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Search Results for " cathepsin l "

35

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T21616	L-006235 L 006235	Cysteine Protease	Proteases/Proteasome
	L-006235 是一种口服有活性的、可逆的cathepsin K 选择性抑制剂，在骨吸收试验中的IC50值为 5 nM。它能够抑制胶原蛋白降解，并较少骨质流失。
T27730	KGP94 KGP-94,KGP 94	Cysteine Protease	Proteases/Proteasome
	KGP94 是一种有效的、选择性的和竞争性的溶酶体内肽酶抑制剂。
T38469	(Rac)-Z-Phe-Phe-FMK Cathepsin L-IN-2	Beta Amyloid; Cysteine Protease	Neuroscience; Proteases/Proteasome
	(Rac)-Z-Phe-Phe-FMK (Cathepsin L-IN-2) 是一种 cathepsin L 抑制剂，抑制 β-淀粉样蛋白诱导凋亡变化的倾向。(Rac)-Z-Phe-Phe-FMK 通过 siRNA 敲低 LC3B 表达可抑制 PI 诱导的 IkappaBalpha 降解。
T72569	Cathepsin L/S-IN-1
	CathepsinL/S-IN-1 是 Cathepsin L 和 Cathepsin S 的双重抑制剂，IC50分别为 4.10 μM 和 1.79 μM。CathepsinL/S-IN-1 对胰腺癌 BxPC-3 和 PANC-1 细胞具有显著的抗转移和侵袭作用。
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)。
T12909	SID 26681509	Cysteine Protease; Parasite	Microbiology/Virology; Proteases/Proteasome
	SID 26681509 是可逆的，竞争性的人组织蛋白酶 L 选择性抑制剂，IC50为 56 nM。它抑制Plasmodium falciparum 的体外繁殖，IC50为15.4 μM，抑制Leishmania major，IC5012.5 μM。
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。
TP2056L	Acetyl-Calpastatin (184-210)(human) acetate Acetyl-Calpastatin (184-210) (human) acetate(123714-50-1 Free base )	Cysteine Protease	Proteases/Proteasome
	Acetyl-Calpastatin (184-210)(human) acetate 是一种有效，选择性和可逆的钙蛋白酶 (calpain) 抑制剂，对 μ-钙蛋白酶和组织蛋白酶 L 的 Ki 值分别为 0.2 nM 和 6 μM。
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。
T35753	Z-Phe-Tyr(tBu)-diazomethylketone
	Irreversible cathepsin L inhibitor which is ca 10'000 times more effective in inactivating cathepsin L than cathepsin S.
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
T80105	Z-Phe-Phe-Diazomethylketone
	Z-Phe-Phe-Diazomethylketone 为cathepsin L 特异性抑制剂。
T71275	CID16725315
	Thiocarbazate, also known as CID16725315, is an inhibitor of human cathepsin L. Inhibition of cathepsin L thus holds promise for therapeutic intervention for both SARS-CoV and Ebola virus infection. With respect to the development of antiviral agents, inhibitors of human cathepsin L are not subject to resistance because of rapid mutations of the viral genome. Cathepsin L is therefore an attractive target for drug development.
T26938	CAA0225 CAA 0225,CAA-0225
	CAA0225 is a selective inhibitor of cathepsin L. CAA0225 is a probe for autophagic proteolysis.
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。
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...
T71618	Oxocarbazate
	Oxocarbazate, also known as CID23631927, is an inhibitor of human cathepsin L. In the cathepsin L inhibition assay, The oxocarbazate caused a time-dependent 17-fold drop in IC50 from 6.9 nM (no preincubation) to 0.4 nM (4-h preincubation). Slowly reversible inhibition was demonstrated in a dilution assay. CID23631927 demonstrate activity in blocking both SARS-CoV (IC50 = 273 nM) and Ebola virus (IC50 = 193 nM) entry into human embryonic. CID 23631927 was a subnanomolar, slow-binding, reversible...
T81265	RKLLW-NH2
	RKLLW-NH2为一种组织蛋白酶L抑制剂。
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。
T41236	Z-FY-CHO
	Z-FY-CHO (Z-Phe-Tyr-CHO) 是一种特异且有效的组织蛋白酶 L (CTSL) 抑制剂。
T40463	Relacatib SB-462795
	Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V. It exhibits high affinity for these enzymes, with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Moreover, Relacatib effectively inhibits endogenous cathepsin K in situ in human osteoclasts, as well as human osteoclast-mediated bone resorption, with IC 50 values of 45 nM and 70 nM, respectively. Additionally, in vitro studies demonstrate Relacatib's inhibitory effect on bone resorption in ...
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.()
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。
T63831	SID 26681509 quarterhydrate
	SID 26681509 quarterhydrate 是可逆的、有效的、选择性的、竞争性的人组织蛋白酶 L (human cathepsin L) 抑制剂 (IC50: 56 nM)。SID 26681509 quarterhydrate 能够抑制Plasmodium falciparum 的体外繁殖 (IC50: 15.4 μM)，并抑制Leishmania major (IC50: 12.5 μM)，且不抑制组织蛋白酶 G 的活性。
TP2056	Acetyl-Calpastatin(184-210)(human) Acetyl-Calpastatin (184-210) (human)
	Selective calpain inhibitor. Strongly inhibits calpain I (Ki = 0.2 nM) and II but does not inhibit papain, trypsin and cathepsin L (Ki = 6 μM). Increases secretion of amyoid β-protein (Aβ) 42, Aβ40 and Aβ42 ratio.
T73395	ASPER-29
	ASPER-29是一种Asperphenamate类似物，对组织蛋白酶L和S均显示出双重抑制作用，其IC50值分别为6.03 μM和5.02 μM。此化合物主要应用于癌症迁移和侵袭的研究。
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。
T75794	Acetyl-Calpastatin(184-210)(human) TFA
	Acetyl-Calpastatin(184-210)(human) TFA 是一种有效，选择性和可逆的钙蛋白酶 (calpain) 抑制剂，对 μ-钙蛋白酶和组织蛋白酶 L 的Ki 值分别为 0.2 nM 和 6 μM。
T11864	Iptacopan LNP023	Others	Others
	Iptacopan (LNP023) 是一种与factor B 亲和力较高的抑制剂。
T72446	SARS-CoV-2 Mpro-IN-4
	SARS-CoV-2 Mpro-IN-4是针对主要蛋白酶(MPro)和组织蛋白酶L(CatL)的双重抑制剂，其IC50s分别为900 nM和60 nM。此化合物对SARS-CoV2展现出抗病毒活性，在hACE2表达的A549细胞中可有效阻断SARS-CoV2复制，其IC50值为8.2 nM。
T72447	SARS-CoV-2 Mpro-IN-5
	SARS-CoV-2 Mpro-IN-5是一种针对主要蛋白酶(MPro)和组织蛋白酶L(CatL)的双重抑制剂，具备IC50s分别为1800 nM和145 nM。该化合物在对抗SARS-CoV2方面显示出显著的抗病毒活性，并能在表达hACE2的A549细胞中阻断SARS-CoV2复制，IC50值达14.7 nM。

化合物

Cat.No: T21616

Synonym: L 006235

Target: Cysteine Protease

Cat.No: T27730

Synonym: KGP-94,KGP 94

Target: Cysteine Protease

(Rac)-Z-Phe-Phe-FMK

Cat.No: T38469

Synonym: Cathepsin L-IN-2

Target: Beta Amyloid, Cysteine Protease

Cathepsin L/S-IN-1

Cat.No: T72569

Cathepsin Inhibitor 1

Cat.No: T6015

Target: Cysteine Protease

Cat.No: T12909

Target: Cysteine Protease, Parasite

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)

Acetyl-Calpastatin (184-210)(human) acetate

Cat.No: TP2056L

Synonym: Acetyl-Calpastatin (184-210) (human) acetate(123714-50-1 Free base )

Target: Cysteine Protease

Cat.No: T1850

Synonym: AAE581,巴利卡替

Target: Cysteine Protease

Cat.No: T15641

Synonym: APC-3316

Target: P450, Cysteine Protease, CCR

Z-Phe-Tyr(tBu)-diazomethylketone

Cat.No: T35753

Cat.No: T16092

Target: Others

Z-Phe-Phe-Diazomethylketone

Cat.No: T80105

Cat.No: T71275

Cat.No: T26938

Synonym: CAA 0225,CAA-0225

Cat.No: T80739

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

Cat.No: T37053

Cat.No: T71618

Cat.No: T81265

Cat.No: T78186

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

Cat.No: T41236

Cat.No: T40463

Synonym: SB-462795

Cat.No: T36942

Synonym: SSAA09E1

Cat.No: T73554

Cat.No: T73553

SID 26681509 quarterhydrate

Cat.No: T63831

Acetyl-Calpastatin(184-210)(human)

Cat.No: TP2056

Synonym: Acetyl-Calpastatin (184-210) (human)

Cat.No: T73395

Cathepsin C-IN-5

Cat.No: T62494

Acetyl-Calpastatin(184-210)(human) TFA

Cat.No: T75794

Cat.No: T11864

Synonym: LNP023

Target: Others

SARS-CoV-2 Mpro-IN-4

Cat.No: T72446

SARS-CoV-2 Mpro-IN-5

Cat.No: T72447

Cat. No.	Product Name	Target	Signaling Pathways
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。
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。
T19392	L-Homocysteine	Others	Others
	L-Homocysteine, an L-configured homocysteine metabolite, induces the upregulation of cathepsin V, which mediates vascular endothelial inflammation in hyperhomocysteinaemia.
T72898	Gallinamide A
	Gallinamide A 是一种组织蛋白酶 L 的有效抑制剂，其 IC50值为 17.6 pM。

天然产物

Aurantiamide acetate

Cat.No: TJS2216

Synonym: 金色酰胺醇酯,Asperglaucide

Target: Cysteine Protease

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: T19392

Target: Others

Cat.No: T72898

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