a-esterase 1

Fluorescein diacetate (Di-O-acetylfluorescein) 是一种人谷胱甘肽硫转移酶 Pi 的荧光底物，是一种细胞渗透性的酯酶底物。

胆固醇酯酶 (Cholesterol esterase) 是一种在肠道内将胆固醇酯水解为胆固醇和游离脂肪酸的酶。胆固醇在腺泡细胞中合成，储存在酶原颗粒中。胆固醇酯酶又称胆盐刺激脂肪酶、羧基酯脂肪酶，具有促进胆固醇吸收的作用。

SN-38-CM2 BS2是一种分裂酯酶，在体外5 min内转化为SN-38的转化率超过95%。SN-38-CM2通过诱导蛋白-蛋白相互作用 (PPI) 依赖的酯酶介导MDA-MB-231细胞死亡。

Benastatin C is a polyketide synthase-derived benastatin that has been found inStreptomycesand has diverse biological activities.1,2It inhibits glutathione S-transferase (GST; IC50= 24 μg ml for the rat liver enzyme).2Benastatin C also inhibits the esterase activity of isolated porcine pancreatic lipase (IC50= 10 μg ml). It increases LPS- or concanavalin A-induced blastogenesis of isolated mouse spleen lymphocytes in a concentration-dependent manner. 1.Xu, Z., Schenk, A., and Hertweck, C.Molecular analysis of the benastatin biosynthetic pathway and genetic engineering of altered fatty acid-polyketide hybridsJ. Am. Chem. Soc.129(18)6022-6030(2007) 2.Aoyama, T., Kojima, F., Yamazaki, T., et al.Benastatins C and D, new inhibitors of glutathione S-transferase, produced by Streptomyces sp. MI384-DF12. Production, isolation, structure determination and biological activitiesJ. Antibiot. (Tokyo)46(5)712-718(1993)

Monometacrine 是一种胆固醇酯酶抑制剂，具有抗抑郁作用。

sPLA2-IIA Inhibitor 是 FLSYK 的环状五肽类似物，具有环2-Nal-Leu-Ser-2-Nal-Arg (c2) 结构，能够特异性结合 hGIIA（人类 IIA 磷脂酶 A2），有效抑制其酯键水解活性。该化合物作为酯酶超家族的一员，主要作用于甘油磷脂 sn-2 位置的酯键，从而阻断游离脂肪酸和花生四烯酸等物质的释放。

α-Glycosidase-IN-1 (compound MZ7) 是 α-GLY(α- 糖苷酶) 的有效抑制剂 (IC50: 44.72 nM, Ki: 44.74 nM)。α-Glycosidase-IN-1 也能够抑制人碳酸酐酶同工酶 I 和 II (hCA I 和hCA II)以及乙酰胆碱酯酶 (AChE)，其IC50值分别为 104.87、100.04 和 654.87 nM。α-Glycosidase-IN-1 能够用于研究糖尿病、阿尔茨海默病、溃疡、心力衰竭、癫痫等多种疾病。

Clostripain(Clostridiopeptidase B)为源自Clostridium histolyticum的蛋白质水解酶，展现酯酶、酰胺酶及蛋白酶活性，特异性高，针对精氨酸羧基肽键。

Homogentisic acid lactone (Compound 1) 是一种真菌代谢物，具有抗真菌活性，发现于真菌WF5。它对植物病原菌F. graminearum表现出抑制效果。此外，Homogentisic acid lactone 可作为底物用于测定血清对氧酮酶 芳香酯酶 1 (PON1) 活性。

TEI-9648, a Vitamin D3 Lactone analogue, is a potent and specific vitamin D receptor (VDR) antagonist. TEI-9648 inhibits VDR/VDRE-mediated genomic actions of 1α,25(OH)2D3. TEI-9648 also inhibits HL-60 cell differentiation induced by of 1α,25(OH)2D3. TEI-9648 has the potential for bone metabolism research[1][2]. TEI-9648 (10-1000 nM) dose-dependently blocks the reciprocal changes of CD11b and CD71 expression associated with HL-60 cell differentiation induced by 1α,25(OH)2D3[1]. TEI-9648 has consistently weaker suppressive effect than TEI-9647[1]. TEI-9648 can not induce cell differentiation even after treatment at 1 μM in HL-60 cell[1]. TEI-9648 alone can not induce activation of NBT-reducing activity or α-NB esterase activity. In contrast, TEI-9648 markedly suppresses the up-regulation induced by 1α,25(OH)2D3 (0.1 nM) in HL-60 cells[1]. [1]. Miura D, et al. Antagonistic action of novel 1α,25-dihydroxyvitamin D3-26, 23-lactone analogs on differentiation of human leukemia cells (HL-60) induced by 1α,25-dihydroxyvitamin D3. J Biol Chem. 1999 Jun 4;274(23):16392-9. [2]. Kazuya Takenouchi, et al. Synthesis and structure-activity relationships of TEI-9647 derivatives as Vitamin D3 antagonists. J Steroid Biochem Mol Biol. 2004 May;89-90(1-5):31-4.

CEase-IN-1 (Compound A1H3) 是胆固醇酯酶（CEase）有效的、选择性的抑制剂，IC50值为 0.36 μM，它可用于研究高胆固醇血症。

Tefinostat (CHR-2845) 是一种有效的单核细胞 巨噬细胞靶向组蛋白脱乙酰酶 (HDAC) 抑制剂。 Tefinostat 可被胞内酯酶人羧酸酯酶-1 (hCE-1) 裂解成活性酸 CHR-2847。Tefinostat 具有抗肿瘤活性，可用于研究白血病和晚期血液系统恶性肿瘤。