α/β hydrolase in 1

α β-Hydrolase-IN-1 demonstrates exceptional potency, with MICs of 50 μM (25 μg mL) against M. smegmatis and 16 μM (8.4 μg mL) against M. tuberculosis H37Ra, establishing it as a superior compound in this class.

Soluble epoxide hydrolase (sEH) PROTAC 1a是一种利用蛋白质降解靶向嵌合体(PROTAC)技术，通过连接区域将cereblon配体1与sEH抑制剂t-TUCB结合。该化合物通过促进sEH的降解，特异性抑制sEH的水解酶活性(IC50 = 0.8 nM)，相较于其磷酸酶活性(IC50 = >10,000 nM)具有较高选择性。sEH PROTAC 1a还特定促进细胞质中而非过氧体中的sEH降解，并通过溶酶体而非蛋白酶体实现其降解。它能够降低thapsigargin诱导的HepG2与293T细胞中磷酸化的inositol-requiring enzyme 1α (IRE1α)水平和X-box结合蛋白1 (XBP1)剪接，表明能减少ER应激。

Acetylhydrolase-IN-1 is an inhibitor of the esterase 1-Alkyl-2-acetylglycerophosphocholine (Alkylacetyl-GPC: acetylhydrolase).

mEH-IN-1 (Compound 62) is a potent inhibitor of microsomal epoxide hydrolase (mEH), with an IC50 value of 2.2 nM. mEH is an α β-fold hydrolase enzyme that is widely expressed in various mammalian tissues, responsible for the hydrolysis of a diverse range of epoxide-containing molecules. This enzyme is primarily localized in the endoplasmic reticulum (ER) of eukaryotic cells. Research involving mEH-IN-1 can contribute to the understanding of preeclampsia, hypercholanemia, and cancer [1].

Orlistat-d3 is intended for use as an internal standard for the quantification of orlistat by GC- or LC-MS. Orlistat is a digestive lipase inhibitor. It inhibits diacylglycerol lipase α (DAGLα), DAGLβ, α β-hydrolase domain-containing protein 12 (ABHD12), ABHD16A, and platelet-activating factor acetylhydrolase (PAF-AH; IC50s = 0.06, 0.1, 0.08, 0.03, and 0.05 µM, respectively), as well as pancreatic lipase and hormone-sensitive lipase (IC50s = 0.65 and 2.1 µg ml, respectively) but does not inhibit fatty acid amide hydrolase (FAAH) or KIAA1363 (IC50s = >100 µM for both). Orlistat decreases ionomycin-induced production of the endocannabinoid 2-arachidonoyl glycerol (2-AG) in N18TG2 murine neuroblastoma cells when used at a concentration of 1 µM. It also inhibits fatty acid synthase (FASN; Kiapp = ~0.1 µM for the human enzyme) and the proliferation of PC3 prostate cancer cells in a concentration-dependent manner. Orlistat (10 mg kg) decreases serum cholesterol levels and total bod......

JZP-MA-11是一种用于正电子发射断层扫描(PET)的配体，专一性靶向内源性大麻素α β-水解酶结构域6(ABHD6)酶，并具有126 nM的IC50值，表明其对ABHD6有选择性抑制作用。JZP-MA-11能有效穿过血脑屏障(BBB)。[18F]JZP-MA-11展现出在靶向小鼠及非人灵长类(NHP)大脑ABHD6方面的临床前评估潜力。

ABHD antagonist 1 是一种具有 ABHD6 (α β-Hydrolase domain containing 6) 抑制活性的化合物，涉及调节由 ABHD6 参与的生物化学途径，从而影响细胞功能和炎症反应。ABHD antagonist 1 可用于疼痛、神经性疾病、炎症性疾病、自身免疫疾病、代谢性疾病以及癌症等领域的研究。