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
GC15764 Cilastatin sodium
西司他丁钠; MK0791 sodium
An inhibitor of dipeptidase (dehydropeptidase I)
GC17658 Guggulsterone
香胶甾酮; Z/E-Guggulsterone
Guggulsterone 是一种植物甾醇，来自于 Commiphora wightii 的树胶树脂。 Guggulsterone 通过下调抗凋亡基因产物（IAP1、xIAP、Bfl-1/A1、Bcl-2、cFLIP 和 survivin），调节细胞周期蛋白（cyclin D1 和c-Myc)，激活半胱天冬酶和 JNK，抑制 Akt。 Guggulsterone 是一种法尼醇 X 受体 (FXR) 拮抗剂，可降低 CDCA 诱导的 FXR 活化，对 Z- 和 E-Guggulsterone 的 IC50 分别为 17 和 15 μM。
GC12661 Indirubin-3'-oxime
靛玉红-3'-单肟,IDR3O; I3O
Inhibitor of GSK3β and cyclin-dependent kinases
GC16103 Oleylethanolamide
油酰单乙醇胺,N-Oleoylethanolamide; Oleamide MEA; Oleic acid monoethanolamide
An endogenous, potent agonist for PPARα
GC15239 Butabindide oxalate
[S-(R*,R*)]-1-(2-氨基-1-氧代丁基)-N-丁基-2,3-二氢-1H-吲哚-2-甲酰胺草酸盐,UCL-1397 oxalate
A potent inhibitor of CCK-inactivating peptidase/TPP-2
GC16553 N-Desmethylclozapine
N-去甲基氯氮平; Norclozapine; Desmethylclozapine; Normethylclozapine
An active metabolite of clozapine
GC17777 Palmitoylethanolamide
十六酰胺乙醇,Palmidrol; Loramine P 256
An endogenous cannabinoid
GC14042 Oleamide
油酸酰胺
An amide of oleic acid and agonist of CB₁ receptors
GC10318 Hexa-D-arginine
Furin Inhibitor II
A furin inhibitor
GC13077 RETF-4NA RETF-4NA 是一种糜酶特异性底物，当游离或与 α2M 结合时，它是一种敏感和选择性的糜酶底物。
GC16775 Rotenone
鱼藤酮
Rotenone是一种线粒体电子传递链复合物 I 抑制剂，可通过增强线粒体活性氧的产生来诱导细胞凋亡。
GC18105 Enterostatin
人肠抑素
A pentapeptide involved in the regulation of food intake
GC15108 Decanoyl-RVKR-CMK
Furin Inhibitor I
Decanoyl-RVKR-CMK 是一种枯草杆菌蛋白酶/Kex2p 样前蛋白转化酶抑制剂；阻断所有七种转化酶（PC1、PC2、PC4、PACE4、PC5、PC7 和弗林蛋白酶）的活性。
GC17642 JMV 390-1 JMV 390-1 (Compound 6a) 是一种有效的多肽酶抑制剂。
GC17117 CGS 35066 endothelin-converting enzyme (ECE) inhibitor
GC11236 [Leu5]-Enkephalin
亮氨酸脑啡肽,Leu-enkephalin; Leucine enkephalin; Leucyl-enkephalin
[Leu5]-Enkephalin 是一种具有吗啡样特性的五肽。
GC14064 p-Chlorophenylalanine
芬克洛宁; 4-Chloro-DL-phenylalanine; PCPA; CP-10188; DL-4-Chlorophenylalanine; 对氯苯丙氨酸
An inhibitor of tryptophan hydroxylase
GC14727 CCCP
羰基氰化氯苯腙,Carbonyl cyanide 3-chlorophenylhydrazone; Carbonyl Cyanide m-Chlorophenylhydrazone
Carbonylcyanide-3-chlorophenylhydrazone (CCCP) 是一种质子载体，可导致线粒体内膜中的质子梯度解偶联，从而抑制 ATP 合成速率。
GC12664 Urea
尿素; Carbamide; Carbonyldiamide
尿素是一种强大的蛋白质变性剂，通过直接和间接机制。
GC12203 L-Glutathione Reduced
还原型谷胱甘肽; GSH; γ-L-Glutamyl-L-cysteinyl-glycine

Nucleophilic co-substrate to glutathione transferases and electron donor to glutathione peroxidases
GC17937 2-MPPA
GPI-5693
2-MPPA (GPI-5693) 是一种具有口服活性的选择性谷氨酸羧肽酶 II (GCP II; PSMA) 抑制剂，IC50 为 90 nM。
GC13670 Methylmalonate
甲基丙二酸; Methylpropanedioic acid; Methylmalonate
A dicarboxylic acid and byproduct of propionate catabolism
GC10481 TRC 051384 TRC 051384 是一种热休克蛋白 70 (HSP70) 诱导剂。
GC13228 Phosphocreatine disodium salt
磷酸肌酸钠,Disodium creatine phosphate
磷酸肌酸二钠盐是一种称为 α 氨基酸和衍生物的有机化合物，是测定肌酸激酶的底物，用于在骨骼肌收缩过程中再生 ATP。
GC11459 Xanthurenic acid
4,8-二羟基喹啉-2-甲酸
Xanthurenic acid是一种内源性II组代谢型谷氨酸受体激动剂，参与丘脑的感觉传递。
GC12327 Corticosterone
皮质酮; 17-Deoxycortisol; 11β,21-Dihydroxyprogesterone; Kendall's compound B
Corticosterone (17 deoxycortisol) 是一种具有口服活性的糖皮质激素，由肾上腺皮质产生，对调节边缘系统（包括海马、前额叶皮层和杏仁核）的神经元功能具有重要作用。
GC14203 Citric acid
柠檬酸
柠檬酸是一种天然防腐剂和食品酸味增强剂。
GC17470 (-)-Cotinine
可替宁; (-)-Cotinine; (S)-Cotinine; NIH-10498
A major metabolite of nicotine
GC15042 Macbecin I
Macbecin I; NSC 330499
An Hsp90 inhibitor
GC11195 Sarcosine
肌氨酸; N-Methylglycine; Sarcosin
An intermediate in the biosynthesis of glycine
GC15975 α-Estradiol
α-雌二醇; Alfatradiol; Epiestradiol; Epiestrol
A weak estrogen with neuroprotective effects
GC12090 Nonactin
无活菌素; Ammonium ionophore I
A mixture of macrotetralide antibiotics that act as ionophores
GC15948 Prostaglandin E2
前列腺素 E2; PGE2; Dinoprostone
Prostaglandin E2是花生四烯酸在环氧合酶(COX)催化下产生的主要代谢物。
GC15649 Substance P
P物质; Neurokinin P
An endogenous NK₁ receptor agonist
GC11064 Spermine tetrahydrochloride
精胺四盐酸盐
A natural polyamine
GC16831 Agmatine sulfate
胍基丁胺；硫酸胍基丁胺；硫酸鲱精胺；胍基丁胺硫酸盐
A polyamine metabolite
GC17591 D-erythro-Sphingosine (synthetic)
鞘氨醇; Erythrosphingosine; erythro-C18-Sphingosine; trans-4-Sphingenine
D-erythro-sphingosine (Erythrosphingosine) 是一种非常有效的 p32 激酶激活剂，EC50 值为 8μM。
GC13890 (±)-Palmitoylcarnitine chloride
C16:0 Carnitine, CAR 16:0, DL-Carnitine hexadecanoyl ester, DL-Carnitine palmitoyl ester, Hexadecanoyl-DL-carnitine, DL-Hexadecanoylcarnitine, NSC 628323, DL-Palmitoylcarnitine
A long-chain acylcarnitine with intracellular and extracellular roles
GC14301 Spaglumic acid
异冬谷酸,N-Acetylaspartylglutamic acid
A peptide neurotransmitter
GC10123 O-Phospho-L-serine
L-O-磷酸丝氨酸,L-Serine O-phosphate; L-SOP
A glutamate receptor agonist
GC14547 Quinolinic acid
喹啉酸
An excitotoxic agonist at NMDA receptors
GC17823 L-Cysteinesulfinic acid
L-半胱氨酸亚磺酸
L-半胱氨酸亚磺酸是几种大鼠代谢型谷氨酸受体 (mGluR) 的有效激动剂，对 mGluR1、mGluR5、mGluR2、mGluR4、mGluR6 和 mGluR8 的 pEC50 分别为 3.92、4.6、3.9、2.7、4.0 和 3.94 .
GC14943 Hypotaurine
亚牛磺酸; 2-Aminoethanesulfinic acid
An endogenous inhibitory amino acid and antioxidant
GC10897 2'-Deoxyguanosine
2′-脱氧鸟苷; Deoxyguanosine; Guanine deoxyriboside
2'-脱氧鸟苷（Deoxyguanosine）由嘌呤核苷鸟嘌呤通过其N9氮与脱氧核糖的C1碳相连。
GC12344 TAPI-1
TAPI
A TACE inhibitor
GC12647 NVP-CGM097
CGM097
An inhibitor of the MDM2-p53 interaction
GC13851 GW311616 hydrochloride
GW311616A
An inhibitor of neutrophil elastase
GC11615 GW311616 GW-311616 是一种有效的、可口服的、长效的、选择性的人中性粒细胞弹性蛋白酶 (HNE) 抑制剂，IC50 值为 22 nM，Ki 值为 0.31 nM。
GC14851 Vidofludimus
维多氟拉迪莫,4sc-101; SC12267
An immunosuppressive drug that inhibits DHODH
GC10018 Talabostat mesylate
[(2R)-1-[(2S)-2-氨基-3-甲基丁酰基]吡咯烷-2-基]硼酸甲磺酸盐,Val-boroPro mesylate; PT100 mesylate
Talabostat (PT100)是一种口服活性和非选择性二肽基肽酶IV（DPP-IV）抑制剂(IC50 < 4 nM; Ki = 0.18 nM)和成纤维细胞活化蛋白(FAP)的第一种临床抑制剂(IC50 = 560 nM)，抑制DPP 8/9(IC50= 4/11 nM; Ki = 1.5/0.76 nM)，静止细胞脯氨酸二肽酶(QPP)( IC50= 310 nM)，DPP 2和其他一些DASH家族酶。