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12
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T73594 |
Chymotrypsin
Chymotrypsin A |
Serine/threonin kinase | Cell Cycle/Checkpoint; Metabolism |
Chymotrypsin (Chymotrypsin A) 是胰腺产生的丝氨酸蛋白酶,可切割芳香族氨基酸羧基侧的蛋白质链。 | |||
T23233L |
RETF-4NA acetate
RETF-4NA acetate(1160928-63-1 free base) |
Others | Others |
RETF-4NA acetate 是一种敏感的、特异性的糜蛋白酶底物。 | |||
T6941 |
PI-1840
PI 1840 |
PARP; Proteasome | Chromatin/Epigenetic; DNA Damage/DNA Repair; Proteases/Proteasome; Ubiquitination |
PI-1840 是一种高效的、选择性的蛋白酶体chymotrypsin-like (CT-L)抑制剂,IC50=27nM。 | |||
T1795 |
Carfilzomib
卡非佐米,PR-171 |
Apoptosis; Proteasome; Autophagy | Apoptosis; Autophagy; Proteases/Proteasome; Ubiquitination |
Carfilzomib (PR-171) 是一种蛋白酶体抑制剂,与 20S 蛋白酶体的糜蛋白酶不可逆结合。Carfilzomib 具有抗肿瘤活性,可以用于治疗多发性骨髓瘤。 | |||
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。 | |||
T0372 |
Gabexate mesylate
甲磺酸加贝酯,FOY |
Factor Xa; Serine Protease; Proteasome | Metabolism; Proteases/Proteasome; Ubiquitination |
Gabexate mesylate (FOY) 是一种非抗原的类胰蛋白酶丝氨酸蛋白酶抑制剂。 | |||
T7016 |
VR23
|
Apoptosis; Proteasome; Caspase | Apoptosis; Proteases/Proteasome; Ubiquitination |
VR23 是一种蛋白酶体抑制剂,对胰蛋白酶样蛋白酶体、糜蛋白酶样蛋白酶体和半胱天冬酶样蛋白酶体的 IC50 分别是1 nM、50-100 nM 和3 μM。 | |||
T21617 |
MG-115
Z-LL-Nva-CHO |
Proteasome | Proteases/Proteasome; Ubiquitination |
MG-115 (Z-LL-Nva-CHO) 是一种有效且可逆的蛋白酶体抑制剂,对20S 和26S 蛋白酶体的 Ki 值分别为 21 nM 和 35 nM。MG-115 特异性抑制蛋白酶体的胰凝乳蛋白酶样活性,诱导 p53 依赖性细胞凋亡。 | |||
T2122 |
Ixazomib
艾沙佐米,MLN2238 |
Proteasome; Caspase; Autophagy | Apoptosis; Autophagy; Proteases/Proteasome; Ubiquitination |
Ixazomib (MLN2238) 含硼肽蛋白酶体抑制剂(PI),可抑制 20S 蛋白酶体的糜蛋白酶样蛋白水解 (β5) 位点,IC50为 3.4 nM,Ki 为 0.93 nM。它还抑制半胱天冬酶样 (β1) 和胰蛋白酶样 (β2) 蛋白水解位点,IC50值为 31和3500 nM。 | |||
TP1832 |
Gluten Exorphin C
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
Gluten exorphin C 是来源于谷朊粉的阿片肽。在 GPI 和 MVD 检测中,抑制 μ 阿片和 δ 阿片活性,IC50值分别为 40 和13.5 μM。 | |||
T36352 |
Suc-Leu-Tyr-AMC
|
||
Suc-Leu-Tyr-AMC 是钙蛋白酶 I 和 II 以及木瓜蛋白酶(另一种半胱氨酸蛋白酶)的荧光底物,用于测量 20S 蛋白酶体的糜蛋白酶样肽酶活性(Ex-max:360 nm;Em-max:460 nm)。Suc-Leu-Tyr-AMC 也能被大肠杆菌的 Ti 蛋白酶裂解。 | |||
T14529 |
Bentiromide
|
Others | Others |
Bentiromide 是一种可被胰腺分泌的胰凝乳蛋白酶分解的多肽。Bentiromide 通过胰凝乳蛋白酶功能的体外试验确认胰腺外分泌功能。 | |||
T63321 |
20S Proteasome activator 1
|
Proteasome | Proteases/Proteasome; Ubiquitination |
20S Proteasome activator 1 是一种 20S 蛋白酶激活剂,对胰蛋白酶样位点、胰凝乳蛋白酶样位点和半胱天冬酶位点的 IC50 分别为 0.3 μM、0.7 μM 和 1.8 μM。20S Proteasome activator 1 通过在细胞系统中翻译来防止致病性 α-synuclein A53T 突变体积累从而减少疾病发生的概率。20S Proteasome activator 1 可用于研究神经退行性疾病。 | |||
T26297 |
Tryptophanamide
S-Tryptophanamide |
||
Tryptophanamide is a chymotrypsin inhibitor. | |||
T76157 |
Chymotrypsinogen
|
||
Chymotrypsinogen 是Chymotrypsin 的无活性前体。Chymotrypsinogen 是一种由胰腺产生的丝氨酸蛋白酶 (serine protease)。 | |||
T25280 |
Cyanopeptolin 954
Cyanopeptolin-954,Cyanopeptolin954 |
||
Cyanopeptolin 954 is a chlorine-containing Microcystis aeruginosa NIVA Cya 43 chymotrypsin Inhibitor. | |||
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 | |||
T68534 | FK-448 methanesulfonate | ||
FK-448 methanesulfonate is a chymotrypsin inhibitor that has been shown to affect intestinal absorption of insulin in rats and dogs . | |||
T37418 |
Z-LLL-AMC
|
||
Z-LLL-AMC is a fluorogenic substrate for the chymotrypsin-like activity of the 26S proteasome or 20S proteolytic core. Chymotrypsin-like activity can be quantified by fluorescent detection of free AMC (also known as 7-amino-4-methylcoumarin), which is excited at 340-360 nm and emits at 440-460 nm. Z-LLL-AMC is typically used in cell lysates after experimental treatment. | |||
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. | |||
T36962 |
MMP Inhibitor I (trifluoroacetate salt)
|
||
MMP inhibitor I is a peptide inhibitor of matrix metalloproteinase-1 (MMP-1), MMP-2, and MMP-3 (IC50s = 1.3, 30, and 150 μM, respectively). It is selective for MMP-1, MMP-2, and MMP-3 over the proteases thermolysin, urease, trypsin, α-chymotrypsin, plasmin, and elastase at concentrations up to 4 mM. | |||
TP1308 |
Suc-Leu-Leu-Val-Tyr-AMC
|
||
Suc-Leu-Leu-Val-Tyr-AMC is a fluorescent substrate for the 20S proteasome, other chymotrypsin-like proteases. | |||
T36338 |
AAF-CMK (trifluoroacetate salt)
|
||
Tripeptidyl peptidase II (TPPII) is a serine peptidase of the subtilisin-type which removes tripeptides from the free NH2 terminus of oligopeptides. AAF-CMK is an irreversible inhibitor of TPPII commonly used at 10-100 μM. It does not significantly interfere with the chymotrypsin-like activity of the proteasome. AAF-CMK also inhibits bleomycin hydrolase and puromycin-sensitive aminopeptidase when used at 50 μM. | |||
T80102 |
Z-Leu-Leu-Tyr-COCHO
|
Proteasome | Proteases/Proteasome; Ubiquitination |
Z-Leu-Leu-Tyr-COCHO为胰凝乳蛋白酶样活性抑制剂,具有Ki值为3.0 nM的高效性。 | |||
T76621 |
Suc-Ala-Ala-Pro-Phe-SBzl
|
||
Suc-Ala-Ala-Pro-Phe-SBzl 是一种化合物,可以作为大鼠小肠肥大细胞蛋白酶(RMCP I)、大鼠骨骼肌肥大细胞蛋白酶(RMCP II)和胰凝乳蛋白酶(Chymotrypsin)的底物。此外,Suc-Ala-Ala-Pro-Phe-SBzl 能够被甘氨酸(R208G)水解。 | |||
T14529L |
Bentiromide acetate
Bentiromide acetate(37106-97-1 Free base) |
Others | Others |
Bentiromide acetate 是一种肽,用于外分泌胰腺功能不全的筛选试验和监测补充胰腺治疗的充分性。它被胰酶胰凝乳蛋白酶分解,生成对氨基苯甲酸(PABA)。 | |||
T76231 | Cyclotheonellazole A | ||
Cyclotheonellazole A为一天然大环肽类化合物,对弹性蛋白酶具显著的抑制效果(IC50=0.034 nM),且对糜蛋白酶亦有抑制作用,IC50值达0.62 nM。 | |||
T62080 |
GSK3494245
|
||
GSK3494245 (DDD01305143) 是一种有效的、选择性的、口服具有活力的、可在夹在 β4 和 β5 亚基之间的位点结合寄生虫蛋白酶体 (proteasome) 的糜蛋白酶样活性抑制剂,能够作用于 WTL.donovani 蛋白酶体,其 IC50 值为 0.16μM。GSK3494245 表现出良好的生物安全特性。GSK3494245 对人蛋白酶体的糜蛋白酶样活性具有适当的抑制作用 (IC50: 26S=13 μM;富集的 THP-1 提取物 IC50=40 μM)。 | |||
T62479 |
3CPLro-IN-1
|
||
3CPLro-IN-1 (compound A17) 是一种有效的、口服具有活力的 SARS-CoV-2 3CLpro 抑制剂 (IC50: 5.65 μM)。3-糜蛋白酶样半胱氨酸蛋白酶 (3CLpro) 是一种病毒复制中不可或缺的蛋白质,是一种有吸引力的、对抗 COVID-19 的药物靶点。 | |||
T78407 |
Suc-Ala-Ala-Phe-AMC
|
||
Suc-Ala-Ala-Phe-AMC为一荧光胰凝乳蛋白酶底物,可遭肽链内切酶所水解。该化合物适用于顶体反应的体内测定及体外酶活性分析。 | |||
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 | |||
T70170 |
Milvexian TFA
|
||
Milvexian, also known as BMS-986177 and JNJ-70033093, is a blood coagulation factor XIa inhibitor. Milvexian demonstrated good selectivity over plasma kallikreinKi = 44 nM (400-fold selective), and chymotrypsinKi = 35 nM (318-fold selective). At a dose of 1.5 mg/kg, Milvexian exhibited an overall exposure of 1215 nM/h, low clearance of 10.3 mL/min/kg, and oral bioavailability of 32%. | |||
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... | |||
T74878 |
Enzyme-IN-1
|
||
Enzyme-IN-1(compound 1)为基于肽的N端亲核试剂(Ntn)水解酶抑制剂,特别针对20S蛋白酶体的糜胰蛋白酶样活性(CT-L)进行抑制,可能展现出抗炎特性。 | |||
T63760 |
3CPLro-IN-2
|
||
3CPLro-IN-2 是有效的、口服具有活力的 SARS-CoV-2 3CLpro 抑制剂 (IC50: 1.55 μM, Ki: 6.09 μM)。3-糜蛋白酶样半胱氨酸蛋白酶 (3CLpro) 是病毒复制中不可或缺的蛋白质,是有潜力的对抗 COVID-19 的药物靶点。 | |||
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。 | |||
T81372 |
Proteasome-activating peptide 1
|
||
Proteasome-activating peptide 1 是一种肽,其作用是提升胰凝乳蛋白酶样蛋白酶体(proteasome)的催化活性,有效增强体外及细胞培养环境下的蛋白质降解效率。此外,该肽能阻止肌萎缩侧索硬化症(Amyotrophic Lateral Sclerosis, ALS)细胞模型中蛋白质的过度聚集。 | |||
T78640 |
Z-LLF-CHO
Z-Leu-Leu-Phe-CHO |
Proteasome | Proteases/Proteasome; Ubiquitination |
Z-LLF-CHO(Z-Leu-Leu-Phe-CHO)为垂体多催化蛋白酶复合物所具有的胰凝乳蛋白酶样活性提供有效抑制,具有Ki值为460 nM。此外,Z-LLF-CHO同样作为NF-κB核转位的抑制剂。 | |||
T38363 |
MeOSuc-AAPV-pNA
|
||
Proteinase 3 (PR3, myeloblastin) is a polymorphonuclear leukocyte serine proteinase that degrades matrix proteins including fibronectin, laminin, vitronectin, and collagen type IV to generate antimicrobial peptides. Neutrophil elastase is a serine proteinase that is secreted by neutrophils during inflammation to destroy pathogens. Evaluating these enzymes is helpful to understanding inflammatory autoimmune processes. MeOSuc-AAPV-pNA is a highly sensitive peptide substrate that is hydrolyzed by b... | |||
T76243 |
Proteasome-activating peptide 1 TFA
|
||
Proteasome-activating peptide 1 TFA 是一种肽类蛋白酶体激活剂,能显著增强胰凝乳蛋白酶样蛋白酶体的催化活性,进而提升体外及培养环境中的蛋白质水解效率。此外,Proteasome-activating peptide 1 TFA 还能有效阻止肌萎缩侧索硬化症细胞模型内的蛋白质聚集现象。 | |||
T80735 |
Z-Gly-Pro-Phe-Leu-CHO
Z-GPFL-CHO |
Proteasome | Proteases/Proteasome; Ubiquitination |
Z-Gly-Pro-Phe-Leu-CHO(Z-GPFL-CHO)是一种具有高选择性和高效率的四肽醛类蛋白酶体抑制剂,优先抑制支链氨基酸(Ki为1.5 µM),对小中性氨基酸的Ki值为2.3 µM,胰凝乳蛋白酶样活性的Ki值为40.5 µM,对肽基-谷氨酰肽水解活性的IC50为3.1 µM。 | |||
T69288 |
CEP-7055
|
||
CEP-18770 is an orally bioavailable synthetic P2 threonine boronic acid inhibitor of the chymotrypsin-like activity of the proteasome, with potential antineoplastic activity. Proteasome inhibitor CEP 18770 represses the proteasomal degradation of a variety of proteins, including inhibitory kappaBalpha (IkappaBalpha), resulting in the cytoplasmic sequestration of the transcription factor NF-kappaB; inhibition of NF-kappaB nuclear translocation and transcriptional up-regulation of a variety of cel... | |||
T73986 | ONX-0914 TFA | ||
ONX-0914 (PR-957) TFA 为针对免疫蛋白酶体中的LMP7(低分子量多肽-7)的选择性抑制剂,LMP7为类糜蛋白酶亚单位。该化合物通过抑制细胞因子产生,减缓实验性关节炎进展,并已证实为分枝杆菌蛋白酶体的非竞争性不可逆抑制剂(Ki=5.2 μM)。此外,ONX-0914 TFA 能通过HSF-1介导的p-TEFb活化,激活潜伏的HIV-1。 | |||
T75394 | Picornain 3C | ||
Picornain 3C为发现于小核糖核酸病毒中的蛋白酶,具有切割非末端序列肽键的能力。该酶是丝氨酸肽酶胰凝乳蛋白酶与半胱氨酸肽酶木瓜蛋白酶中间产物,展示内肽酶活性。特别地,Picornain 3C选择性切割脊髓灰质炎病毒多聚蛋白中的Gln-Gly键,以及在其他小核糖核酸病毒中,Gln被Glu替代,Gly被Ser或Thr替代的情况下亦能切割。 | |||
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... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN1372 |
Alpha-Amyrin
alpha-Amyrenol,α-Amyrin,alpha-Amyrine,Viminalol,α-香树脂醇 |
P450; Serine Protease; ROS | Immunology/Inflammation; Metabolism; Proteases/Proteasome |
Alpha-Amyrin (alpha-Amyrine) 是一种具有抗肿瘤作用的胰蛋白酶和糜蛋白酶抑制剂。 alpha-Amyrin 可用于作为肝调节剂的研究。 | |||
T2O2730 |
L-Serine
(S)-Serine,L-丝氨酸,丝氨酸,serine,(-)-Serine,(S)-2-Amino-3-hydroxypropanoic acid |
Endogenous Metabolite | Metabolism |
L-Serine (serine) 是一种人体非必需氨基酸,它存在于许多蛋白质中,并且在功能上很重要。L-Serine 也存在于丝氨酸蛋白酶类的活性位点,包括胰蛋白酶和凝乳胰蛋白酶。 | |||
TN3228 |
7-Hydroxy-3-(4-hydroxybenzyl)chroman
|
Others | Others |
7-Hydroxy-3-(4-hydroxybenzyl)chroman shows moderate inhibitory activity against a chymotrypsin-like activity of the proteasome. | |||
T15638 |
K-252c
|
PKC | Chromatin/Epigenetic; Cytoskeletal Signaling |
K-252c is a staurosporine analog isolated from Nocardiopsis sp. and is a cell-permeable PKC inhibitor (IC50: 2.45 μM). K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase. K-252c causes apoptosis in human chronic myelogenous leukemia cancer cells. | |||
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。 | |||
TN3383 |
α-Amyrin palmitate
alpha-Amyrin palmitate |
PKA | Tyrosine Kinase/Adaptors |
alpha-Amyrin palmitate is antiarthritic in the adjuvant model of arthritis in rats. alpha-Amyrin palmitate is a potent non-competitive inhibitor of chymotrypsin (Ki=6 microM), it also shows weak cytotoxicity against the A2780 human ovarian cancer cell line. | |||
T10238 |
Aclacinomycin A hydrochloride
盐酸阿柔比星,Aclarubicin hydrochloride |
Proteasome | Proteases/Proteasome; Ubiquitination |
Aclacinomycin A (Aclarubicin) hydrochloride is a fluorescent molecule and the first described non-peptidic inhibitor showing discrete specificity for the CTRL (chymotrypsin-like) activity of the 20S proteasome. Aclacinomycin A hydrochloride is also a dual inhibitor of topoisomerase I and II. | |||
TN5655 | Broussonin B | ||
Broussonins A and B, new phytoalexins from diseased paper mulberry. Broussonin B can induce neurite outgrowth in PC-12 cells at concentration of 50 microg/ml, and show moderate inhibitory activities against a chymotrypsin-like activity of the proteasome.B | |||
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。 | |||
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。 | |||
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。 |