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41

抑制剂 & 化合物

2

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Cat. No. Product Name Target Signaling Pathways
T11666 IPR-803

Serine/threonin kinase Cell Cycle/Checkpoint; Metabolism
IPR-803 是一种有效的 uPAR·uPA 蛋白-蛋白相互作用抑制剂,具有抗肿瘤活性。 IPR-803 直接与 uPAR 结合,Ki 为 0.2 μM。
T4058 R-IMPP

Others; Serine/threonin kinase Cell Cycle/Checkpoint; Metabolism; Others
R-IMPP 是抗 PCSK9分泌的药物 (IC50=4.8 μM),靶向作用于 80S 核糖体,抑制 PCSK9 蛋白的翻译。
T7017 WNK463

Serine/threonin kinase Cell Cycle/Checkpoint; Metabolism
WNK463 是口服有活性的 WNK 激酶抑制剂,能够抑制 WNK1 (IC50:5 nM)、WNK2 (IC50:1 nM)、WNK3 (IC50:6 nM)及 WNK4 (IC50:9 nM)。
TP1277 Bradykinin

缓激肽

Endogenous Metabolite; Bradykinin Receptor GPCR/G Protein; Metabolism
Bradykinin 是由激肽释放酶-激肽系统产生的活性肽。 它是炎症调节因子和神经调节因子,对几种血管和肾功能也有调节作用。
T10547 BioE-1115

Serine/threonin kinase; Casein Kinase Cell Cycle/Checkpoint; Metabolism; Stem Cells
BioE-1115 是一种特异性和有效的丝氨酸-苏氨酸蛋白激酶抑制剂 (PASK, IC50 = 4 nM)。 BioE-1115 是一种有效的酪蛋白激酶 2α 抑制剂 (IC50 = 10 μM)。
T11885 LSP-249

Others Others
LSP-249是血浆 kallikrein 的抑制剂,用于血管性水肿的研究,EC50值小于 100 nM。
T8350 TPCK

Proteasome Proteases/Proteasome; Ubiquitination
TPCK 是丝氨酸蛋白酶抑制剂,通过与 HPV-18 E7 蛋白的视网膜母细胞瘤蛋白 (RB) 结合核心发生反应,并能够消除其 RB 结合能力。将它添加到培养基内,可修饰活角质形成细胞中的 E7 蛋白。
T13408 ZK824190

Others; Serine Protease Others; Proteases/Proteasome
ZK824190 是具有口服活性尿激酶型纤溶酶原激活剂 (uPA) 选择性抑制剂,对 uPA,tPA 和 Plasmin 的IC50分别为 237,1600 和 1850 nM。ZK824190在多发性硬化症中有研究价值。
T13257 Upamostat

PAI-1; Serine/threonin kinase; Serine Protease Cell Cycle/Checkpoint; Metabolism; Proteases/Proteasome
Upamostat 是一种丝氨酸蛋白酶抑制剂,也是一种具有口服活性的 WX-UK1 前药,是一种尿激酶型纤溶酶原激活剂 (uPA) 抑制剂。
T8362 Benzamidine hydrochloride

Benzamidine HCl,苄脒盐酸盐

Serine/threonin kinase; Serine Protease Cell Cycle/Checkpoint; Metabolism; Proteases/Proteasome
Benzamidine hydrochloride (Benzamidine HCl) 是可逆的胰蛋白酶样丝氨酸蛋白酶 (trypsin-like serine proteases) 竞争性抑制剂,对 uPA、类胰蛋白酶、胰蛋白酶和 Xa 因子作用的Ki 分别为 97 µM、20 µM、21 µM 和 110 µM。
T9920 Evolocumab

Others Others
Evolocumab 是人源化单克隆抗体PCSK9的抑制剂。它与循环的 PCSK9 蛋白结合,使得PCSK9与 LDLR 结合受到抑制。它可用研究于高胆固醇血症以及动脉粥样硬化性心血管疾病的研究。
T6370 AEBSF hydrochloride

AEBSF HCl,Pefabloc SC

Thrombin; Serine Protease; Influenza Virus Microbiology/Virology; Proteases/Proteasome
AEBSF hydrochloride (Pefabloc SC) 是一种丝氨酸蛋白酶的不可逆抑制剂。
T14358 Avoralstat

BCX4161

Others Others
Avoralstat (BCX4161) 是血浆激肽释放酶(PKK)抑制剂,具有口服活性,可用于遗传性血管性水肿的研究。
T4524 SBC-110736

SBC110736

Others; Serine/threonin kinase Cell Cycle/Checkpoint; Metabolism; Others
SBC-110736 是一种蛋白转化酶枯草杆菌蛋白酶 9 型 (PCSK9) 抑制剂。
T8645 PF-06446846

Others Others
PF-06446846 是口服有活性的 PCSK9抑制剂。它能够在密码子区域附近阻断 80S ribosome,选择性地直接抑制 PCSK9 的翻译。
T5456 WNK-IN-11

Allosteric WNK Kinase Inhibitor

Serine/threonin kinase Cell Cycle/Checkpoint; Metabolism
WNK-IN-11 (Allosteric WNK Kinase Inhibitor) 是(WNK)激酶的变构抑制剂,能够抑制 WNK1 (IC50:4 nM) 。
T8676 FOY 251

Others; Serine/threonin kinase; SARS-CoV Cell Cycle/Checkpoint; Metabolism; Microbiology/Virology; Others
FOY 251 是一种蛋白酶抑制剂,是具有抗蛋白水解活性的 Camostate 代谢物,能抑制 SARS-CoV-2 的感染。
T9276 SBC-115337

Others; Serine/threonin kinase Cell Cycle/Checkpoint; Metabolism; Others
SBC-115337 是苯并呋喃化合物,也是 PCSK9抑制剂 (IC50:0.5 μM) 。
T2626 SBC-115076

SBC115076

Others; Serine/threonin kinase Cell Cycle/Checkpoint; Metabolism; Others
SBC-115076 是前蛋白转化酶枯草杆菌蛋白酶/ kexin 9型(PCSK9)抑制剂。其中PCSK9 是一种前蛋白转化酶,在 LDL 受体代谢中的重要物质。
T3359 Aprotinin

抑酶肽,抑肽酶,Bovine Pancreatic Trypsin Inhibitor,Traskolan,Antilysin

Others; Serine Protease; Influenza Virus; Proteasome Microbiology/Virology; Others; Proteases/Proteasome; Ubiquitination
Aprotinin (Traskolan) 是分离自牛肺的一种广谱丝氨酸蛋白酶抑制剂,可抑制多种不同酯酶和蛋白酶的活性。
T31206 Darexaban

YM 150,Darexaban, Tanexaban,YM150

Factor Xa Metabolism
Darexaban (Tanexaban, YM-150) 是选择性的、口服具有活力的 Xa 因子 (FXa) 抑制剂,IC50=54.6 nM。它对其他相关丝氨酸蛋白酶(如胰蛋白酶、凝血酶和激肽释放酶)具有高选择性。它具有抗凝和抗血栓形成作用。
T2392 Nafamostat mesylate

甲磺酸萘莫司他,FUT-175

Apoptosis; Serine/threonin kinase; SARS-CoV; Serine Protease Apoptosis; Cell Cycle/Checkpoint; Metabolism; Microbiology/Virology; Proteases/Proteasome
Nafamostat mesylate (FUT-175) 是一种广谱丝氨酸蛋白酶抑制剂,血管舒缓素抑制剂,能抑制血液凝固。它通过降低颗粒酶活性和 CTL 细胞溶解抑制T 细胞自身反应活性,可抑制SARS-CoV-2 的激活。它还是潜在的补体抑制剂。
T19763 Cetraxate hydrochloride

DV-1006,DV 1006,Cetraxate HCl,盐酸西曲酸酯,DV1006

Serine/threonin kinase Cell Cycle/Checkpoint; Metabolism
Cetraxate hydrochloride (DV10062) 是一种有效的顶体蛋白酶 (acrosomal proteinase acrosin) 抑制剂,Ki 和 IC50分别为 0.94 μM 和 3.3 μM。它是一种口服有活性的抗溃疡试剂 (anti-ulcer),具有粘膜保护作用,可用于研究胃溃疡。
T8936 Proteinase K

proteinase K for tritirachium album,Protease K,蛋白酶 K

Others Others
Proteinase K (proteinase K for tritirachium album) 是一种非特异性丝氨酸蛋白酶,可用于蛋白消化。它在有 SDS 或尿素存在的情况下,在很大 pH 值 (4-12)、盐浓度和温度单位内均有活性。
T2391 Camostat mesylate

FOY-S980,甲磺酸卡莫司他,FOY305,Camostat mesilate

Serine/threonin kinase; SARS-CoV; Sodium Channel Cell Cycle/Checkpoint; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology
Camostat mesylate (FOY-S980) 是口服活性合成的丝氨酸蛋白酶抑制剂,用于慢性胰腺炎。它是TMPRSS2的抑制剂,对SARS-CoV-2具有抗病毒活性。它抑制前列腺素、胰蛋白酶和苦参多糖的活性。
T4317 PF 429242

NPC1L1; Lipid Membrane transporter/Ion channel; Metabolism
PF 429242 是甾醇调节元件结合蛋白 (SREBP) 位点 1 蛋白酶的竞争性抑制剂 (IC50 = 0.175 μM)。它对位点 1 蛋白酶对一组丝氨酸蛋白酶具有选择性。 PF-429242 抑制 CHO 细胞中胆固醇的合成速率 (IC50 = 0.53 μM)。
T25218 CE-2072

CE2072,CE 2072

CE-2072 is a synthetic host serine proteases inhibitor.
T37019 p-APMSF (hydrochloride)

p-APMSF is an irreversible inhibitor of serine proteases with Ki values of 1.02, 1.18, 1.5, and 1.54 μM for bovine trypsin, human thrombin, bovine plasmin, and bovine Factor Xa, respectively. It is selective for these proteases over bovine chymotrypsin and acetylcholinesterase.
T78409 Boc-Val-Pro-Arg-MCA hydrochloride

Boc-Val-Pro-Arg-MCA HCl

Boc-Val-Pro-Arg-MCA hydrochloride (Boc-Val-Pro-Arg-MCA HCl) 为测定胰蛋白酶样丝氨酸蛋白酶 (trypsin-like serine proteases) 活性的敏感荧光底物。
T14555 BI-1230

HCV Protease Microbiology/Virology; Proteases/Proteasome
BI-1230 is a potent inhibitor of HCV NS3 protease, exhibiting efficacy in the low nanomolar range, and notably suppresses viral replication. This compound demonstrates high selectivity, distinguishing effectively between other serine/cysteine proteases. Additionally, BI-1230 exhibits favorable pharmacokinetic (PK) properties[1].
T77221 Benzenecarboximidamide, hydrochloride, hydrate (1:1:x)

Benzenecarboximidamide, hydrochloride, hydrate (1:1:x) (Benzamidine hydrochloride hydrate) 是一种可逆的竞争性胰蛋白酶样丝氨酸蛋白酶 (trypsin-like serine proteases) 抑制剂,对 Tryptase、Trypsin、uPA、Factor Xa、Thrombin 和 tPA 的Ki 值分别为 20、21、97、110、320 和 750 μM。
T26202 SP-Chymostatin B

alpha-Mapi

SP-Chymostatin B is a potent inhibitor of many proteases, including chymotrypsin, papain, chymotrypsin-like serine proteinases, chymases, and lysosomal cysteine proteinases. It weakly inhibits human leucocyte elastase. It is effective at a final concentra
TP1013 N-CBZ-Phe-Arg-AMC

Z-FR-AMC

N-CBZ-Phe-Arg-AMC (Z-FR-AMC) is a substrate for serine proteases, including cathepsins, kallikrein and plasmin. Absorption/emission of substrate = 330/390 nm (weak fluorescence); absorption/emission of end product (AMC) = 342/441 nm (strong fluorescence).
T80094 Dansyl-Glu-Gly-Arg-Chloromethylketone

Dansyl-Glu-Gly-Arg-Chloromethylketone,一种蛋白酶抑制剂,特异性针对丝氨酸/苏氨酸蛋白酶。此化合物有效抑制活化猪因子IX。
T74390 VD2173

VD2173 是一种HGF 激活丝氨酸蛋白酶的侧链环化大环肽抑制剂。VD2173 有效抑制matriptase 和hepsin。VD2173 可用于肺癌的研究。
T39029 APC-6860

APC-6860 is a trypsin-like serine proteases inhibitor with k i values of 0.21, 0.44, 1.5, 16.8, 20, 30 μM for uPA, trypsin, tryptase, tPA, thrombin and factor Xa, respectively. APC-6860 has a selectivity ratio for tPA versus uPA of 80. APC-6860 has k i values of 0.1, 0.082 μM for human and murine urokinases, respectively. APC-6860 can be used for the research of cancer.
T81711 N-Acetyl-DL-phenylalanine β-naphthyl ester

N-Acetyl-DL-phenylalanine β-naphthyl ester 为一芳香族氨基酸酯,用作糜蛋白酶及微生物丝氨酸蛋白酶(例如枯草杆菌蛋白酶)的显色底物。
T36943 Aminopeptidase N Inhibitor

Aminopeptidase N (AP-N) inhibitor is a reversible inhibitor of AP-N/CD13 (IC50 = 25 μM). It is selective for AP-N/CD13 over matrix metalloproteinase-9 (MMP-9), angiotensin converting enzyme (ACE), neutral endopeptidase (NEP), γ-glutamyl transpeptidase, and the serine proteases dipeptidyl peptidase 4 (DPP-4) and cathepsin G at a concentration of 1 mM. AP-N inhibitor is non-cytotoxic to U937 cells at a concentration of 100 μM.
T39035 FXIa-IN-6

FXIa-IN-6 是一种有效的 FXIa 抑制剂,对大多数相关丝氨酸蛋白酶具有选择性(Ki= 0.3 nM)。FXIa-IN-6 还在多个临床前物种中展示了出色的药代动力学 (PK) 特性(高口服生物利用度和低清除率)。
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。
T37861 Talabostat

Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8/9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9,...

化合物

IPR-803
Cat.No: T11666
Synonym:
Target: Serine/threonin kinase
R-IMPP
Cat.No: T4058
Synonym:
Target: Others, Serine/threonin kinase
WNK463
Cat.No: T7017
Synonym:
Target: Serine/threonin kinase
Bradykinin
Cat.No: TP1277
Synonym: 缓激肽
Target: Endogenous Metabolite, Bradykinin Receptor
BioE-1115
Cat.No: T10547
Synonym:
Target: Serine/threonin kinase, Casein Kinase
LSP-249
Cat.No: T11885
Synonym:
Target: Others
TPCK
Cat.No: T8350
Synonym:
Target: Proteasome
ZK824190
Cat.No: T13408
Synonym:
Target: Others, Serine Protease
Upamostat
Cat.No: T13257
Synonym:
Target: PAI-1, Serine/threonin kinase, Serine Protease
Benzamidine hydrochloride
Cat.No: T8362
Synonym: Benzamidine HCl,苄脒盐酸盐
Target: Serine/threonin kinase, Serine Protease
Evolocumab
Cat.No: T9920
Synonym:
Target: Others
AEBSF hydrochloride
Cat.No: T6370
Synonym: AEBSF HCl,Pefabloc SC
Target: Thrombin, Serine Protease, Influenza Virus
Avoralstat
Cat.No: T14358
Synonym: BCX4161
Target: Others
SBC-110736
Cat.No: T4524
Synonym: SBC110736
Target: Others, Serine/threonin kinase
PF-06446846
Cat.No: T8645
Synonym:
Target: Others
WNK-IN-11
Cat.No: T5456
Synonym: Allosteric WNK Kinase Inhibitor
Target: Serine/threonin kinase
FOY 251
Cat.No: T8676
Synonym:
Target: Others, Serine/threonin kinase, SARS-CoV
SBC-115337
Cat.No: T9276
Synonym:
Target: Others, Serine/threonin kinase
SBC-115076
Cat.No: T2626
Synonym: SBC115076
Target: Others, Serine/threonin kinase
Aprotinin
Cat.No: T3359
Synonym: 抑酶肽,抑肽酶,Bovine Pancreatic Trypsin Inhibitor,Traskolan,Antilysin
Target: Others, Serine Protease, Influenza Virus, Proteasome
Darexaban
Cat.No: T31206
Synonym: YM 150,Darexaban, Tanexaban,YM150
Target: Factor Xa
Nafamostat mesylate
Cat.No: T2392
Synonym: 甲磺酸萘莫司他,FUT-175
Target: Apoptosis, Serine/threonin kinase, SARS-CoV, Serine Protease
Cetraxate hydrochloride
Cat.No: T19763
Synonym: DV-1006,DV 1006,Cetraxate HCl,盐酸西曲酸酯,DV1006
Target: Serine/threonin kinase
Proteinase K
Cat.No: T8936
Synonym: proteinase K for tritirachium album,Protease K,蛋白酶 K
Target: Others
Camostat mesylate
Cat.No: T2391
Synonym: FOY-S980,甲磺酸卡莫司他,FOY305,Camostat mesilate
Target: Serine/threonin kinase, SARS-CoV, Sodium Channel
PF 429242
Cat.No: T4317
Synonym:
Target: NPC1L1, Lipid
CE-2072
Cat.No: T25218
Synonym: CE2072,CE 2072
Target:
p-APMSF (hydrochloride)
Cat.No: T37019
Synonym:
Target:
Boc-Val-Pro-Arg-MCA hydrochloride
Cat.No: T78409
Synonym: Boc-Val-Pro-Arg-MCA HCl
Target:
BI-1230
Cat.No: T14555
Synonym:
Target: HCV Protease
Benzenecarboximidamide, hydrochloride, hydrate (1:1:x)
Cat.No: T77221
Synonym:
Target:
SP-Chymostatin B
Cat.No: T26202
Synonym: alpha-Mapi
Target:
N-CBZ-Phe-Arg-AMC
Cat.No: TP1013
Synonym: Z-FR-AMC
Target:
Dansyl-Glu-Gly-Arg-Chloromethylketone
Cat.No: T80094
Synonym:
Target:
VD2173
Cat.No: T74390
Synonym:
Target:
APC-6860
Cat.No: T39029
Synonym:
Target:
N-Acetyl-DL-phenylalanine β-naphthyl ester
Cat.No: T81711
Synonym:
Target:
Aminopeptidase N Inhibitor
Cat.No: T36943
Synonym:
Target:
FXIa-IN-6
Cat.No: T39035
Synonym:
Target:
Cathepsin C-IN-5
Cat.No: T62494
Synonym:
Target:
Talabostat
Cat.No: T37861
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
TN2082 Pinostrobin

Beta Amyloid; IL Receptor; Serine/threonin kinase; TNF Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation; Metabolism; Neuroscience
Pinostrobin 是一种 PCSK9抑制剂,可抑制 PCSK9 的催化活性。它是能够在多种植物中发现的黄酮类化合物,并具有抗氧化,抗炎,抗癌和神经保护作用。它是有前景的胆固醇调节和脂质管理剂。
T5S0689 Demethylwedelolactone

去甲蟛蜞菊内酯,去甲基蟛蜞内酯

Serine Protease Proteases/Proteasome
Demethylwedelolactone 是一种分离自 Eclipta alba 中的 coumestan 天然产物。它能抑制乳腺癌细胞的移动和侵袭,是一种有效的trypsin 抑制剂(IC50:3.0 μM)。

天然产物

Pinostrobin
Cat.No: TN2082
Synonym:
Target: Beta Amyloid, IL Receptor, Serine/threonin kinase, TNF
Demethylwedelolactone
Cat.No: T5S0689
Synonym: 去甲蟛蜞菊内酯,去甲基蟛蜞内酯
Target: Serine Protease
TargetMol Loading
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