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29

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T6015 Cathepsin Inhibitor 1

Cysteine Protease Proteases/Proteasome
Cathepsin inhibitor 1Cathepsin 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)。
TP1015 NFAT Inhibitor

VIVIT peptide

Others Others
NFAT Inhibitor (VIVIT peptide) 是NFAT 的细胞渗透性肽抑制剂,能够选择性抑制钙调磷酸酶介导的NFAT 脱磷酸作用。
T3088 N-Ethylmaleimide

1-Ethyl-1H-pyrrole-2,5-dione,n-乙基马来酰亚胺,Ethylmaleimide,NEM

Cysteine Protease; DUB Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Proteases/Proteasome; Ubiquitination
N-Ethylmaleimide (NEM) 是烷基化自由巯基的试剂, 是一种半胱氨酸蛋白酶抑制剂,用于实验生化研究。它也是一种去泛素化酶抑制剂,特异性抑制线粒体中的磷酸盐转运。
T60812 Cathepsin X-IN-1

Cysteine Protease Proteases/Proteasome
Cathepsin X-IN-1 (compound 25) 降低人前列腺癌细胞 PC-3 的迁移且具有较低的细胞毒性,它是组织蛋白酶 X 的有效抑制剂 (IC50 = 7.13 μM)。
T6035 Odanacatib

奥达卡替,奥当卡替,MK-0822

Cysteine Protease Proteases/Proteasome
Odanacatib 是组织蛋白酶K(人/兔)的选择性抑制剂,IC50分别为0.2 nM 和 1 nM。
T80105 Z-Phe-Phe-Diazomethylketone

Z-Phe-Phe-Diazomethylketone 为cathepsin L 特异性抑制剂。
T62659 Cathepsin C-IN-4

Cathepsin C-IN-4 是一种组织蛋白酶 C (Cat C) 的有效抑制剂 (IC50: 65.6 nM)。Cathepsin C-IN-4 对 THP-1 (IC50: 203.4 nM)和 U937 (IC50: 177.6 nM) 细胞具有抑制作用。
T81265 RKLLW-NH2

RKLLW-NH2为一种组织蛋白酶L抑制剂。
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。
T80740 Z-FG-NHO-Bz

Z-FG-NHO-Bz 为选择性针对组织蛋白酶(cathepsin)的抑制剂。
T72569 Cathepsin L/S-IN-1

CathepsinL/S-IN-1Cathepsin 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。
T63854 Cathepsin C-IN-3

Cathepsin C-IN-3 是组织蛋白酶 C (Cat C) 的有效抑制剂 (IC50: 61.79 nM),也能抑制 THP-1 细胞 (IC50: 101.5 nM) 和 U937 细胞 (IC50: 86.5 nM)。
T14187 ALLM

Calpain inhibitor II

Others Others
ALLM (Calpain inhibitor II), a potent calpain and cathepsin protease inhibitor, not only prevents neuronal cell death but also enhances chronic neurological function following spinal cord injury (SCI)[1][2].
T60838 Gü2602

Gü2602 可抑制组织蛋白酶 K 酶原的自催化激活,它是组织蛋白酶 K (CatK) 的可逆抑制剂,其对成熟 CatK (mCatK) 的 Ki 值为 0.013 nM。
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。
TP2161 Z-WEHD-FMK

Caspase Apoptosis; Proteases/Proteasome
Z-WEHD-FMK is a cell-permeable and irreversible inhibitor of caspase-1/5. It also shows a robust inhibitory effect on cathepsin B activity (IC50: 6 μM).
T61413 1303

1303 is a highly potent and reversible inhibitor of Cathepsin K (CatK), with a Ki value of 0.91 nM for mature CatK (mCatK). This compound effectively suppresses the autocatalytic activation of the CatK zymogen [1].
T78185 Ac-PLVE-FMK

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

Others Others
Ac-PLVE-FMK(Ac-Pro-Leu-Val-Glu(OMe)-CH2F),一种四肽基m-FMK化合物,具有Cats抑制作用,常用于癌症研究。
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.()
T79496 Cathepsin C-IN-6

CathepsinC-IN-6 (compound 2) 是基于E-64c-肼的cathepsin C抑制剂,展现抗炎活性。能有效抑制中性粒细胞弹性蛋白酶的激活,对于中性粒细胞浓度高的炎症性疾病(例如慢性阻塞性肺疾病)有潜在治疗作用。
T11466 GSK-2793660

Others Others
GSK-2793660 是一种具有口服活性并且不可逆的组织蛋白酶 C (Cathepsin C;CTSC) 抑制剂。GSK-2793660 是一种生物活性肽,可用于支气管扩张的研究。
T76599 Ac-Leu-Val-Lys-Aldehyde

Ac-Leu-Val-Lys-Aldehyde 是有效的组织蛋白酶 B (cathepsin B) 抑制剂,其 IC50 值为 4 nM。该化合物能显着降低喹啉酸引起的纹状体细胞死亡,并促使 LC3-II 积累。
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。
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.
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。
T21949 Calpain Inhibitor XII

(Rac)-Calpain Inhibitor XII是一种可逆的,选择性抑制钙蛋白酶I(calpain I; μ-calpain)的化合物,具有19 nM的Ki值。其对钙蛋白酶II(calpain II; m-calpain; Ki=120 nM)和组织蛋白酶B(cathepsin B; Ki=750 nM)显示出较低的抑制亲和力。(Rac)-Calpain Inhibitor XII用于研究钙蛋白酶在多种生理过程中的角色,如嗜中性粒细胞趋化性、神经元信号传导和心脏对损伤的响应。
T80653 Larixol

(+)-Larixol

Akt Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
Larixol作为一种fMLP抑制剂,在免疫调节作用上,能够抑制Src激酶、ERK1/2、p38以及AKT的磷酸化信号。它能够通过干扰fMLP受体Gi蛋白的βγ亚基与下游分子之间的作用,抑制fMLP引发的呼吸爆发。此外,Larixol可有效降低由fMLP (0.1 μM) 诱导的超氧阴离子生成(IC50: 1.98 μM)、组织蛋白酶G的释放(IC50: 2.76 μM)及趋化反应,有助于缓解中性粒细胞的过度激活,减少炎症或组织损伤。Larixol衍生物对FSGS相关TRPC6功能突变有显著的抑制效果。

化合物

Cathepsin Inhibitor 1
Cat.No: T6015
Synonym:
Target: Cysteine Protease
NFAT Inhibitor
Cat.No: TP1015
Synonym: VIVIT peptide
Target: Others
N-Ethylmaleimide
Cat.No: T3088
Synonym: 1-Ethyl-1H-pyrrole-2,5-dione,n-乙基马来酰亚胺,Ethylmaleimide,NEM
Target: Cysteine Protease, DUB
Cathepsin X-IN-1
Cat.No: T60812
Synonym:
Target: Cysteine Protease
Odanacatib
Cat.No: T6035
Synonym: 奥达卡替,奥当卡替,MK-0822
Target: Cysteine Protease
Z-Phe-Phe-Diazomethylketone
Cat.No: T80105
Synonym:
Target:
Cathepsin C-IN-4
Cat.No: T62659
Synonym:
Target:
RKLLW-NH2
Cat.No: T81265
Synonym:
Target:
Z-FG-NHO-BzOME
Cat.No: T80739
Synonym:
Target:
Z-FG-NHO-Bz
Cat.No: T80740
Synonym:
Target:
Cathepsin L/S-IN-1
Cat.No: T72569
Synonym:
Target:
Cathepsin C-IN-3
Cat.No: T63854
Synonym:
Target:
ALLM
Cat.No: T14187
Synonym: Calpain inhibitor II
Target: Others
Gü2602
Cat.No: T60838
Synonym:
Target:
Ac-VLPE-FMK
Cat.No: T78186
Synonym: Ac-Val-Leu-Pro-Glu(OMe)-CH2F
Target:
Z-FY-CHO
Cat.No: T41236
Synonym:
Target:
Z-WEHD-FMK
Cat.No: TP2161
Synonym:
Target: Caspase
1303
Cat.No: T61413
Synonym:
Target:
Ac-PLVE-FMK
Cat.No: T78185
Synonym: Ac-Pro-Leu-Val-Glu(OMe)-CH2F
Target: Others
SSAA09E1
Cat.No: T36942
Synonym: SSAA09E1
Target:
Cathepsin C-IN-6
Cat.No: T79496
Synonym:
Target:
GSK-2793660
Cat.No: T11466
Synonym:
Target: Others
Ac-Leu-Val-Lys-Aldehyde
Cat.No: T76599
Synonym:
Target:
MeOSuc-AAPV-CMK
Cat.No: T78633
Synonym: Elastase Inhibitor III
Target:
Aminopeptidase N Inhibitor
Cat.No: T36943
Synonym:
Target:
Cathepsin C-IN-5
Cat.No: T62494
Synonym:
Target:
Acetyl-Calpastatin(184-210)(human) TFA
Cat.No: T75794
Synonym:
Target:
Calpain Inhibitor XII
Cat.No: T21949
Synonym:
Target:
Larixol
Cat.No: T80653
Synonym: (+)-Larixol
Target: Akt
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。
T3417 Amentoflavone

Didemethyl-ginkgetin,穗花杉双黄酮,Amenthoflavone,3',8''-Biapigenin

Apoptosis; P450; Phospholipase; Reactive Oxygen Species; Opioid Receptor; COX; Antibacterial; RSV; Antifungal Apoptosis; Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience; NF-κB
Amentoflavone (3',8''-Biapigenin) 是一种具有很多生物活性的双黄酮类天然产物,有抗炎、抗氧化和神经保护等作用。

天然产物

Aurantiamide acetate
Cat.No: TJS2216
Synonym: 金色酰胺醇酯,Asperglaucide
Target: Cysteine Protease
Amentoflavone
Cat.No: T3417
Synonym: Didemethyl-ginkgetin,穗花杉双黄酮,Amenthoflavone,3',8''-Biapigenin
Target: Apoptosis, P450, Phospholipase, Reactive Oxygen Species, Opioid Receptor, COX, Antibacterial, RSV, Antifungal
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