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29

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T80052	Cathepsin B
	Cathepsin B为一种半胱氨酸蛋白酶，涉及多种程序性细胞死亡（包括细胞凋亡、焦亡、铁亡、坏死亡及自噬性细胞死亡）。
T3420	CA-074 methyl ester Cathepsin B Inhibitor IV,CA-074Me	Cysteine Protease	Proteases/Proteasome
	CA-074 methyl ester (Cathepsin B Inhibitor IV) 是Cathepsin B 的选择性抑制剂，具有保护神经、抗炎、抗癌等多种作用。
T27989	MDK0734 Cathepsin B Inhinitor-42
	MDK0734 is a selective inhibitor of cathepsin B endopeptidase and exopeptidase activities.
T28003	MDK7677 Cathepsin B Inhinitor-17,MDK 7677
	MDK7677 is a selective inhibitor of cathepsin B endopeptidase and exopeptidase activities.
T10924	Cysteine protease inhibitor-2	Cysteine Protease	Proteases/Proteasome
	Cysteine protease inhibitor-2 是半胱氨酸蛋白酶抑制剂。
T6015	Cathepsin Inhibitor 1	Cysteine Protease	Proteases/Proteasome
	Cathepsin inhibitor 1 是Cathepsin 的选择性抑制剂，能够抑制CatL(pIC50:7.9)、CatL2(pIC50:6.7)、CatS(pIC50:6.0)、CatK(pIC50:5.5)和CatB(pIC50:5.2)。
T21509	CA 074	Cysteine Protease	Proteases/Proteasome
	CA 074 是一种高效的组织蛋白酶B (cathepsin B) 抑制剂， Ki 值为2 to 5 nM。CA 074 抑制灵长类动物缺血性海马神经元死亡，可减轻 SJL/J 小鼠诱导的实验性自身免疫性脑脊髓炎的视网膜病变和视神经炎。
T13288	VBY-825	Cysteine Protease	Proteases/Proteasome
	VBY-825是cathepsin 一种新型的可逆抑制剂，对cathepsin B, L, S 和V 都有很高的抑制力。
T16089	MK-0674	Cysteine Protease	Proteases/Proteasome
	MK-0674 是一种可口服且具有选择性和高效性的 cathepsin K 抑制剂（IC50：0.4 nM），抑制 Cat B、Cat F、Cat L 和 Cat S，可用于和代谢相关的疾病。
T37504L	Cathepsin D and E FRET Substrate acetate(839730-93-7 Free base) Cathepsin D and E FRET Substrate acetate(839730-93-7 Free base)
	Cathepsin D and E FRET Substrate acetate 是组织蛋白酶 D 和 E 的荧光底物，但不适用于 B、H 或 L。Cathepsin D and E FRET Substrate acetate 可用于组织蛋白酶 D 和 E 研究的机理研究。
T1850	Balicatib AAE581,巴利卡替	Cysteine Protease	Proteases/Proteasome
	Balicatib (AAE581) 是组织蛋白酶K 抑制剂，其对组织蛋白酶K 的抑制作用是组织蛋白酶B、L 和S 的抑制性的10到100倍。
T15641	K777 APC-3316	P450; Cysteine Protease; CCR	Immunology/Inflammation; Metabolism; Microbiology/Virology; Proteases/Proteasome
	K777 是有效的，具有口服活性的，不可逆的半胱氨酸蛋白酶 (cysteine protease) 抑制剂。K777是有效的 CYP3A4 抑制剂(IC50= 60 nM)。K777也是选择性的 CCR4 拮抗剂，显示出强的趋化性抑制作用。K777 对 Cruzain（克鲁斯锥虫的主要半胱氨酸蛋白酶）和组织蛋白酶 B 和 L 具有不可逆的抑制作用。K777 通过靶向组织蛋白酶介导的细胞进入，显示出广谱的抗病毒作用。K777 抑制 EBOV 和 SARS-CoV 病毒的进入，IC50 值分别为 0.87 nM 和 0.68 nM。
T16092	L-873724	Others	Others
	L-873724 inhibits bone resorption. L-873724 is an effective, selective, and reversible non-basic cathepsin K inhibitor (IC50s: 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively). L-873724 also shows an IC50 of
T37053	Z-(L-Arg)-AMC (hydrochloride)
	Z-(L-Arg)-AMC is a fluorogenic substrate for trypsin, cathepsin B, and cathepsin H.1,2Upon enzymatic cleavage by trypsin, cathepsin B, or cathepsin H, 7-amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify trypsin, cathepsin B, and cathepsin H activity. AMC displays excitation/emission maxima of 340-360/440-460 nm, respectively. 1.Zimmerman, M., Ashe, B., Yurewicz, E.C., et al.Sensitive assays for trypsin, elastase, and chymotrypsin using new fluorogenic substrat...
T80739	Z-FG-NHO-BzOME
	Z-FG-NHO-BzOME 是一种选择性半胱氨酸蛋白酶抑制剂，主要作用于组织蛋白酶 B、组织蛋白酶 L、组织蛋白酶 S 及木瓜蛋白酶。
T78186	Ac-VLPE-FMK Ac-Val-Leu-Pro-Glu(OMe)-CH2F
	Ac-VLPE-FMK为一种四肽基单氟甲基酮(m-FMK)，兼作Cat-B及Cat-L抑制剂，适用于癌症侵袭性研究。
T73220	RO5461111
	RO5461111 是一种高特异性、口服有效的Cathepsin S 拮抗剂 (IC50: 0.4 nM, humanCathepsin S ; 0.5 nM, murineCathepsin S)。RO5461111 能够有效抑制抗原特异性 T 细胞和 B 细胞活化。RO5461111 对肺部炎症和狼疮性肾炎有改善作用。
T76599	Ac-Leu-Val-Lys-Aldehyde
	Ac-Leu-Val-Lys-Aldehyde 是有效的组织蛋白酶 B (cathepsin B) 抑制剂，其 IC50 值为 4 nM。该化合物能显着降低喹啉酸引起的纹状体细胞死亡，并促使 LC3-II 积累。
T36942	SSAA09E1 SSAA09E1
	SSAA09E1 is an inhibitor of severe acute respiratory syndrome coronavirus (SARS-CoV) viral entry.1It reduces infection of HEK293T cells transiently transfected with angiotensin-converting enzyme 2 (ACE2) by an HIV-based virus system pseudotyped with SARS-CoV surface glycoprotein (EC50= 6.7 μM). SSAA09E1 also inhibits the proteolytic activity of cathepsin L (IC50= 5.33 μM) but not cathepsin B when used at a concentration of 20 μM. 1.()
TP2161	Z-WEHD-FMK	Caspase	Apoptosis; Proteases/Proteasome
	Z-WEHD-FMK is a cell-permeable and irreversible inhibitor of caspase-1/5. It also shows a robust inhibitory effect on cathepsin B activity (IC50: 6 μM).
T15064	DBCO-NHCO-PEG4-NHS ester	Others	Others
	DBCO-NHCO-PEG4-NHS ester ester is a MMP-2- and cathepsin B- (CatB) cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
T73554	SPR38
	SPR38 是一种有效的 SARS-CoV-2 主要蛋白酶 (SARS-CoV-2 main protease) 抑制剂，Ki 为 0.260 μM。SPR38 还抑制hCatL 和hCatB，Ki 值分别为 1.92 μM 和 11.1 μM。
T73553	SPR39
	SPR39 是一种有效的 SARS-CoV-2 主要蛋白酶抑制剂，对 SARS-CoV-2 Mpro, hCatL, hCatB 的 Ki 值分别为 0.252、3.38、7.88 µM。SPR39 具有抗病毒和细胞毒性。
T75367	Z-Arg-Arg-4MβNA triacetate
	Z-Arg-Arg-4MβNA triacetate 为特异性针对组织蛋白酶 B（cathepsin B）的底物，其降解后可释放荧光产物4MβNA（λex= 355 nm, λem= 430 nm）。
T62494	Cathepsin C-IN-5
	CathepsinC-IN-5 (compound SF38) 为一高效、选择性、口服活性的组织蛋白酶 C (Cat C) 抑制剂，其针对Cat C、Cat L、Cat S、Cat B、Cat K 的IC50s 分别为 59.9 nM、4.26 µM、>5 µM、>5 µM、>5 µM。该化合物能够抑制骨髓和血液中的Cat C活性，降低中性粒细胞丝氨酸蛋白酶（NSP）的激活，并展现抗炎活性。
T6564L	Leupeptin Leupeptin Ac-LL,NK-381
	Leupeptin is a competitive protease inhibitor produced by actinomycetes. Leupeptin can inhibit cysteine, serine and threonine peptidases. Leupeptin inhibits serine proteinases (trypsin (Ki=3.5 nM), plasmin (Ki= 3.4 nM), porcine kallikrein), and cysteine p
T11864	Iptacopan LNP023	Others	Others
	Iptacopan (LNP023) 是一种与factor B 亲和力较高的抑制剂。
T69297	Leupeptin HCl
	Leupeptin is a naturally occurring protease inhibitor that can inhibit cysteine, serine and threonine peptidases. Leupeptin is an organic compound produced by actinomycetes. Leupeptin inhibits serine proteinases (trypsin (Ki=3.5 nM), plasmin (Ki= 3.4 nM), porcine kallikrein), and cysteine proteinases (papain, cathepsin B (Ki = 4.1 nM), endoproteinase Lys-C). It does not inhibit α-chymotrypsin or thrombin. Leupeptin is a competitive transition state inhibitor and its inhibition may be relieved by...
T21949	Calpain Inhibitor XII
	(Rac)-Calpain Inhibitor XII是一种可逆的，选择性抑制钙蛋白酶I（calpain I; μ-calpain）的化合物，具有19 nM的Ki值。其对钙蛋白酶II（calpain II; m-calpain; Ki=120 nM）和组织蛋白酶B（cathepsin B; Ki=750 nM）显示出较低的抑制亲和力。(Rac)-Calpain Inhibitor XII用于研究钙蛋白酶在多种生理过程中的角色，如嗜中性粒细胞趋化性、神经元信号传导和心脏对损伤的响应。

化合物

Cat.No: T80052

CA-074 methyl ester

Cat.No: T3420

Synonym: Cathepsin B Inhibitor IV,CA-074Me

Target: Cysteine Protease

Cat.No: T27989

Synonym: Cathepsin B Inhinitor-42

Cat.No: T28003

Synonym: Cathepsin B Inhinitor-17,MDK 7677

Cysteine protease inhibitor-2

Cat.No: T10924

Target: Cysteine Protease

Cathepsin Inhibitor 1

Cat.No: T6015

Target: Cysteine Protease

Cat.No: T21509

Target: Cysteine Protease

Cat.No: T13288

Target: Cysteine Protease

Cat.No: T16089

Target: Cysteine Protease

Cathepsin D and E FRET Substrate acetate(839730-93-7 Free base)

Cat.No: T37504L

Synonym: Cathepsin D and E FRET Substrate acetate(839730-93-7 Free base)

Cat.No: T1850

Synonym: AAE581,巴利卡替

Target: Cysteine Protease

Cat.No: T15641

Synonym: APC-3316

Target: P450, Cysteine Protease, CCR

Cat.No: T16092

Target: Others

Z-(L-Arg)-AMC (hydrochloride)

Cat.No: T37053

Cat.No: T80739

Cat.No: T78186

Synonym: Ac-Val-Leu-Pro-Glu(OMe)-CH2F

Cat.No: T73220

Ac-Leu-Val-Lys-Aldehyde

Cat.No: T76599

Cat.No: T36942

Synonym: SSAA09E1

Cat.No: TP2161

Target: Caspase

DBCO-NHCO-PEG4-NHS ester

Cat.No: T15064

Target: Others

Cat.No: T73554

Cat.No: T73553

Z-Arg-Arg-4MβNA triacetate

Cat.No: T75367

Cathepsin C-IN-5

Cat.No: T62494

Cat.No: T6564L

Synonym: Leupeptin Ac-LL,NK-381

Cat.No: T11864

Synonym: LNP023

Target: Others

Cat.No: T69297

Calpain Inhibitor XII

Cat.No: T21949

Cat. No.	Product Name	Target	Signaling Pathways
T6564	Leupeptin Hemisulfate 亮肽素	Serine Protease; Cysteine Protease	Proteases/Proteasome
	Leupeptin hemisulfate 是一种蛋白酶抑制剂，具有细胞膜渗透性、可逆性、竞争性和口服活性。Leupeptin hemisulfate 可以抑制 Cathepsin B、Cathepsin H、Cathepsin L 的活性，阻断两性溶酶体的融合。Leupeptin hemisulfate 还具有抗炎活性。
TN1249	3-Epiursolic acid	Cysteine Protease; Immunology/Inflammation related	Immunology/Inflammation; Proteases/Proteasome
	3-Epiursolic Acid 是一种三萜类物质，分离自桃金娘科植物，是组织蛋白酶 L 的竞争性抑制剂（IC50=6.5 μM，Ki=19.5 μM），对 cathepsin B 无明显作用。
T3417	Amentoflavone Didemethyl-ginkgetin,穗花杉双黄酮,Amenthoflavone,3',8''-Biapigenin	Apoptosis; P450; Phospholipase; Reactive Oxygen Species; Opioid Receptor; COX; Antibacterial; RSV; Antifungal	Apoptosis; Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience; NF-κB
	Amentoflavone (3',8''-Biapigenin) 是一种具有很多生物活性的双黄酮类天然产物，有抗炎、抗氧化和神经保护等作用。
TJS2216	Aurantiamide acetate 金色酰胺醇酯,Asperglaucide	Cysteine Protease	Proteases/Proteasome
	Aurantiamide acetate (Asperglaucide) 是抑制口服有活性的 cathepsin 选择性抑制剂，分离自 Portulaca oleracea L。它具有抗炎作用，可用于研究炎性相关疾病。

天然产物

Leupeptin Hemisulfate

Cat.No: T6564

Synonym: 亮肽素

Target: Serine Protease, Cysteine Protease

3-Epiursolic acid

Cat.No: TN1249

Target: Cysteine Protease, Immunology/Inflammation related

Cat.No: T3417

Synonym: Didemethyl-ginkgetin,穗花杉双黄酮,Amenthoflavone,3',8''-Biapigenin

Target: Apoptosis, P450, Phospholipase, Reactive Oxygen Species, Opioid Receptor, COX, Antibacterial, RSV, Antifungal

Aurantiamide acetate

Cat.No: TJS2216

Synonym: 金色酰胺醇酯,Asperglaucide

Target: Cysteine Protease

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