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
GC10794 BMS-626529
1-(4-苯甲酰基哌嗪-1-基)-2-[4-甲氧基-7-(3-甲基-1H-1,2,4-三氮唑-1-基)-1H-吡咯并[2,3-C]吡啶-3-基)乙烷-1,2-二酮,BMS 626529;BMS626529
An HIV-1 attachment inhibitor
GC10448 Bivalirudin Trifluoroacetate
比伐卢定,Bivalirudin
A thrombin inhibitor
GC10930 Balapiravir
4'-C-迭氮基胞嘧啶核苷2',3',5'-三异丁酸酯,R-1626; R1626; Ro 4588161;R1626;Ro4588161;Ro-4588161
Balapiravir (Ro 4588161; R1626) 是 HCV (R1479; 4'-Azidocytidine) 的 RNA 依赖性 RNA 聚合酶 (RdRp) 的核苷类似物抑制剂的口服活性前药。
GC11475 AZD7687
[反式-4-[4-(6-氨基甲酰基-3,5-二甲基吡嗪-2-基)苯基]环己基]乙酸,AZD 7687; AZD-7687
AZD7687 是一种有效的、选择性的、可逆的和具有口服活性的 diacylglycerol acyltransferase 1 (DGAT1) 抑制剂，对人 DGAT1 的 IC50 为 80 nM。
GC14458 Asunaprevir (BMS-650032)
阿那匹韦,BMS-650032;BMS 650032;BMS650032,Asunaprevir
An HCV NS3/4A protease inhibitor
GC14937 Anguizole
7-(氯二氟甲基)-5-(2-呋喃基)-N-(2-噻吩基甲基)吡唑并[1,5-A]嘧啶-2-甲酰胺,7-[chloro(difluoro)methyl]-5-(furan-2-yl)-N-(thiophen-2-ylmethyl)pyrazolo[1,5-a]pyrimidine-2-carboxamide
Anguizole 是一种 HCV 复制的小分子抑制剂，可改变 NS4B 的亚细胞分布。
GC13949 Alogliptin Benzoate
苯甲酸阿格列汀; SYR 322
A DPP-4 inhibitor
GC14757 AGI-6780
AGI 6780;AGI6780
A potent, selective inhibitor of mutant IDH2
GC11101 5-R-Rivaroxaban
5-R-利伐沙班
5-R-Rivaroxaban 是 Rivaroxaban 的 (R)-对映异构体。
GC17566 24, 25-Dihydroxy VD3
24,25-二羟基维生素 D3
24, 25-二羟基VD3是一种与1,25-二羟基维生素D3密切相关的化合物，是维生素D3的活性形式。
GC17210 17-AAG Hydrochloride
Tanespimycin Hydrochloride;NSC 330507 Hydrochloride;CP 127374 Hydrochloride;17AAG Hydrochloride;17 AAG Hydrochloride
Hsp90 inhibitor,geldanamycin analogue
GC16892 XL-888
Xl 888, Xl888
An orally bioavailable Hsp90 inhibitor
GC16966 VER 155008
adenosine-derived inhibitor, VER155008, VER-155008
An Hsp70 inhibitor
GC13885 Elesclomol (STA-4783)
伊利司莫; STA-4783
Elesclomol（也称为 STA-4783）最初是在基于细胞的表型筛选中发现的促凋亡活性，是一种新型小分子，可通过快速产生活性氧 (ROS) 有效诱导癌细胞凋亡以及难以控制的氧化应激水平的诱导。
GC17655 Ganetespib (STA-9090)
STA9090, STA 9090
Ganetespib (STA-9090) (STA-9090) 是一种热休克蛋白 90 (HSP90) 抑制剂，在多种血液和实体肿瘤细胞系中表现出强效细胞毒性。 Ganetespib (STA-9090) 通过抑制 HIF-1α 在结直肠癌中具有抗血管生成作用；和 STAT3。
GC15274 PF-04620110
PF 04620110,PF04620110
A potent, bioavailable inhibitor of DGAT-1
GC15614 A922500
DGAT-1抑制剂,A-922500, A 922500
A diacylglycerol acyltransferase 1 inhibitor
GC10330 Lonafarnib
洛那法尼,Sch 66336, Sch66336, Sch-66336
A farnesyltransferase inhibitor with antitumor activity
GC10406 Tosedostat (CHR2797)
托舍多特,CHR-2797
An aminopeptidase inhibitor
GC13130 Apixaban
阿哌沙班; BMS-562247-01
An inhibitor of Factor Xa
GC10531 AGI-5198
AGI5198, AGI 5198
A potent, selective inhibitor of IDH1 mutations
GC15382 Isotretinoin
异维A酸; 13-cis-Retinoic acid
A retinoid
GC10999 Avasimibe
阿伐麦布,CI-1011; PD-148515
Avasimibe是一种选择性口服酰基辅酶A：胆固醇酰基转移酶（ACAT）抑制剂（IC₅₀=12μmol/L）。
GC12653 LY3039478
LY3039478
A Notch inhibitor
GC12117 JNJ-26854165 (Serdemetan)
N-[2-(1H-吲哚-3-基)乙基]-N'-(4-吡啶基)-1,4-苯二胺,JNJ 26854165
An antagonist of MDM2 action
GC16051 Nutlin-3
4-[[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,Nutlin 3,MDM2 Antagonist
A racemic mixture of (?)-nutlin-3 and (+)-nutlin-3
GC15442 Tipifarnib (Zarnestra)
替吡法尼; IND 58359; R115777
A farnesyltransferase inhibitor with antitumor activity
GC13456 Doxycycline hyclate
多西环素盐酸盐半乙醇半水合物; Doxycycline hydrochloride hemiethanolate hemihydrate; WC2031
Doxycycline hyclate是四环素的衍生物，具有抗炎和抗菌活性。
GC14210 NSC 405020
NSC-405020

NSC 405020是一种特异性膜基质金属蛋白酶（MT1-MMP）小分子抑制剂。
GC14523 GM 6001
伊洛马司他; GM6001; Galardin
GM 6001 是一种广谱 MMP 抑制剂，可用于癌症和神经退行性疾病的研究，GM 6001对 MMP-1、2、3、8 和 9 的 Ki 值分别为 0.4、0.5、27、0.1和 0.2 nM。
GC14099 Marimastat
马立马司他; BB2516; TA2516
A broad-spectrum inhibitor of MMPs and TACE
GC14152 Amprenavir (agenerase)
安瑞那韦; VX-478
A selective HIV protease inhibitor
GC16602 Darunavir
达芦那韦; TMC114; UIC-94017
An HIV-1 protease inhibitor
GC17303 Ritonavir
利托那韦; ABT 538; RTV
An HIV protease inhibitor
GC10240 Atazanavir sulfate (BMS-232632-05)
硫酸阿扎那韦; BMS-232632 sulfate
An inhibitor of HIV-1 protease
GC12945 Atazanavir
阿扎那韦; BMS-232632

An inhibitor of HIV-1 protease
GC15130 Alogliptin (SYR-322)
阿格列汀; SYR-322 free base
Alogliptin (SYR-322) (SYR-322 free base) 是一种有效的、选择性的、具有口服活性的 DPP-4 抑制剂，IC50 <10 nM，选择性比 DPP-8 和 DPP-9 高 10,000 倍以上.
GC16733 Vildagliptin (LAF-237)
维格列汀; LAF237; NVP-LAF 237
A DPP-4 inhibitor
GC10298 Sitagliptin phosphate monohydrate
西他列汀磷酸盐一水合物; MK-0431 phosphate monohydrate
Sitagliptin phosphate monohydrate (MK-0431 phosphate monohydrate) 是一种有效的 DPP4 抑制剂，在 Caco-2 细胞提取物中的 IC50 为 19 nM。
GC14827 Linagliptin (BI-1356)
利格列汀; BI 1356
A potent DPP-4 inhibitor
GC10104 Glimepiride
格列美脲; Glimperide; HOE-490
An antidiabetic sulfonylurea
GC10832 VX-222 (VCH-222, Lomibuvir)
Lomibuvir, VCH222,VCH-222, VX222
An HCV polymerase inhibitor
GC12299 Telaprevir (VX-950)
特拉匹韦; VX-950
An HCV NS3/4A protease inhibitor
GC12879 Danoprevir (RG7227)
丹诺普韦; ITMN-191; R7227; RO5190591; RG7227
An HCV NS3/4A protease inhibitor
GC15084 2-Methoxyestradiol (2-MeOE2)
二甲氧基雌二醇; 2-ME2; NSC-659853
2-Methoxyestradiol (2-MeOE2/2-Me)是一种HIF-1α抑制剂。
GC16752 Olmesartan medoxomil
奥美沙坦酯; CS 866
A prodrug form of olmesartan
GC16223 Captopril
卡托普利; SQ 14225
An ACE inhibitor
GC16293 BIBR 953 (Dabigatran, Pradaxa)
达比加群; BIBR 953; BIBR 953ZW
A thrombin inhibitor
GC17906 S/GSK1349572
度鲁特韦; S/GSK1349572
A potent inhibitor of HIV integrase
GC11956 Raltegravir (MK-0518)
雷特格韦; MK-0518
Raltegravir (MK-0518) 是一种有效的整合酶 (IN) 抑制剂，用于治疗 HIV 感染。