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
GC13852 Calcitriol
骨化三醇; 1,25-Dihydroxyvitamin D3
骨化三醇作为类固醇激素维生素 D 的最具生物活性的代谢产物，抑制骨化三醇会导致抗癌药物的作用降低。
GC16205 D-Sorbitol
D-山梨醇
D-山梨醇（Sorbitol）是一种六碳糖醇，可用作糖的替代品。
GC12859 Cilazapril
西拉普利; Ro 31-2848
A prodrug form of cilazaprilat
GC11266 Lisinopril dihydrate
赖诺普利二水合物; MK-521 dihydrate
An ACE inhibitor
GC16296 MI-773
(2'R,3S,4'S,5'R)-6-氯-4'-(3-氯-2-氟苯基)-2'-(2,2-二甲基丙基)-1,2-二氢-N-(反式-4-羟基环己基)-2-氧代螺[3H-吲哚-3,3'-吡咯烷]-5'-甲酰胺
MI-773 是一种有效的 MDM2-p53 蛋白-蛋白相互作用 (PPI) 抑制剂，对 MDM2 具有高结合亲和力 (Kd=8.2 nM)。 MI-773 具有抗肿瘤活性。
GC16138 AHU-377 hemicalcium salt
LCZ696中间体,AHU-377 hemicalcium salt
A prodrug form of LBQ657
GC12751 Balicatib
巴利卡替; AAE581
A cathepsin K inhibitor
GC16279 Telotristat
LP778902
A TPH1 inhibitor
GC17456 NMDA (N-Methyl-D-aspartic acid)
N-甲基-D-天冬氨酸; N-Methyl-D-aspartic acid
An excitatory neurotransmitter
GC15771 PYR-41 An irreversible inhibitor of ubiquitin-activating enzyme
GC16990 Z-LEHD-FMK Z-LEHD-FMK 是一种选择性且不可逆的 caspase-9 抑制剂，可防止致命的再灌注损伤并减轻细胞凋亡。
GC12407 Z-IETD-FMK
CASPASE-8抑制剂,Benzyloxycarbonyl-Ile-Glu(OMe)-Thr-Asp(OMe)-fluoromethylketone, Z-Ile-Glu(OMe)-Thr-Asp(OMe)-FMK
Z-IETD-FMK（Z-IE(OMe)TD(OMe)-FMK）是一种选择性和细胞可渗透的 caspase-8抑制剂。
GC15770 Atglistatin An inhibitor of adipose triglyceride lipase
GC15828 AMG232
2-((3R,5R,6S)-5-(3-氯苯基)-6-(4-氯苯基)-1-((S)-1-(异丙基磺酰基)-3-甲基丁烷-2-基)-3-甲基-2-氧代哌啶-3-基)乙酸,AMG 232;AMG-232
An inhibitor of the MDM2 and p53 interaction
GC10140 Thrombin Receptor Agonist Peptide
凝血酶受体兴奋剂
A peptide agonist of the α-thrombin receptor
GC12895 Saxagliptin
沙格列汀; BMS-477118
A potent DPP-4 inhibitor
GC12391 Xanthohumol
黄腐醇

A natural prenylated chalcone
GC15577 Bestatin hydrochloride
盐酸乌苯美司; Ubenimex hydrochloride
Bestatin hydrochloride是氨基肽酶N（APN/CD13）抑制剂，其IC₅₀值为14.9±3.4μM。
GC12040 L-Kynurenine
L-犬尿氨酸
L-Kynurenine是L-色氨酸的代谢物，也是一种芳香烃受体 (aryl hydrocarbon receptor; AhR) 激动剂。
GC16215 GSK744 (S/GSK1265744)
卡博特韦; GSK-1265744; S/GSK1265744
An HIV-1 integrase inhibitor
GC17978 Vitamin D2 (Ergocalciferol)
维生素D2,Ergocalciferol; Calciferol; Ercalciol
A vitamin produced in fungi and invertebrates
GC13750 Doxycycline HCl
盐酸多西环素
Doxycycline HCl 是一种抗生素，是一种具有口服活性的广谱金属蛋白酶 (MMP) 抑制剂。
GC17252 Dextrose (D-glucose)
葡萄糖; Glucose; D-(+)-Glucose; Dextrose
A monosaccharide
GC11282 β-Estradiol
雌二醇; β-Estradiol; E2; 17β-Estradiol; 17β-Oestradiol

The major premenopausal estrogen
GC14385 Estrone
雌酮; E1; Oestrone
Estrone是三种主要的内源性雌激素之一，其他是雌二醇和雌三醇。
GC10582 Betacarotene
β-胡萝卜素; Provitamin A; beta-Carotene
Antioxidant, precursor of vitamin A
GC18147 Tretinoin (Aberela)
维生素A酸; Vitamin A acid; all-trans-Retinoic acid; ATRA

Tretinoin (Aberela) 是一种维生素 A 衍生的非肽类亲脂性小分子，可作为核 RA 受体 (RAR) 的配体，将其从转录抑制因子转化为激活因子 .在培养的人系膜细胞中，维甲酸 (Aberela) 以剂量和时间依赖性方式增加还原型谷胱甘肽含量和过氧化氢酶活性，从而阻止 H2O2 的细胞毒性。
GC17228 Thiabendazole
噻菌灵; 2-(4-Thiazolyl)benzimidazole
A broad-spectrum anthelmintic
GC10978 Terfenadine
特非那定; (±)-Terfenadine; MDL-991
A selective histamine H₁-receptor antagonist
GC12408 Progesterone
孕酮; Pregn-4-ene-3,20-dione
An endogenous hormone and hormone precursor
GC15180 BIBR-1048
达比加群酯; BIBR 1048
A prodrug form of dabigatran
GC17057 Lithocholic Acid
石胆酸; 3α-Hydroxy-5β-cholanic acid
A toxic secondary bile acid
GC17498 L-Glutamine
L-谷氨酰胺; L-Glutamic acid 5-amide
A conditionally essential amino acid
GC15095 Levodopa
左旋多巴; Levodopa; 3,4-Dihydroxyphenylalanine
A dopamine precursor
GC13078 Imidapril HCl
盐酸咪达普利; TA-6366
A prodrug form of imidaprilat
GC12148 Ethinyl Estradiol
乙炔基雌二醇; 17α-Ethynylestradiol; Ethynylestradiol
A 17β-estradiol analog
GC11242 Calcium Gluceptate
葡庚糖酸钙
葡萄糖酸钙是一种内源性代谢物。
GC11672 Argatroban
阿加曲班; MD-805; MCI-9038; Argipidine
A thrombin inhibitor
GC15322 Allopurinol
别嘌醇
Inhibitor of xanthine oxidase
GC11786 Acetylcysteine
乙酰半胱氨酸; N-Acetylcysteine; N-Acetyl-L-cysteine; NAC
乙酰半胱氨酸是半胱氨酸的 N-乙酰基衍生物。
GC10710 3-Methyladenine
3-甲基腺嘌呤; 3-MA
3-甲基腺嘌呤是一种经典的自噬抑制剂。
GC13441 Cyclopamine
环巴胺; 11-Deoxojervine
Cyclopamine是一种天然存在的Hedgehog (Hh)特异性小分子信号甾体生物碱抑制剂，对肿瘤生长具有深远的抑制作用，在人乳腺癌细胞中具有显著的抗侵袭、抗增殖和抗雌激素活性。
GC11908 Cisplatin
顺铂; cis-Platinum; CDDP; cis-Diaminodichloroplatinum
顺铂是最好的、最早的基于金属的化疗药物之一，用于治疗广泛的实体癌症，如睾丸癌、卵巢癌、膀胱癌、肺癌、宫颈癌、头颈部肿瘤和胃癌等。
GC12508 Nutlin-3b
4-[[(4R,5S)-4,5-双(4-氯苯基)-4,5-二氢-2-[4-甲氧基-2-(1-甲基乙氧基)苯基]-1H-咪唑-1-基]羰基]-2-哌嗪酮
The less active enantiomer of (–)-nutlin-3
GC12057 Daclatasvir (BMS-790052) An NS5A inhibitor
GC16014 Zileuton
齐留通; A 64077; Abbott 64077
A reversible inhibitor of 5-lipoxygenase
GC16319 Febuxostat
非布司他; TEI 6720; TMX 67
An inhibitor of the oxidized and reduced forms of xanthine oxidase
GC15166 Perindopril Erbumine
培哚普利叔丁胺; Perindopril tert-butylamine salt; S-9490 erbumine
An orally active ACE inhibitor
GC16388 Odanacatib (MK-0822)
奥当卡替; MK-0822
A potent, selective, and neutral inhibitor of cathepsin K
GC13044 17-DMAG (Alvespimycin) HCl
阿螺旋霉素盐酸盐; 17-DMAG hydrochloride; KOS-1022; BMS 826476
Water-soluble inhibitor of Hsp90