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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. GC68710 AXKO-0046 dihydrochloride AXKO-0046 dihydrochloride,吲哚衍生物,是 LDHB 选择性抑制剂。AXKO-0046 dihydrochloride 具有 LDHB 抑制活性,EC50 值为 42 nM。AXKO-0046 dihydrochloride 可用于癌症代谢的研究。
  3. GC68703 AT-533 AT-533 是一种有效的 Hsp90 和 HSV 抑制剂。AT-533 通过阻断 HIF-1α/VEGF/VEGFR-2 信号通路抑制肿瘤生长和血管生成。AT-533 还抑制下游通路的激活,包括 Akt/mTOR/p70S6K, Erk1/2 和 FAK。AT-533 抑制人脐静脉内皮细胞 (HUVEC) 的管形成、细胞迁移和侵袭。
  4. GC68656 Andecaliximab Andecaliximab 是一种靶向基质金属蛋白酶 9 (MMP9) 的重组 IgG4 单克隆抗体。Andecaliximab 在特发性肺纤维化小鼠模型中显示出抗纤维化疗效。Andecaliximab 可用于胃腺癌和特发性肺纤维化 (IPF) 的研究。
  5. GC68641 ALOX15-IN-1 ALOX15-IN-1 (compound 8b) 是一种有效且选择性的兔和人 ALOX15 亚油酸加氧酶 (linoleate oxygenase) 活性抑制剂,对 ALOX15 直系同源物亚油酸 (LA) 和花生四烯酸 (AA) 的 IC50 分别为 0.04 和 2.06 μM。
  6. GC68635 ALDH3A1-IN-1 ALDH3A1-IN-1 (Compound 18) 是一种有效的 ALDH3A1 抑制剂,IC50 为 1.61 μM。ALDH3A1-IN-1 作为单药或与多西紫杉醇联合研究,对患者来源的原发性前列腺肿瘤上皮细胞比 DEAB 更有效。
  7. GC68621 Ac-WEHD-AFC TFA Ac-WEHD-AFC TFA 是一种荧光 caspase-1 底物。Ac-WEHD-AFC TFA 可检测 caspase-1 荧光活性,用于肿瘤和炎症的研究。
  8. GC68620 Ac-VLPE-FMK Ac-VLPE-FMK 是一种四肽基单氟甲基酮 (m-FMK),是一种 Cat-B 和 Cat-L 抑制剂。Ac-VLPE-FMK 可用于癌症侵袭性研究。
  9. GC68603 Acetyl-CoA Carboxylase-IN-1 Acetyl-CoA Carboxylase-IN-1 是一种有效的乙酰辅酶 A 羧化酶 (ACC) 抑制剂,IC50 值为 <5 nM。 Acetyl-CoA Carboxylase-IN-1 具有抗菌活性。
  10. GC68600 Ac-DEVD-CMK TFA Ac-DEVD-CMK (Caspase-3 Inhibitor III) TFA 是一种选择性且不可逆的 caspase-3 抑制剂。Ac-DEVD-CMK TFA 显着抑制由高水平葡萄糖或 3,20-dibenzoate (IDB; 5) 诱导的凋亡。Ac-DEVD-CMK TFA 可以用于多种实验方法以抑制细胞凋亡。
  11. GC68598 Ac-Ala-OH-d3 Ac-Ala-OH-d3 是 Ac-Ala-OH 氘代物。Ac-Ala-OH 是一种内源性代谢产物。
  12. GC68587 A-908292 A-908292 是一种有效和选择性的乙酰辅酶 A 羧化酶 2 (ACC2) 抑制剂,抑制 hACC2 的 IC50 值为 23 nM。A-908292 可用于脂肪酸代谢的研究。
  13. GC68578 7-Methoxy obtusifolin 7-Methoxy obtusifolin (Compound 4) 是一种竞争性 tyrosinase 抑制剂,IC50 为 7.0 μM。
  14. GC68550 4-Hydroxybenzoic acid-d4 4-Hydroxybenzoic acid-d4 是 4-Hydroxybenzoic acid 的氘代物。4-Hydroxybenzoic acid 是苯甲酸的酚衍生物,可以抑制绝大多数的革兰氏阳性菌和部分革兰氏阴性菌,其 IC50 值为160 μg/mL。
  15. GC68540 3-Methyl-L-histidine-d3 3-Methyl-L-histidine-d3 是 3-Methyl-L-histidine 的氘代物。3-Methyl-L-histidine 能够作为肉类尤其是鸡肉摄入,以及大豆制品摄入的生物标记。
  16. GC68536 3-Indolepropionic acid-d2 3-Indolepropionic acid-d2 是 3-Indolepropionic acid 的氘代物。3-Indolepropionic acid 是一个强效的抗氧化剂,有研究阿尔兹海默症的潜能。
  17. GC68519 2-Hydroxyisobutyric acid-d6 2-Hydroxyisobutyric acid-d6 是 2-Hydroxyisobutyric acid 的氘代物。2-Hydroxyisobutyric acid 是一种内源性代谢产物。
  18. GC68509 (25R)-12α-Hydroxyspirost-4-en-3-one (25R)-12α-Hydroxyspirost-4-en-3-one 是由 Nocardia globerula 作用于 Hecogenin 产生的一种次要代谢物。
  19. GC68504 2-(2-Methylbenzamido)acetic acid-d7 2-(2-Methylbenzamido)acetic acid-d7 是 2-(2-Methylbenzamido)acetic acid 的氘代物。2-(2-Methylbenzamido)acetic acid 为一种代谢物,可以在尿液中检测到。
  20. GC68502 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine 1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine 可以选择作为用于研究氧化磷脂酰胆碱分子种类的挥发性化合物的模型。这个方法应用于实际食品样品,即大豆卵磷脂。
  21. GC68501 1-Palmitoyl-2-oleoyl-sn-glycerol 1-Palmitoyl-2-oleoyl-sn-glycerol 是一种内源性代谢物,也是藻殖段诱导因子 (HIF)-1 中主要的二酰基甘油。
  22. GC68496 1-Hexadecanol-d5 1-Hexadecanol-d5 是 1-Hexadecanol 的氘代物。 1-Hexadecanol 是脂肪醇,一种亲脂性底物。
  23. GC68495 1-Hexadecanol-d4 1-Hexadecanol-d4 是 1-Hexadecanol 的氘代物。 1-Hexadecanol 是脂肪醇,一种亲脂性底物。
  24. GC68486 1,4-Diaminobutane-d8 dihydrochloride 1,4-Diaminobutane-d8 (dihydrochloride) 是 1,4-Diaminobutane dihydrochloride 的氘代物。 1,4-Diaminobutane (Putrescine) dihydrochloride 是一种内源性代谢物,能作为高等植物大麦和油菜受 Cr (III) 或 Cr (VI) 胁迫引起污染的指标。
  25. GP26352 THBD Human THBD Human Recombinant produced in Sf9 Baculovirus cells is a single, glycosylated polypeptide chain containing 500 amino acids (22-515a
  26. GP26168 MMP9 Mouse MMP9 Mouse produced in Sf9 Insect cells is a single, glycosylated polypeptide chain containing 711 amino acids (20-730 a
  27. GP26167 MMP2 Mouse MMP2 Mouse produced in Sf9 Baculovirus cells is a single, glycosylated polypeptide chain containing 644 amino acids (30-662 aa) and having a molecular mass of 72
  28. GP26143 CTSZ Mouse, Active CTSZ Mouse Recombinant produced in Baculovirus is a single, glycosylated, polypeptide chain containing 292 amino acids (23-306 aa) and having a molecular mass of32
  29. GP26142 CTSF Human, Sf9 CTSF produced in Sf9 Baculovirus cells is a single, glycosylated polypeptide chain containing 474 amino acids (20-484
  30. GC26092 Z-LEHD-FMK TFA Z-LEHD-FMK TFA (Caspase-9 Inhibitor) is a cell-permeable, competitive and irreversible inhibitor of enzyme caspase-9, which helps in cell survival.
  31. GC26017 UK-371804 HCl UK-371804 is a potent and selective urokinase-type plasmogen activator (uPA) inhibitor with excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin).
  32. GC25727 PF-06446846 PF-06446846 is an orally active proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor. PF-06446846 selectively inhibits translation of PCSK9 by stalling the 80S ribosome in the proximity of codon region.
  33. GC25726 PF-05221304 PF-05221304 is an orally bioavailable, liver-targeted inhibitor of acetyl-CoA carboxylase (ACC), an enzyme that catalyzes the first committed step in de novo lipogenesis (DNL).
  34. GC25723 Perindopril L-Arginine Perindopril L-Argininel is a prodrug that is metabolized in the liver to its active diacid metabolite perindoprilat, which is rapidly and extensively absorbed, and become one of the highest tissue angiotensin-converting enzyme (ACE) affinities among the ACE inhibitors.
  35. GC25536 JHU395 JHU395 is a novel orally bioavailable GA (glutamine antagonists) prodrug designed to circulate inert in plasma, but permeate and release active GA within target tissues. JHU395 delivers active GA to malignant peripheral nerve sheath tumor (MPNST), and significantly inhibits tumor growth without observed toxicity.
  36. GC25337 D-Carnitine hydrochloride D-Carnitine hydrochloride ((S)-Carnitine hydrochloride, (+)-Carnitine hydrochloride) is biosynthesized from lysine. It might be associated with the energy production from branched chain amino acids.
  37. GC25188 Calcium 2-oxoglutarate Calcium 2-oxoglutarate (Calcium oxoglurate, Calcium 2-oxopentanedioate, Calcium α-ketoglutarate, Calcium AKG, Calcium 2-ketoglutaric acid, Calcium oxoglutaric acid) is the Calcium salt form of 2-oxoglutarate. 2-oxoglutarate is naturally found in organisms and is a well-known intermediate in the production of ATP or GTP in the Krebs cycle. 2-oxoglutarate is a reversible inhibitor of tyrosinase with IC50 of 15 mM.
  38. GC25117 Azvudine Azvudine (RO-0622) is a novel nucleoside reverse transcriptase inhibitor with antiviral activity against human immunodeficiency virus (HIV), hepatitis B virus (HBV) and hepatitis C virus (HCV), potently inhibits HIV-1 (EC50 range 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM).
  39. GC68478 Bictegravir sodium Bictegravir sodium 是一种有效的 HIV-1 整合酶抑制剂,其 IC50 值为 7.5 nM。Bictegravir sodium 表现出强大的选择性的抗 HIV 活性和低的细胞毒性。
  40. GC68468 MPO-IN-3 MPO-IN-3 是一种有效的 myeloperoxidase 抑制剂 (WO2013068875A1, example 191)。髓过氧化物酶 (MPO) 是一种含血红素的酶,属于过氧化物酶超家族。
  41. GC68464 ALDH1A3-IN-1 ALDH1A3-IN-1 (Compound 14) 是一个有效的 ALDH1A3 抑制剂,其 IC50 值为 0.63 µM,Ki 值为 0.46 µM。ALDH1A3-IN-1 能被用于研究前列腺癌 (prostate cancer)。
  42. GC68462 ALDH1A3-IN-2 ALDH1A3-IN-2 (Compound 15) 是一种有效的 ALDH1A3 抑制剂,IC50 为 0.30 μM。醛脱氢酶 (ALDH) 在包括前列腺癌在内的各种肿瘤类型中过度表达。ALDH1A3-IN-2 具有研究癌症疾病的潜力。
  43. GC68453 ITMN 4077 ITMN 4077 是一种大环类抑制剂,可抑制丙型肝炎病毒 (HCV) NS3 蛋白酶活性 (EC50: 2131 nM)。
  44. GC68450 Hsp90-IN-17 hydrochloride Hsp90-IN-17 (Example 5) hydrochloride 是一种 HSP90 抑制剂,可用于增殖性疾病,例如癌症和神经退行性疾病的研究。
  45. GC68426 17a-Hydroxypregnenolone-d3 17a-Hydroxypregnenolone-d3 是 17a-Hydroxypregnenolone 的氘代物。17a-Hydroxypregnenolone 是一种孕烷类固醇, 是形成脱氢表雄酮 (DHEA) 的一种激素原。
  46. GC68421 L-Aspartic acid-13C4,15N L-Aspartic acid-13C4,15N 是一种 13C 和 15N 标记的 L-Aspartic acid。L-Aspartic acid 是一种氨基酸,被证明是一种结肠特异性药物输送的前体药物。
  47. GC68417 Homovanillic acid-d5 Homovanillic acid-d5 (Vanilacetic acid-d5) 是 Homovanillic acid 的氘代物。Homovanillic acid 是一种多巴胺代谢物,它与芳香族氨基酸脱羧酶缺乏症、乳糜泻、生长激素缺乏以及脂联素还原酶缺乏症相关。
  48. GC68415 Glycolic acid-d2 Glycolic acid-d2 是 Glycolic acid 的氘代物。Glycolic acid 是酪氨酸酶 (tyrosinase) 的抑制剂,能抑制黑色素的形成,从而减淡皮肤的颜色。
  49. GC68414 (Rac)-Atropine-d3 (Rac)-Atropine-d3 是 (Rac)-Atropine 的氘代物。
  50. GC68399 Isolindleyin Isolindleyin 是一种丁酰苯,是酪氨酸酶抑制剂,对人酪氨酸酶的 Kd 值为 54.8 μM。Isolindleyin 具有抗炎和抗黑色素生成活性,可用于缓解疼痛的研究。
  51. GC68395 L-Isoleucine-d10 L-Isoleucine-d10 是 L-Isoleucine 的氘代物。L-Isoleucine 是一种非极性疏水性氨基酸。L-Isoleucine 是一种必需氨基酸。

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