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38

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T76139 Cholesterol esterase

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。
T15082 DDAO

Others Others
DDAO 是有潜在用途的近红外红色荧光探针,其激发波长 (600-650 nm) 和长发射波长 (λem = 656 nm)可以调节。它可用于不同酶活性的检测,如 β-半乳糖苷酶,羧酸酯酶 2,硫酸酯酶,蛋白质磷酸酶 2A,人白蛋白和酯酶。
T0157 Roxatidine Acetate hydrochloride

HOE 760,盐酸罗沙替丁醋酸酯,Roxatidine Acetate HCl

Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Roxatidine Acetate hydrochloride (HOE 760) 是一种特异性和竞争性的组胺 H2 受体拮抗剂,能抑制胃酸分泌,可用于胃溃疡和十二指肠溃疡的研究。
T18894 5(6)-CFDA

CFDA,5-(6)-Carboxyfluorescein diacetate,5(6)-羧基荧光素二乙酸酯

Others Others
5(6)-CFDA (5-(6)-Carboxyfluorescein diacetate) 是具有细胞渗透性的胺反应型绿色荧光探针(λex: 492 nm; λem: 517 nm),可用于细胞染色分析。
T77524 Carboxylesterase-IN-2

Wnt/beta-catenin; Lipid Cytoskeletal Signaling; Metabolism; Stem Cells
Carboxylesterase-IN-2 是一种有效的 Carboxylesterase Notum 抑制剂(IC50 ≤10 nM)。Carboxylesterase-IN-2具有研究癌症疾病的潜力。
T60788 Carboxylesterase-IN-3

Wnt/beta-catenin; Lipid Cytoskeletal Signaling; Metabolism; Stem Cells
Carboxylesterase-IN-3 是一种有效的Carboxylesterase Notum 抑制剂(IC50≤ 10 nM)。Carboxylesterase-IN-3 具有研究癌症疾病的潜力。
T60057 Notum pectinacetylesterase-1

Others Others
Notum pectinacetylesterase-1是一种 Notum Pectinacetylesterase 抑制剂, IC50 < 0.025 μM。
T76138 Phosphodiesterase

Phosphodiesterase(PDE) 是一种可以催化环核苷酸3 '环磷酸键水解的酶,常用于生化研究。Phosphodiesterase 可作为第二信使分子 cAMP 和 cGMP 介导的信号转导的重要调节因子。根据其对环核苷酸的特异性也可以分别不同类型,如 PDE1-PDE11,在多种疾病方面也具有一定的潜力。
T76156 Sphingomyelin phosphodiesterase

Sphingomyelinphosphodiesterase 是一种水解酶,参与鞘磷脂代谢过程。Sphingomyelinphosphodiesterase 水解鞘磷脂,使其向磷酸胆碱和神经酰胺转化。Sphingomyelinphosphodiesterase 还在细胞分化、各种免疫和炎症反应以及细胞内胆固醇运输和代谢中发挥重要作用。
T63015 Pancreatic lipase/Carboxylesterase 1-IN-1

Pancreatic lipase/Carboxylesterase 1-IN-1 (Compound 39) 是一种有效的、双重的胰脂酶 (PL) 和人羧酸酯酶 1A (hCES1A) 抑制剂,作用于 PL (IC50: 2.13 μM) 和 hCES1A (IC50: 0.055 μM)。
T76133 Phosphodiesterase II

PhosphodiesteraseII,即磷酸二酯酶 2,主要参与水解重要的第二信使环磷酸腺苷 (cAMP) 和环磷酸鸟苷 (cGMP),常用于生化研究。PhosphodiesteraseII 表达于多种组织,如肾上腺髓质、脑、心脏、血小板、巨噬细胞和内皮细胞,可参与调节许多不同的细胞内过程。
T76123 Carboxylesterase

Carboxylesterase (CESs), 即羧酸酯水解酶,广泛分布于自然界,常见于哺乳动物肝脏,常用于生化研究。Carboxylesterase 催化多种内源和外源底物的水解,包括酯、硫酯、氨基甲酸酯和酰胺,使羧酸酯水解成相应的醇和羧酸。
T36018 Phosphodiesterase 4 Inhibitor

Phosphodiesterase 4 (PDE4) inhibitor is an inhibitor of PDE4 with an IC50 value of 0.10 μM for the human recombinant enzyme.
T40237 Carboxylesterase-IN-1

Carboxylesterase-IN-1, a novel pesticide, acts as an inhibitor of carboxylesterase at a concentration of 50 μg/mL, displaying comparable inhibitory activity to the established inhibitor triphenyl phosphate.
T76130 Acetylcholinesterase

Acetylcholinesterase(ACHE; EC 3.1.1.7), 即乙酰胆碱酯酶,是一种胆碱能酶,主要存在于神经肌肉接头和胆碱能类型的化学突触中,常用于生化研究。Acetylcholinesterase 可以催化乙酰胆碱和其他一些充当神经递质的胆碱酯分解或水解为乙酸和胆碱。Acetylcholinesterase 主要作用是终止突触之间的神经元传递和信号传导,以防止 ACh 扩散和附近受体的激活。
T5943 4,4'-DIMETHOXYBENZIL

p-Anisil,4,4'-二甲氧基苯酚酯

Others Others
4,4'-Dimethoxybenzil (trans-4-Sphingenine) 是人肠胃羧基酯酶抑制剂(Ki:70 nM)。
T18880 BCDA

酯酶显色底物-1,5-bromo-4-chloroindoxyl acetate

Others Others
BCDA (5-bromo-4-chloroindoxyl acetate) 是酯酶的显色底物,可有效检测酯酶的活性。
T19323 Fluorescein diacetate

荧光素二乙酸酯,3,6-Diacetoxyfluoran,Di-O-acetylfluorescein

Others Others
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。
T17028 Tefinostat

CHR-2845

HDAC Chromatin/Epigenetic; DNA Damage/DNA Repair
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。
T12936 SMP-028

Others Others
SMP-028 is a neutral cholesterol esterase (CEase) inhibitor(IC50 : 1.01 μM).
T38119 4-Methylumbelliferyl Caprylate

4-Methylumbelliferyl caprylate (MUCAP) is a fluorogenic substrate for C8 esterase. MUCAP is cleaved by C8 esterase to release the fluorescent moiety 4-methylumbelliferyl (4-MU). 4-MU fluorescence is pH-dependent with excitation maxima of 320 and 360 nm at low (1.97-6.72) and high (7.12-10.3) pH, respectively, and an emission maximum ranging from 445 to 455 nm, increasing as pH decreases.
T78413 ETZ

C3-CA-DTZ

ETZ (C3-CA-DTZ) 是一种具潜力的荧光素酶前体,能在体内经非特异性酯酶活化,促进荧光素在脑部的传输。
T70577 PEN-866

PEN-866 is a potential agent for controlling early stage tumor growth for non-small cell lung cancer (NSCLC). PEN-866 is a novel esterase-cleavable conjugate of an HSP90i and a topoisomerase I inhibitor, SN-38
T38895 Zanapezil free base

TAK-147 free base,Zanapezil free base

Zanapezil (TAK-147) is a powerful and selective inhibitor of acetylcholine esterase (AChE). It demonstrates significant and reversible inhibition of AChE activity in rat cerebral cortex homogenates (IC50 = 51.2 nM). Furthermore, Zanapezil exhibits moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. This compound holds promise for the investigation of the initial stages of Alzheimer's disease (AD).
T24256 KBR 2822

KBR 2822 is an inhibitor of esterase.
T83294 5-Bromo-1H-indol-3-yl octanoate

5-Bromo-1H-indol-3-yl octanoate 是一种酯酶的显色底物,具有 C8 活性。该化合物在裂解时产生蓝色沉淀。
T13529 Acetylhydrolase-IN-1

Others Others
Acetylhydrolase-IN-1 is an inhibitor of the esterase 1-Alkyl-2-acetylglycerophosphocholine (Alkylacetyl-GPC: acetylhydrolase).
TD0055 Fluo-8, AM

Fluo-8,AM is one of the most commonly used fluorescent probes to detect intracellular calcium concentration.Fluo-8, which penetrates the cell membrane and enters the cell, is cut by the intracellular esterase to form fluO-8, and thus is trapped in the cel
T76145 Clostripain

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。
T74382 AChE-IN-4

AChE-IN-4为乙酰胆碱酯酶抑制(AChEI),其 IC50值为24.1μM。
T35979 Benastatin C

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.Molecul...
T60579 CEase-IN-1

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。
T81115 sPLA2-IIA Inhibitor

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。
T83293 5-CFDA-AM

5-CFDA-AM作为一种细胞渗透性的酯酶底物,用于测定酶活性和细胞膜完整性,该化合物为电子中性,其渗透细胞的能力超过CFDA且所需浓度更低。在细胞内部,5-CFDA-AM经酯酶水解生成羧基荧光素,后者带有额外负电荷,因此能更有效地在细胞内保留。
T79493 HIV-1 protease-IN-10

PKC Chromatin/Epigenetic; Cytoskeletal Signaling
HIV-1protease-IN-10(化合物2)显示出对HIV-1潜伏期的逆转活性,IC50值为0.22 μM。该化合物通过与PKCδC1b结构域结合展现活性,IC50值为0.69 μM。此外,HIV-1protease-IN-10对于酯酶介导的水解表现出稳定性。
T63941 α-Glycosidase-IN-1

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。
T37214 5-trans Latanoprost (free acid)

Latanoprost is an F-series prostaglandin (PG) analog which has been approved for use as an ocular hypotensive drug. Latanoprost is an isopropyl ester, a prodrug form which is converted to latanoprost (free acid) by endogenous esterase enzymes. The free acid form is 200 times more potent than latanoprost as a ligand for the human recombinant FP receptor. 5-trans Latanoprost (free acid) is an isomer of latanoprost (free acid) wherein the double bond between carbons 5 and 6 has been changed from ci...
T36593 TEI-9648

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 cons...

化合物

Cholesterol esterase
Cat.No: T76139
Synonym:
Target:
DDAO
Cat.No: T15082
Synonym:
Target: Others
Roxatidine Acetate hydrochloride
Cat.No: T0157
Synonym: HOE 760,盐酸罗沙替丁醋酸酯,Roxatidine Acetate HCl
Target: Histamine Receptor
5(6)-CFDA
Cat.No: T18894
Synonym: CFDA,5-(6)-Carboxyfluorescein diacetate,5(6)-羧基荧光素二乙酸酯
Target: Others
Carboxylesterase-IN-2
Cat.No: T77524
Synonym:
Target: Wnt/beta-catenin, Lipid
Carboxylesterase-IN-3
Cat.No: T60788
Synonym:
Target: Wnt/beta-catenin, Lipid
Notum pectinacetylesterase-1
Cat.No: T60057
Synonym:
Target: Others
Phosphodiesterase
Cat.No: T76138
Synonym:
Target:
Sphingomyelin phosphodiesterase
Cat.No: T76156
Synonym:
Target:
Pancreatic lipase/Carboxylesterase 1-IN-1
Cat.No: T63015
Synonym:
Target:
Phosphodiesterase II
Cat.No: T76133
Synonym:
Target:
Carboxylesterase
Cat.No: T76123
Synonym:
Target:
Phosphodiesterase 4 Inhibitor
Cat.No: T36018
Synonym:
Target:
Carboxylesterase-IN-1
Cat.No: T40237
Synonym:
Target:
Acetylcholinesterase
Cat.No: T76130
Synonym:
Target:
4,4'-DIMETHOXYBENZIL
Cat.No: T5943
Synonym: p-Anisil,4,4'-二甲氧基苯酚酯
Target: Others
BCDA
Cat.No: T18880
Synonym: 酯酶显色底物-1,5-bromo-4-chloroindoxyl acetate
Target: Others
Fluorescein diacetate
Cat.No: T19323
Synonym: 荧光素二乙酸酯,3,6-Diacetoxyfluoran,Di-O-acetylfluorescein
Target: Others
Tefinostat
Cat.No: T17028
Synonym: CHR-2845
Target: HDAC
SMP-028
Cat.No: T12936
Synonym:
Target: Others
4-Methylumbelliferyl Caprylate
Cat.No: T38119
Synonym:
Target:
ETZ
Cat.No: T78413
Synonym: C3-CA-DTZ
Target:
PEN-866
Cat.No: T70577
Synonym:
Target:
Zanapezil free base
Cat.No: T38895
Synonym: TAK-147 free base,Zanapezil free base
Target:
KBR 2822
Cat.No: T24256
Synonym:
Target:
5-Bromo-1H-indol-3-yl octanoate
Cat.No: T83294
Synonym:
Target:
Acetylhydrolase-IN-1
Cat.No: T13529
Synonym:
Target: Others
Fluo-8, AM
Cat.No: TD0055
Synonym:
Target:
Clostripain
Cat.No: T76145
Synonym:
Target:
AChE-IN-4
Cat.No: T74382
Synonym:
Target:
Benastatin C
Cat.No: T35979
Synonym:
Target:
CEase-IN-1
Cat.No: T60579
Synonym:
Target:
sPLA2-IIA Inhibitor
Cat.No: T81115
Synonym:
Target:
5-CFDA-AM
Cat.No: T83293
Synonym:
Target:
HIV-1 protease-IN-10
Cat.No: T79493
Synonym:
Target: PKC
α-Glycosidase-IN-1
Cat.No: T63941
Synonym:
Target:
5-trans Latanoprost (free acid)
Cat.No: T37214
Synonym:
Target:
TEI-9648
Cat.No: T36593
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
TN3820 Demethoxydeacetoxypseudolaric acid B

Others Others
Demethoxydeacetoxypseudolaric acid B 是 pseudolaric acid C2 的一种代谢物。
T11203 Enocyanin

Others Others
Enocyanin, an anthocyanin extracted from grapes, exhibits inhibitory effects on leucine aminopeptidase, acid phosphatase, γ-glutamyl transpeptidase, and esterase activity.

天然产物

Demethoxydeacetoxypseudolaric acid B
Cat.No: TN3820
Synonym:
Target: Others
Enocyanin
Cat.No: T11203
Synonym:
Target: Others
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