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78

抑制剂 & 化合物

17

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T40495	Elastase from porcine pancreas 弹性蛋白酶,EC 3.2.1.35	Others	Others
	Elastase from porcine pancreas 由 240 个氨基酸残基组成，是一种丝氨酸蛋白酶，可以水解蛋白质和多肽。它可诱发仓鼠气肿。
T78633	MeOSuc-AAPV-CMK Elastase Inhibitor III
	MeOSuc-AAPV-CMK (Elastase Inhibitor III) 为一种特定抗体，不仅抑制白细胞弹性蛋白酶，也能够抑制组织蛋白酶 G 及蛋白酶 3。此外，MeOSuc-AAPV-CMK 可有效阻断白细胞弹性蛋白酶对脂联素进行裂解的作用。
T60855	Elastase-IN-1
	Elastase-IN-1 (Compound Q11) 是无毒的弹性蛋白酶抑制剂，IC50值为 0.897 μM。
T74243	Tyrosinase/elastase-IN-1
	Tyrosinase/elastase-IN-1，一种来源于悬钩子叶的三萜类化合物，具有抑制酪氨酸酶和弹性蛋白酶活性的功能。
T82483	Elastase LasB-IN-1
	ElastaseLasB-IN-1 (Compound 4b) 是一种选择性弹性蛋白酶LasB抑制剂，展现出抗菌活性，其IC50值为76 nM。
T79397	Neutrophil elastase inhibitor 4
	Neutrophilelastase inhibitor4 (compound 4f) 是竞争性抑制HNE的化合物，具有较低的半抑制浓度(IC50: 42.30 nM)和解离常数(Ki: 8.04 nM)。此外，该化合物能够诱导T47D细胞的apoptosis，并在多种细胞系中展现出抗增殖作用，分别在T47D、RPMI 8226、A549、HSF细胞系的IC50值为21.25、34.17、29.93、99.11 nM。
T12613L	BAY-85-8501	Serine Protease	Proteases/Proteasome
	BAY-85-8501 是选择性的人类中性脂酶抑制剂，IC50=65 pM。
T9964	BOS-318	Others	Others
	BOS-318是一种Furin 抑制剂，具有缓慢解离，高选择性，细胞通透性等特点。
T3107	Alvelestat AZD9668,Avelestat	Others; Serine Protease	Others; Proteases/Proteasome
	Alvelestat (AZD9668) 是一种口服活性，亲和性和选择性的中性粒细胞弹性蛋白酶 (NE) 抑制剂，pIC50=7.9 nM，Ki=为 9.4 nM，Kd=9.5 nM。
TP1012	CH 5450 Z-Ile-Glu-Pro-Phe-Ome	Others	Others
	CH 5450 (Z-Ile-Glu-Pro-Phe-Ome) 是一种人心脏糜酶 chymase 的短肽类抑制剂。
T6986	Sivelestat ONO5046,EI546,西维来司他,LY544349	Others; SARS-CoV; Serine Protease	Microbiology/Virology; Others; Proteases/Proteasome
	Sivelestat (ONO5046) 是一种选择性的中性粒细胞弹性蛋白酶抑制剂，其 IC50值为 44 nM，Ki 值为 200 nM。它有潜力研究 COVID-19 的急性肺损伤、急性呼吸窘迫综合征或弥散性血管内凝血。
T20163	Acetyltrialanine
	Acetyltrialanine 是一种二肽化合物，在 Tb+3-胰腺弹性蛋白酶复合物上的两个位点结合，可做为氮源使用。
T8563	2-(2-bromophenyl)-5-chloro-4H-3,1-benzoxazin-4-one	Serine Protease	Proteases/Proteasome
	2-(2-bromophenyl)-5-chloro-4H-3,1-benzoxazin-4-one 是一种人类中性粒细胞弹性蛋白酶抑制剂。
T8602	2-CHLOROMETHYL-1,1-DIOXO-1,2-DIHYDRO-1LAMBDA6-BENZO[D]ISOTHIAZOL-3-ONE	Serine Protease	Proteases/Proteasome
	2-CHLOROMETHYL-1,1-DIOXO-1,2-DIHYDRO-1LAMBDA6-BENZO[D]ISOTHIAZOL-3-ONE 靶向中性粒细胞弹性蛋白酶（人）。
T8677	3,4 Dichloroisocoumarin	Others; Serine Protease; Cysteine Protease	Others; Proteases/Proteasome
	3,4 Dichloroisocoumarin 是一种颗粒酶、组织蛋白酶 G 和中性粒细胞弹性蛋白酶抑制剂
T68099	midesteine MR-889	Others	Others
	Midesteine (MR-889) 是一种可逆、慢结合、完全竞争的蛋白酶抑制剂。
T38364	MeOSuc-AAPV-AMC MeOSuc-Ala-Ala-Pro-Val-AMC
	MeOSuc-AAPV-AMC (MeOSuc-Ala-Ala-Pro-Val-AMC)是人类白细胞和猪胰腺弹性蛋白酶的荧光底物，是一种四肽。
T10473	BAY-678	Others	Others
	BAY-678是一种人中性粒细胞弹性蛋白酶（HNE；IC50：20 nM）抑制剂，具有口服生物活性、高效性和选择性。BAY-678 是被基因结构组学联盟 (SGC) 推荐的化学探针。
T20762	Sivelestat sodium tetrahydrate ONO-5046 sodium tetrahydrate,Elaspol,ONO 5046,ONO5046 sodium tetrahydrate,Elaspol sodium tetrahydrate,ONO-5046,Sivelestat Sodium,Sivelestat Sodium Hydrate,ONO5046	Serine Protease	Proteases/Proteasome
	Sivelestat sodium tetrahydrate (ONO5046 sodium tetrahydrate) 是竞争性的人类中性粒细胞弹性蛋白酶的抑制剂，其 IC50 值为 44 nM， Ki 值为 200 nM。Sivelestat (EI546) sodium tetrahydrate 有潜力用于 COVID-19的急性肺损伤/急性呼吸窘迫综合征或弥散性血管内凝血的研究。
T25131	AZD8309 AZD 8309,AZD-8309	Glutathione Peroxidase; CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation; Metabolism
	AZD8309 是一种强效的、可口服的趋化因子受体CXCR2的拮抗剂，能够调节中性粒细胞的转运，可显著降低胰腺和肺部的MPO，并降低胰腺内的胰蛋白酶和弹性蛋白酶活性。AZD8309 能够用于研究炎症系列疾病。
T15285	FK706	Serine Protease	Proteases/Proteasome
	FK706 is a slow-binding and competitive human neutrophil elastase inhibitor (IC50: 83 nM; Ki: 4.2 nM). FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase (IC50s: 22 nM and 100 nM, respectively). FK706 has an anti-inflammatory ef
T13389	ZD-0892	PI3K	PI3K/Akt/mTOR signaling
	ZD-0892 is a selective and poten neutrophil elastaset inhibitor(human neutrophil elastase and porcine pancreatic elastase with Kis of 6.7 and 200 nM, respectively).
T10254	AE-3763	Serine Protease	Proteases/Proteasome
	AE-3763 is a peptide-based human neutrophil elastase inhibitor (IC50: 29 nM).
T11865	Lodelaben 氯德拉苯,SC-39026,Declaben	Others	Others
	Lodelaben is a human neutrophil elastase inhibitor with an IC50 and Ki of 0.5 and 1.5 μM, respectively.
T17288	ZD8321	Serine Protease	Proteases/Proteasome
	ZD8321 is an effective inhibitor of human Neutrophil elastase (Ki: 13±1.7 nM).
T31877	Freselestat ONO-PO 736,ONO-6818,ONO 6818,ONO6818
	Freselestat (ONO-6818) is a potent neutrophil elastase inhibitor that significantly reduces the production of interleukin 8 and C5B-9. Freselestat reduces inflammatory mediators during simulated cardiopulmonary bypass.
T25520	ICI 200355 ICI-200,355,ICI 200,355,ICI-200355,ICI200,355,ICI200355
	ICI 200355 is an inhibitor of human neutrophil elastase.
T24328	L 680833 L680,833,L680833,L-680,833,L 680,833,L-680833
	L 680833 is an orally active monocyclic beta-lactam human polymorphonuclear leukocyte elastase inhibitor.
T30303	BAY8040 BAY 8040,BAY-8040
	BAY8040 is a potent selective human neutrophilic elastase inhibitor with excellent potency and selectivity with promising pharmacokinetic characteristics.
T11525L	GW311616 hydrochloride GW311616A	Others	Others
	GW-311616 hydrochloride is a long duration, orally bioavailable, and selective human neutrophil elastase (HNE) inhibitor (IC50: 22 nM; Ki: 0.31 nM).
T34465	S 2484 S-2484,S2484,Pyro-glu-pro-val-pna
	S 2484 is a chromogranic specific granulocyte elastase substrate.
T15144	DMP 777 L-694458	Others	Others
	DMP 777 is an orally active inhibitor of human leukocyte elastase.
T25784L	MDL-101146, (S)- MDL101146, (S)-
	MDL-101146, (S)- is an effective orally active inhibitor of human neutrophil elastase.
T62846	Freselestat quarterhydrate
	Freselestat quarterhydrate (ONO-6818 quarterhydrate) 是一种有效的、口服具有活力的嗜中性粒细胞弹性蛋白酶 (neutrophil elastase) 抑制剂 (Ki: 12.2 nM)。Freselestat quarterhydrate 对其他蛋白酶（例如胰蛋白酶，蛋白酶3，胰弹性蛋白酶，凝血酶，纤溶酶，胶原酶，组织蛋白酶G 和鼠巨噬细胞弹性蛋白酶）的活性低 100 倍以上，表现出有效的抗炎作用。
T25880	Nostopeptin B
	Nostopeptin B is an inhibitor of elastase.
T25782	MDL 27324 MDL-27,324,MDL-27324,MDL27,324,MDL 27,324,MDL27324
	MDL 27324 is an inhibitor of human neutrophil elastase.
T68179	Neltenexine
	Neltenexine is an elastase inhibitor that may be useful for preventing pulmonary emphysema.
T27747	KRP-109 KRP 109,KRP109
	KRP-109, a neutrophil elastase (NE) inhibitor, acts by decreasing expression of TGF-ß Signal Related Genes.
T70767	SR 26831
	SR 26831 is a selective elastase inhibitor.
T25781	MDL 101146 MDL-101146,MD 101,146,MDL101146,MDL 101,146,MDL-101,146
	MDL 101146 is an orally active neutrophil elastase inhibitor.
T25518	Ici 186756 Ici186756,Ici--186756
	Ici 186756 is a novel, effective, and selective inhibitor of human neutrophil elastase.
T71198	Eglin c (60-63)
	Eglin c (60-63) is a sequence of a peptide that has been studied for its inhibitory activity towards human leukocyte elastase, cathepsin G, porcine pancreatic elastase and alpha-chymotrypsin.
T36351	Suc-AAP-Abu-pNA
	Suc-AAP-Abu-pNA 是胰腺弹性蛋白酶的特异性底物 (Km = 100 μM; Kcat/Km = 35,300 s-1 M-1 for rat pancreatic elastase; Km = 30 μM; Kcat/Km = 351,000 s-1 M-1 for porcine pancreatic elastase)。
T41043	Lonodelestat POL6014
	Lonodelestat (POL6014) is a potent, orally active and selective peptide inhibitor of human neutrophil elastase (hNE).
T3107L	Alvelestat tosylate
	Alvelestat can inhibit neutrophil elastase (NE), which acts an important role in NET formation.
T25521	Ici 200880 Ici 200,880,Ici-200880,Ici200,880,Ic-200,880,Ici200880
	Ici 200880 is a human neutrophil elastase synthetic peptide inhibitor.
T69790	GW-475151
	GW-475151 inhibits human neutrophil elastase (HNE).
T27251	Elasnin
	Elasnin is a reversible inhibitor of elastase for human granulocyte and pancreatic enzymes with IC50 values of 1.3 and 30 µg/ml, respectively.
T20130	Elastatinal BRN0873543,BRN 0873543,BRN-0873543
	Elastatinal is an elastase inhibitor. It is found in culture filtrates of various species of actinomyces.
T25784	MDL-101146, (R)- MDL101146, (R)-
	MDL-101146, (R)- is an effective orally active inhibitor of human neutrophil elastase.

化合物

Elastase from porcine pancreas

Cat.No: T40495

Synonym: 弹性蛋白酶,EC 3.2.1.35

Target: Others

MeOSuc-AAPV-CMK

Cat.No: T78633

Synonym: Elastase Inhibitor III

Elastase-IN-1

Cat.No: T60855

Tyrosinase/elastase-IN-1

Cat.No: T74243

Elastase LasB-IN-1

Cat.No: T82483

Neutrophil elastase inhibitor 4

Cat.No: T79397

Cat.No: T12613L

Target: Serine Protease

Cat.No: T9964

Target: Others

Cat.No: T3107

Synonym: AZD9668,Avelestat

Target: Others, Serine Protease

Cat.No: TP1012

Synonym: Z-Ile-Glu-Pro-Phe-Ome

Target: Others

Cat.No: T6986

Synonym: ONO5046,EI546,西维来司他,LY544349

Target: Others, SARS-CoV, Serine Protease

Acetyltrialanine

Cat.No: T20163

2-(2-bromophenyl)-5-chloro-4H-3,1-benzoxazin-4-one

Cat.No: T8563

Target: Serine Protease

2-CHLOROMETHYL-1,1-DIOXO-1,2-DIHYDRO-1LAMBDA*6*-BENZO[D]ISOTHIAZOL-3-ONE

Cat.No: T8602

Target: Serine Protease

3,4 Dichloroisocoumarin

Cat.No: T8677

Target: Others, Serine Protease, Cysteine Protease

Cat.No: T68099

Synonym: MR-889

Target: Others

MeOSuc-AAPV-AMC

Cat.No: T38364

Synonym: MeOSuc-Ala-Ala-Pro-Val-AMC

Cat.No: T10473

Target: Others

Sivelestat sodium tetrahydrate

Cat.No: T20762

Synonym: ONO-5046 sodium tetrahydrate,Elaspol,ONO 5046,ONO5046 sodium tetrahydrate,Elaspol sodium tetrahydrate,ONO-5046,Sivelestat Sodium,Sivelestat Sodium Hydrate,ONO5046

Target: Serine Protease

Cat.No: T25131

Synonym: AZD 8309,AZD-8309

Target: Glutathione Peroxidase, CXCR

Cat.No: T15285

Target: Serine Protease

Cat.No: T13389

Target: PI3K

Cat.No: T10254

Target: Serine Protease

Cat.No: T11865

Synonym: 氯德拉苯,SC-39026,Declaben

Target: Others

Cat.No: T17288

Target: Serine Protease

Cat.No: T31877

Synonym: ONO-PO 736,ONO-6818,ONO 6818,ONO6818

Cat.No: T25520

Synonym: ICI-200,355,ICI 200,355,ICI-200355,ICI200,355,ICI200355

Cat.No: T24328

Synonym: L680,833,L680833,L-680,833,L 680,833,L-680833

Cat.No: T30303

Synonym: BAY 8040,BAY-8040

GW311616 hydrochloride

Cat.No: T11525L

Synonym: GW311616A

Target: Others

Cat.No: T34465

Synonym: S-2484,S2484,Pyro-glu-pro-val-pna

Cat.No: T15144

Synonym: L-694458

Target: Others

MDL-101146, (S)-

Cat.No: T25784L

Synonym: MDL101146, (S)-

Freselestat quarterhydrate

Cat.No: T62846

Cat.No: T25880

Cat.No: T25782

Synonym: MDL-27,324,MDL-27324,MDL27,324,MDL 27,324,MDL27324

Cat.No: T68179

Cat.No: T27747

Synonym: KRP 109,KRP109

Cat.No: T70767

Cat.No: T25781

Synonym: MDL-101146,MD 101,146,MDL101146,MDL 101,146,MDL-101,146

Cat.No: T25518

Synonym: Ici186756,Ici--186756

Eglin c (60-63)

Cat.No: T71198

Suc-AAP-Abu-pNA

Cat.No: T36351

Cat.No: T41043

Synonym: POL6014

Alvelestat tosylate

Cat.No: T3107L

Cat.No: T25521

Synonym: Ici 200,880,Ici-200880,Ici200,880,Ic-200,880,Ici200880

Cat.No: T69790

Cat.No: T27251

Cat.No: T20130

Synonym: BRN0873543,BRN 0873543,BRN-0873543

MDL-101146, (R)-

Cat.No: T25784

Synonym: MDL101146, (R)-

Cat. No.	Product Name	Target	Signaling Pathways
TN1022	Secologanoside	Serine Protease	Proteases/Proteasome
	Secologanoside 来自于Poraqueiba sericea 的萜类化合物，对弹性蛋白酶抑制活性较低，IC50=164 μg/mL。它对成纤维细胞有中度细胞毒性。
T3S0381	Chrysophanol 8-O-glucoside	Serine Protease	Proteases/Proteasome
	Chrysophanol 8-O-glucoside 来自Rumex acetosa 根部，具有中等的弹性蛋白酶抑制特性。它具有温和的细胞毒性和抗糖尿病特性，能够在胰岛素刺激的葡萄糖转运途径中发挥代谢作用。
TJS0314	5,7-Dihydroxy-4-methylcoumarin Methyl-2H-Chromen-2-One,5,7-二羟基-4-甲基香豆素,4-Methyllimetol,4-Methyl-5,7-Dihydroxycoumarin	Others; Antibacterial; Antifungal	Microbiology/Virology; Others
	5,7-Dihydroxy-4-methylcoumarin (Methyl-2H-Chromen-2-One) 是墨西哥龙蒿中的一种香豆素衍生物。它抑制人类中性粒细胞氧化代谢和弹性蛋白酶活性，有抗真菌和抗细菌活性。
TN3926	Eicosanyl caffeate	Others	Others
	Eicosanyl caffeate has anti-ulcer and moderate antioxidant properties, it exhibits potent elastase inhibitory activity, with the IC(50) value of 0.99 microg/mL.
T75619	Aristololactam IIIa
	Aristololactam IIIa 对超氧阴离子生成和弹性蛋白酶的释放有显著抑制作用，其 IC50值分别为 0.12 和 0.20 μg/mL。
TN4214	Hispanone
	Hispanone possesses anti-inflammatory activity, it shows inhibition of superoxide anion generation and elastase release.
T75648	Rivulariapeptolides 1155
	Rivulariapeptolides 1155 是一种有效的丝氨酸蛋白酶 (serine protease) 抑制剂，对糜蛋白酶、弹性蛋白酶、蛋白蛋白酶 K 的 IC50分别为 41.84、4.94、56.54 nM。
TN3879	Docosyl caffeate
	Docosyl caffeate shows moderate antioxidant activity in DPPH and ABTS scavenging assays, it also has significant anti-inflammation activity. Docosyl caffeate exhibits potent elastase inhibitory activity, with the IC50 value of 1.4 microg/mL.
TN1556	Decarine	Antifection	Microbiology/Virology
	Decarine has high antibacterial activity against mycobacterial, gram-positive and gram-negative bacteria, and low cytotoxicity towards human macrophages.Decarine inhibits fMLP/CB-induced elastase release with IC(50) values < or = 5.53 microg/mL.
T75649	Rivulariapeptolides 1185
	Rivulariapeptolides 1185 是一种高效的选择性丝氨酸蛋白酶抑制剂，其对胰凝蛋白酶、弹性蛋白酶和蛋白酶 K 的 IC50分别为 13.17 nM、23.59 nM 和 55.26 nM。
TN4866	Pyracrenic acid	Others	Others
	Pyracrenic acid is a potent elastase inhibitor with an IC50 value of 1.5 mg/mL. Pyracrenic acid shows DPPH radical scavenging activity. It also shows significant cytotoxic activities against human cancer cells COLO 205 and AGS.
T75652	Molassamide B
	Molassamide B，丝氨酸蛋白酶抑制剂，对胰凝乳蛋白酶、弹性蛋白酶及蛋白酶 K 具有显著抑制活性，其IC50值分别为24.65、11.69和5.42 nM。
T75650	Rivulariapeptolides 1121
	Rivulariapeptolides 1121，作为一种高效的选择性丝氨酸蛋白酶抑制剂，对胰凝蛋白酶、弹性蛋白酶和蛋白酶K展示出了显著的抑制活性，其IC50值分别为35.52 nM、13.24 nM和48.05 nM。
T75651	Rivulariapeptolides 988
	Rivulariapeptolides 988作为一种高效选择性丝氨酸蛋白酶抑制剂，对胰凝蛋白酶、弹性蛋白酶和蛋白酶K的IC50分别为95.46 nM、15.29 nM和85.50 nM。
TN4005	erythro-Guaiacylglycerol-beta-O-4'-dehydrodisinapyl ether	Serine Protease	Proteases/Proteasome
	erythro-Guaiacylglycerol-beta-O-4'-dehydrodisinapyl ether 是一种从巴西橡胶种子壳中提取的化合物，对人白细胞弹性蛋白酶具有抑制活性（IC50 ：171 umol/L）。
TN3706	Coronarin A
	Coronarin, A, B, C, and D are cytotoxic prinicples from the rhizomes of Hedychium coronarium, Zingiberaceae. Coronarin A exhibits good growth inhibition activities on HUVEC proliferation, it effectively suppresses the growth factor induced tube formation
TN4584	Morolic acid	IL Receptor; COX; HIV Protease	Immunology/Inflammation; Microbiology/Virology; Neuroscience; Proteases/Proteasome
	Morolic acid and moronic acid have shown sustained antidiabetic and antihyperglycemic action possibly mediated by an insulin sensitization with consequent changes of glucose, cholesterol and triglycerides, in part mediated by inhibition of 11β-HSD 1. Moro

天然产物

Cat.No: TN1022

Target: Serine Protease

Chrysophanol 8-O-glucoside

Cat.No: T3S0381

Target: Serine Protease

5,7-Dihydroxy-4-methylcoumarin

Cat.No: TJS0314

Synonym: Methyl-2H-Chromen-2-One,5,7-二羟基-4-甲基香豆素,4-Methyllimetol,4-Methyl-5,7-Dihydroxycoumarin

Target: Others, Antibacterial, Antifungal

Eicosanyl caffeate

Cat.No: TN3926

Target: Others

Aristololactam IIIa

Cat.No: T75619

Cat.No: TN4214

Rivulariapeptolides 1155

Cat.No: T75648

Docosyl caffeate

Cat.No: TN3879

Cat.No: TN1556

Target: Antifection

Rivulariapeptolides 1185

Cat.No: T75649

Pyracrenic acid

Cat.No: TN4866

Target: Others

Cat.No: T75652

Rivulariapeptolides 1121

Cat.No: T75650

Rivulariapeptolides 988

Cat.No: T75651

erythro-Guaiacylglycerol-beta-O-4'-dehydrodisinapyl ether

Cat.No: TN4005

Target: Serine Protease

Cat.No: TN3706

Cat.No: TN4584

Target: IL Receptor, COX, HIV Protease

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