41
2
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,... |
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)。 |