的研究。

Nitisinone-13C6is intended for use as an internal standard for the quantification of nitisinone by GC- or LC-MS. Nitisinone is an inhibitor of 4-hydroxyphenylpyruvate dioxygenase (HPPD), which converts 4-hydroxyphenylpyruvate (HPPA) to homogentisate in the tyrosine catabolic pathway.1Nitisinone increases urinary levels of HPPA and 4-hydroxyphenyllactate (HPLA) in rats when administered at a dose of 10 mg kg. Nitisinone (3 mg kg) prevents the neonatal lethality of fumarylacetoacetate hydrolase (FAH) deficiency in mice when administered to pregnant dams.2It exhibits hepatoprotective effects inFAH- -mice, such as prevention of increases in plasma levels of aspartate serine aminotransferase (AST) and conjugated bilirubin, when administration is continued following birth at a dose of 1 mg kg. Nitisinone (100 μg) decreases urinary excretion of homogentisate and increases urinary excretion of HPPA, HPLA, and 4-hydroxyphenylacetate in a mouse model of alkaptonuria induced by ethylnitrosourea.3Formulations containing nitisinone have been used in the treatment of hereditary tyrosinemia type 1 (HT-1). 1.Ellis, M.K., Whitfield, A.C., Gowans, L.A., et al.Inhibition of 4-hydroxyphenylpyruvate dioxygenase by 2-(2-nitro-4-trifluoromethylbenzoyl)-cyclohexane-1,3-dione and 2-(2-chloro-4-methanesulfonylbenzoyl)-cyclohexane-1,3-dioneToxicol. Appl. Pharmacol.133(1)12-19(1995) 2.Grompe, M., Lindstedt, S., al-Dhalimy, M., et al.Pharmacological correction of neonatal lethal hepatic dysfunction in a murine model of hereditary tyrosinaemia type INat. Genet.10(4)453-460(1995) 3.Suzuki, Y., Oda, K., Yoshikawa, Y., et al.A novel therapeutic trial of homogentisic aciduria in a murine model of alkaptonuriaJ. Hum. Genet.44(2)79-84(1999)

WWL113 is a selective and orally active Ces3 and Ces1f inhibitor (IC50: 120 nM and 100 nM for Ces3 and Ces1f, respectively). WWL113 appears to display excellent selectivity for the 60-kDa serine hydrolase.

JJH260 is an N-hydroxy hydantoin carbamate that inhibits androgen-induced gene 1 (AIG1), an enzyme that hydrolyzes fatty acid esters of hydroxy fatty acids (FAHFAs). It blocks the hydrolysis of 9-PAHSA with an IC50 value of 0.57 μM. JJH260 also inhibits the novel FAHFA hydrolase androgen-dependent TFPI-regulating protein (ADTRP; IC50 = 8.5 μM), as well as the serine hydrolase ABHD6 and the lysophospholipases LYPLA1 and LYPLA2. JJH260 inhibits the FAHFA hydrolase activity of LNCaP and T cell lysates and intact cells.

JZP-MA-13是一种选择性α β-水解酶结构域6 (ABHD6) 抑制剂，其IC50值为392 nM。该化合物对MAGL、ABHD12、FAAH或其它丝氨酸水解酶不表现出抑制作用。JZP-MA-13还被用作ABHD6在体内成像的正电子发射断层扫描(PET)配体。

ABC44 是丝氨酸水解酶 (serine hydrolase) 的有效抑制剂，对棕榈酰蛋白硫酯酶 1 (PPT1) 原位和体外的 IC50 分别为 0.1 μM 和 6.5 μM。ABC44 能够用于研究婴儿晚期神经元样脂褐质沉积症。

Tripeptidyl peptidase II (TPPII) is a serine peptidase of the subtilisin-type which removes tripeptides from the free NH2 terminus of oligopeptides. AAF-CMK is an irreversible inhibitor of TPPII commonly used at 10-100 μM. It does not significantly interfere with the chymotrypsin-like activity of the proteasome. AAF-CMK also inhibits bleomycin hydrolase and puromycin-sensitive aminopeptidase when used at 50 μM.

Fatty acid amide hydrolase (FAAH), an enzyme responsible for the hydrolysis and inactivation of fatty acid amides like anandamide and oleamide, has been identified as a target by the potent FAAH inhibitor PHOP. PHOP demonstrates remarkable inhibitory activity with K_i values as low as 0.094 nM for human FAAH and 0.2 nM for rat FAAH. Additionally, through a proteomics assay focusing on the serine hydrolase enzyme family, to which FAAH belongs, PHOP's selectivity was evaluated, presenting IC_50 values of 1.1 nM against FAAH, 1.4 nM against triacylglycerol hydrolase (TGH), and greater than 100 µM against an uncharacterized hydrolase (KIAA1363). This specificity profile of PHOP underscores its potential for yielding precise outcomes in studies involving complex biological systems.

ABC34 is an inactive control probe for JJH260 , the inhibitor of androgen-induced gene 1 (AIG1), an enzyme that hydrolyzes fatty acid esters of hydroxy fatty acids (FAHFAs). ABC34 demonstrates an IC50 value greater than 25 μM for the inhibition of 9-PAHSA but is more potent in blocking the serine hydrolase ABHD6 and the palmitoyl-protein hydrolase PPT1, which are both off-targets of JJH260.

Nitisinone (SC0735) 是一种 4-羟基苯丙酮酸双加氧酶抑制剂。