Proteases(蛋白酶)

Proteases, also known as peptidases or proteolytic enzymes, consists of a large number of enzymes catalyzing the hydrolysis of peptide bonds and subsequently resulting in the degradation of protein substrates into amino acids. Proteases are involved in a wide range of human diseases, including cancer, neurodegenerative disorders, inflammatory diseases and cardiovascular diseases. Thus numerous proteases inhibitors (small molecules and proteins) have been identified to block activity of proteases. Proteases inhibitors can be classified into different types based on the class of proteases they inhibit through two general mechanisms, irreversible “trapping” reactions and reversible tight-binding reactions. Proteases inhibitors have been used as diagnostic or therapeutic agents for the treatment of proteases-related diseases.

Products for Proteases

Cat.No. 产品名称 Information
GC38929 MMP-9-IN-1 MMP-9-IN-1是基质金属蛋白酶-9（MMP-9）的特异性抑制剂。它通过选择性靶向MMP-9的血浆铜蓝蛋白（PEX）结构域发挥作用，Kd值为2.1μM。
GC38920 L-Carnitine hydrochloride
L-肉毒碱盐酸盐; (R)-Carnitine hydrochloride; Levocarnitine hydrochloride
L-Carnitine ((R)-Carnitine, Levocarnitine) hydrochloride improves oxygen saturation, and inhibits leukotriene synthesis. L-Carnitine hydrochloride functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation.
GC38909 EN40
EN40 是一种有效的选择性乙醛脱氢酶 3A1 (ALDH3A1) 抑制剂，一种共价配体，IC50 值为 2 uM。
GC38903 Deslanoside
去乙酰西地兰; Deacetyllanatoside C; Desacetyllanatoside C
A cardiac glycoside
GC38885 alpha-D-glucose
a-无水葡萄糖酯
Alpha-D-Glucose is a primary source of energy for living organisms. It is naturally occurring and is found in fruits and other parts of plants in its free state. It is an intermediate in glycolysis/gluconeogenesis pathway.
GC38883 9-Ethyladenine
9-乙基腺嘌呤
9-Ethyladenine 是 APRT (腺嘌呤磷酸核糖基转移酶) 的部分有效抑制剂。
GC38882 5-ALA benzyl ester hydrochloride
5-氨基酮戊酸苄酯盐酸盐,Benzyl-ALA hydrochloride
5-ALA benzyl ester hydrochloride (Benzyl-ALA hydrochloride) 是一种用作光检测器的原卟啉前体。5-ALA benzyl ester hydrochloride 诱导原卟啉 IX (PPIX) 在结肠癌细胞系中的积聚。
GC38881 10,12-Tricosadiynoic acid
10,12-二十三联炔酸
10,12-Tricosadiynoic acid是一种具有高效特异性、选择性和口服活性的酰基辅酶A氧化酶-1（ACOX1）抑制剂。
GC46026 TMI 1
WAY-171318
An ADAM and MMP inhibitor
GC46023 Phenylpyropene A
苯基吡喃菌素A
A fungal metabolite
GC46002 Prunetin
樱黄素
An isoflavone with diverse biological activities
GC45994 Hydrocortisone Acetate
Cortef Acetate, Hydrin 2, Hydrocortisone 21-Acetate, Hydroxycorticosterone Acetate, 17α-Hydroxycorticosterone Acetate, Isopto-Hydrocortisone
A synthetic corticosteroid
GC45978 1,10-Phenanthroline (hydrate)
邻菲罗啉,1,10-Phenanthroline monohydrate
A metal chelator and inhibitor of metalloproteases
GC45969 6β-hydroxy Eplerenone
依普利酮6-BETA-羟基类似物
A major metabolite of eplerenone
GC45962 12-hydroxy Lauric Acid
端羟基12酸
A hydroxylated fatty acid
GC45960 9c(i472)
15-LOX-1 Inhibitor i472
A 15-LO-1 inhibitor
GC45951 BLX3887
15-LO-1 Inhibitor 3887
A 15-LO-1 inhibitor
GC45948 1,2,3-Trilinoelaidoyl-rac-glycerol
十八碳二烯酸甘油三酯(TRANS-9,12)
A triacylglycerol
GC38871 XL-784 free base XL-784 free base 是 MMP 的一个选择性抑制剂，其对 MMP-1，MMP-3，MMP-8，MMP-9，MMP-13 的 IC50 值分别约为 1900，0.81，120，10.8，18，0.56 nM。
GC38859 Tetrahydrocortisone
四氢可的松
A metabolite of cortisol
GC38856 TD-0212 TFA TD-0212 TFA 是一种具有口服活性的、血管紧张素II型1受体AT1 和脑啡肽酶 (NEP)的双抑制剂，其对AT1的pKi值为 8.9，对NEP 的pIC50值为9.2。
GC38837 Prinomastat hydrochloride
AG3340 hydrochloride; KB-R9896 hydrochloride
An inhibitor of MMP-2, -3, -9, -13, and -14
GC38834 Phosphonoacetic acid
磷酰基乙酸
Phosphonoacetic acid (PAA) is an active endogenous metabolite that possesses a restricted potential to block DNA biosynthesis. Phosphonoacetic acid exhibits anti-viral activities.
GC38831 PF-00356231 hydrochloride PF-00356231 hydrochloride 是一种非肽、非锌螯合的基质金属蛋白酶 MMP-12 的配体和抑制剂 (IC50=1.4 μM)。它对 MMP-12 具有特异性并形成 PF-00356231/MMP-12 复合体。PF-00356231 hydrochloride 对 MMP-13、MMP-8、MMP-9、MMP-3 有抑制作用，IC50 分别为 0.00065、1.7、0.98、0.39 μM。
GC38818 Mirificin
芹糖葛根素苷; Puerarin apioside
Mirificin (Puerarin apioside) 是葛根中的异黄酮。Mirificin 抑制酪氨酸酶 (TYR)，IC50 为 12.66 μM。
GC38815 Methyl cinnamate
肉桂酸甲酯; Methyl 3-phenylpropenoate
Methyl cinnamate, an active component of Zanthoxylum armatum, is a widely used natural flavor compound with antimicrobial and tyrosinase inhibitor activities. Methyl Cinnamate Inhibits Adipocyte Differentiation via Activation of the CaMKK2--AMPK Pathway in 3T3-L1 Preadipocytes.
GC38812 MD-224 MD-224 是一种作用强大的MDM2蛋白降解剂，由Cereblon和MDM2配体组成，能够促使MDM2蛋白迅速降解。
GC38809 LHVS LHVS是一种有效的、非选择性的、不可逆的、可透过细胞的半胱氨酸蛋白酶和组织蛋白酶抑制剂，LHVS还可以抑制T. gondii（IC₅₀=10μM）侵袭。
GC38807 Lapaquistat acetate
TAK-475
Lapaquistat acetate (TAK-475) 是一种角鲨烯合酶 (squalene synthase) 抑制剂，可阻止法呢基二磷酸酯 (FPP) 转化为角鲨烯。Lapaquistat acetate (TAK-475) 最初旨在用于甲羟戊酸激酶缺乏症 (MKD)，可有效降低低密度脂蛋白胆固醇，但可能引起肝脏损害。
GC38782 gamma-secretase modulator 1 hydrochloride gamma-secretase inhibitior-1 是 γ-secretase 调节剂，可作用于阿尔茨海默病。
GC38779 Etilevodopa
左旋多巴乙酯,L-DOPA ethyl ester; Levodopa ethyl ester
Etilevodopa (L-Dopa ethyl ester) 是 Levodopa 的前药，在胃肠道中被非特异性酯酶快速水解为 Levodopa 和乙醇。Etilevodopa 用于治疗帕金森病 (PD)。Levodopa 是多巴胺的直接前体，是一种合适的前体药物，有助于中枢神经系统的渗透和传递多巴胺。
GC38768 Deserpidine
地舍平; Harmonyl
Deserpidine (Harmonyl), an alkaloid isolated from the roots of Rauwolfia canescens, is a competitive angiotensin converting enzyme (ACE) inhibitor, also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex.
GC38766 Delapril hydrochloride
地拉普利盐酸盐
Delapril Hydrochloride (Alindapril) is the hydrochloride salt form of delapril, which is a lipophilic, non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity.
GC38761 Cyclo(his-pro) TFA
Cyclo(histidyl-proline) TFA; Histidylproline diketopiperazine TFA
Cyclo(his-pro) TFA (Cyclo(histidyl-proline) TFA) 是一种具有口服活性的，结构上与促甲状腺激素释放激素相关的环状二肽。Cyclo(his-pro) TFA 可以抑制 NF-κB 核积累。Cyclo(his-pro) TFA 可以穿越脑血屏障并影响多种炎症和应激反应。
GC38734 Allotetrahydrocortisol
异体-3Α-四氢皮质醇,5a-Tetrahydrocortisol
Allotetrahydrocortisol (5a-Tetrahydrocortisol) 是一种皮质醇的代谢产物。Cortisol 是皮质醇是人体主要的糖皮质激素，在肾上腺皮质产生，在许多生理过程中起着至关重要的作用。
GC38729 2,5-Dimethylpyrazine
2,5-二甲基吡嗪,NSC 49139
2,5-Dimethylpyrazine (NSC 49139) is an endogenous metabolite.
GC38720 (R)-Trolox
(R)-(+)-6-羟基-2,5,7,8-四甲基色满-2-羧酸
(R)-Trolox 是水溶性维生素 E 类似物，是一种竞争性酪氨酸酶抑制剂，Ki 值为 0.83 mM，ID50 值为 1.88 mM。(R)-Trolox 具有比 (S) 对映异构体更强的酪氨酸酶亲和力 (Ki 值为 0.61 mM)。
GC45931 4(S),11(R)-DiHDoHE A neuropeptide with diverse biological activities
GC45926 Nelfinavir-d3 An internal standard for the quantification of nelfinavir
GC45909 17α-hydroxy Pregnenolone
17α-羟基妊娠烯醇酮,NSC 63853
A metabolite of pregnenolone
GC45818 Metoclopramide-d3
甲氧氯普安D3
An internal standard for the quantification of metoclopramide
GC45800 Cytarabine-13C3
Ara-C-13C3, 1-β-D-Arabinofuranosylcytosine-13C3
A neuropeptide with diverse biological activities
GC45768 Pranlukast-d4
ONO-1078-d4
A neuropeptide with diverse biological activities
GC45766 Amprenavir-d4
安瑞那韦 d4
A neuropeptide with diverse biological activities
GC45705 D-Kynurenine
犬尿氨酸
An antagonist of GPR109B
GC45687 Dasatinib N-oxide
达沙替尼N氧化物；达沙替尼杂质
A major metabolite of dasatinib
GC45673 7,8-Dihydroneopterin
7,8-二氢-D-新蝶呤
An antioxidant
GC45650 Des(benzylpyridyl) Atazanavir
Atazanavir metabolite M1
A metabolite of atazanavir
GC45615 3-hydroxy-3-methylglutaryl Coenzyme A (sodium salt)
DL-3-hydroxy-3-methylglutaryl-CoA, HMG-CoA, Hydroxymethylglutaryl-CoA
A neuropeptide with diverse biological activities
GC38703 NSC 8751
巴豆酸,(E)-2-Butenoic acid; (E)-Crotonic acid; trans-2-Butenoic acid; trans-Crotonic acid
NSC 8751 是一种内源性代谢产物。