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Home >> Signaling Pathways >> Proteases

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

  1. Cat.No. 产品名称 Information
  2. GC46041 1,2,3-Trilinoleoyl-rac-glycerol

    甘油三亚油酸酯

     A triacylglycerol
  3. GC39185 Pregnanediol

    孕二醇; NSC 1612; NSC 47462

     Pregnanediol 是一种内源性代谢产物。
  4. GC39173 Phosphorylcholine chloride calcium salt tetrahydrate

    胆碱磷酸氯化钙四水

     Phosphocholine (Phosphorylcholine) chloride calcium salt tetrahydrate is an active endogenous metabolite.
  5. GC39169 CC-92480

    CC-92480

     A modulator of cereblon
  6. GC39157 DS-1001b An inhibitor of mutant IDH1
  7. GC39134 Isofraxidin

    异嗪皮啶

     Isofraxidin (6,8-Dimethoxyumbelliferone), a bioactive coumarin compound isolated from the functional foods Siberian ginseng and Apium graveolens, is an anti-bacterial, anti-oxidant, and anti-inflammatory agent.
  8. GC39119 Isonicotinic acid

    异烟酸

     Isonicotinic acid (Isoniazid, 4-pyridinecarboxylic acid, p-pyridinecarboxylic acid, 4-Picolinic acid) is a metabolite of isoniazid. It is an isomer of nicotinic acid.
  9. GC39115 Terpinen-4-ol

    4-萜烯醇; 4-Carvomenthenol

     Terpinen-4-ol, a naturally occurring monoterpene, is the main bioactive component of tea-tree oil and has been shown to have many biological activities such as antifungal properties.
  10. GC39095 Isoliquiritin apioside

    芹糖异甘草苷

     Isoliquiritin apioside (ISLA, ILA), a component isolated from Glycyrrhizae radix rhizome (GR), significantly decreases PMA-induced increases in matrix metalloproteinase (MMP) activities and suppresses PMA-induced activation of mitogen-activated protein kinase (MAPK) and NF-κB. Isoliquiritin apioside possesses anti-metastatic and anti-angiogenic abilities in malignant cancer cells and ECs, with no cytotoxicity.
  11. GC39068 Rosamultin

    罗莎白素

     Rosamultin is a 19 α-hydroxyursane-type triterpenoid isolated from Potentilla anserina L. that inhibits HIV-1 protease. Rosamultin has protective effects on H2O2-induced oxidative damage and apoptosis.
  12. GC39050 Prudomestin

    3,5,7-三羟基-8,4'-二甲氧基黄酮

     Prudomestin，从 Prunus domestica 心材中分离得到，具有很强的黄嘌呤氧化酶 (XO) 抑制活性(IC50≈6?µM)。
  13. GC39013 FPL 62064

    N-(4-甲氧苯基)-1-苯基-1H-吡唑-3-胺

     FPL 62064 is a potent dual inhibitor of 5-lipoxygenase (5-LOX) and prostaglandin synthetase (cyclooxygenase, COX) with IC50 of 3.5 μM and 3.1 μM for RBL-1 cytosolic 5-lipoxygenase and seminal vesicle prostaglandin synthetase, respectively. FPL 62064 has potent anti-inflammatory activity.
  14. GC38971 Toddalolactone

    毛两面针素

     Toddalolactone, a natural coumarin, inhibits the activity of recombinant human Plasminogen activator inhibitor-1 (PAI-1) in a dose-dependent manner, yielding an IC50 value of 37.31 ± 3.23 μM.
  15. GC38958 Sorbic acid

    山梨酸

     Sorbic acid (2,4-Hexadienoic acid) is a naturally occurring compound that originated from the unripe berries of the Rowan Tree. It inhibits various bacteria, including sporeformers, at various stages of their life cycle (germination, outgrowth and cell division).
  16. GC38931 N-Desmethyltamoxifen hydrochloride

    N-去甲基三苯氧胺盐酸盐

     N-Desmethyltamoxifen hydrochloride (N-Desmethyl tamoxifen HCl), the primary metabolite of tamoxifen, is an estrogen response modifer and protein kinase C inhibitor with IC50 of 25 ?M.
  17. 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。
  18. 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.
  19. 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。
  20. GC38903 Deslanoside

    去乙酰西地兰; Deacetyllanatoside C; Desacetyllanatoside C

     A cardiac glycoside
  21. 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.
  22. 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。
  23. 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。
  24. GC38881 10,12-Tricosadiynoic acid

    10,12-二十三联炔酸

     10,12-Tricosadiynoic acid 是一种高特异性，选择性，高亲和力且具有口服活性的酰基辅酶 A 氧化酶-1 (ACOX1) 抑制剂。10,12-Tricosadiynoic acid 可通过改善线粒体脂质和 ROS 代谢来治疗高脂饮食或肥胖引起的代谢性疾病。
  25. GC46026 TMI 1

    WAY-171318

     An ADAM and MMP inhibitor
  26. GC46023 Phenylpyropene A

    苯基吡喃菌素A

     A fungal metabolite
  27. GC46002 Prunetin

    樱黄素

     An isoflavone with diverse biological activities
  28. GC45994 Hydrocortisone Acetate

    Cortef Acetate, Hydrin 2, Hydrocortisone 21-Acetate, Hydroxycorticosterone Acetate, 17α-Hydroxycorticosterone Acetate, Isopto-Hydrocortisone

     A synthetic corticosteroid
  29. GC45978 1,10-Phenanthroline (hydrate)

    邻菲罗啉,1,10-Phenanthroline monohydrate

     A metal chelator and inhibitor of metalloproteases
  30. GC45969 6β-hydroxy Eplerenone

    依普利酮6-BETA-羟基类似物

     A major metabolite of eplerenone
  31. GC45962 12-hydroxy Lauric Acid

    端羟基12酸

     A hydroxylated fatty acid
  32. GC45960 9c(i472)

    15-LOX-1 Inhibitor i472

     A 15-LO-1 inhibitor
  33. GC45951 BLX3887

    15-LO-1 Inhibitor 3887

     A 15-LO-1 inhibitor
  34. GC45948 1,2,3-Trilinoelaidoyl-rac-glycerol

    十八碳二烯酸甘油三酯(TRANS-9,12)

     A triacylglycerol
  35. 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。
  36. GC38859 Tetrahydrocortisone

    四氢可的松

     A metabolite of cortisol
  37. 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。
  38. GC38837 Prinomastat hydrochloride

    AG3340 hydrochloride; KB-R9896 hydrochloride

     An inhibitor of MMP-2, -3, -9, -13, and -14
  39. 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.
  40. 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。
  41. 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。
  42. 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.
  43. GC38812 MD-224 MD-224 是基于蛋白水解定位嵌合体 (PROTAC) 的高效小分子 (MDM2) 降解物。MD-224 在人白血病细胞中，诱导 MDM2 的快速降解 (<1 nM)，抑制 RS4;11 细胞生长的 IC50 值为 1.5 nM。MD-224 有可能成为一类新的抗癌剂。
  44. GC38809 LHVS LHVS 是有效的，非选择性的 cysteine protease 抑制剂，LHVS 有效阻断 T. gondii 微素蛋白分泌 (IC50=10 μM)，滑动运动和细胞侵袭。
  45. 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。
  46. 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。
  47. 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。
  48. 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.
  49. 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.
  50. 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。
  51. 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。

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