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Proteases

Proteases

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VX-765 (Belnacasan)

Catalog No. A10984
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Caspase-1/4 抑制剂

VX-765 (Belnacasan)是一种新型的Caspase-1抑制剂，是一种控制两种细胞因子IL-1b和IL-18生成的酶。了解更多

Product Citations (7)

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- Arjun Thapa, .et al. Danger-associated molecular pattern molecules take unexpectedly a central stage in Nlrp3 inflammasome-caspase-1-mediated trafficking of hematopoietic stem/progenitor cells, Leukemia, 2021, 23 February
- Prenitha Mercy Ignatius Arokia Doss, .et al. Male sex chromosomal complement exacerbates the pathogenicity of Th17 cells in a chronic model of central nervous system autoimmunity, Cell Rep, 2021, Mar 9;34(10):108833 PMID: 33691111
- Joseph Flores, .et al. Pre-symptomatic Caspase-1 inhibitor delays cognitive decline in a mouse model of Alzheimer disease and aging, Nat Commun, 2020, Sep 11;11(1):4571 PMID: 32917871
- Joseph Flores, .et al. Caspase-1 inhibition alleviates cognitive impairment and neuropathology in an Alzheimer's disease mouse model, Nat Commun, 2018, 9: 3916 PMID: 30254377
- Mohamed F. Ali, .et al. Canonical Stimulation of the NLRP3 Inflammasome by Fungal Antigens Links Innate and Adaptive B-Lymphocyte Responses by Modulating IL-1β and IgM Production, Front Immunol, 2017, 8: 1504 PMID: 29170665
- García-Fernández A, .et al. Targeting inflammasome by the inhibition of caspase-1 activity using capped mesoporous silica nanoparticles, J Control Release, 2017, Feb 28;248:60-70 PMID: 28069553
- Jiujiu Yu, .et al. Inflammasome activation leads to Caspase-1-dependent mitochondrial damage and block of mitophagy, Proc Natl Acad Sci U S A, 2014, 111(43): 15514-15519 PMID: 25313054
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Z-VAD-FMK

Catalog No. A12373
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Pan Caspase 抑制剂

Z-VAD-FMK是一种细胞可渗透、不可逆的泛胱天蛋白酶抑制剂。体外抑制肿瘤细胞caspase加工和凋亡诱导(IC50 = 0.0015 - 5.8 mM)。活跃在体内。了解更多

Product Citations (30)

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- Ming-Chun Hung, .et al. AKT phosphorylation as a predictive biomarker for PI3K/mTOR dual inhibition-induced proteolytic cleavage of mTOR companion proteins in small cell lung cancer, Cell Biosci, 2022, 12: 122 PMID: 35918763
- Kaori Kanemaru, .et al. Plasma membrane phosphatidylinositol (4,5)-bisphosphate is critical for determination of epithelial characteristics, Nat Commun, 2022, May 9;13(1):2347 PMID: 35534464
- Chie Ishikawa, .et al. Exportin-1 is critical for cell proliferation and survival in adult T cell leukemia, Invest New Drugs, 2022, Aug;40(4):718-727 PMID: 35477814
- Aida Falgas, .et al. A diphtheria toxin-based nanoparticle achieves specific cytotoxic effect on CXCR4 + lymphoma cells without toxicity in immunocompromised and immunocompetent mice, Biomed Pharmacother, 2022, Jun;150:112940 PMID: 35421785
- Sumire Suzuki, .et al. Lysosome-targeted drug combination induces multiple organelle dysfunctions and non?canonical death in pancreatic cancer cells, Oncol Rep, 2022, Feb;47(2):40 PMID: 34958115
- Lina Y Abou Zeid, .et al. Caspase-mediated cleavage of miRNA processing proteins Drosha, DGCR8, Dicer, and TRBP2 in heat-shocked cells and its inhibition by HSP70 overexpression, Cell Stress Chaperones, 2022, Jan;27(1):11-25 PMID: 34719748
- Kosar Jabbari, .et al. Protein Ligands in the Secretome of CD36+ Fibroblasts Induce Growth Suppression in a Subset of Breast Cancer Cell Lines, Cancers (Basel), 2021, Sep 8;13(18):4521 PMID: 34572749
- Xiaoyue Deng, .et al. Setd1a Plays Pivotal Roles for the Survival and Proliferation of Retinal Progenitors via Histone Modifications of Uhrf1, Invest Ophthalmol Vis Sci, 2021, May 3;62(6):1 PMID: 33938913
- Liqun Zhao, .et al. Rictor, an essential component of mTOR complex 2, undergoes caspase-mediated cleavage during apoptosis induced by multiple stimuli, Apoptosis, 2021, Apr 27 PMID: 33905036
- Sofia Giacosa, .et al. Cooperative Blockade of CK2 and ATM Kinases Drives Apoptosis in VHL-Deficient Renal Carcinoma Cells through ROS Overproduction, Cancers (Basel), 2021, Feb 2;13(3):576 PMID: 33540838
- Hannes Schmid, .et al. Human invariant natural killer T cells promote tolerance by preferential apoptosis induction of conventional dendritic cells, Haematologica, 2021, Jan 14 PMID: 33440919
- Hua Xu, .et al. Preclinical Study Using ABT263 to Increase Enzalutamide Sensitivity to Suppress Prostate Cancer Progression Via Targeting BCL2/ROS/USP26 Axis Through Altering ARv7 Protein Degradation, Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
- El-Ashmawy NE, .et al. Modulatory Effect of Silymarin on Apoptosis in Testosterone -Induced Benign Prostatic Hyperplasia in Rats, Pathol Oncol Res, 2020, Jan 4 PMID: 31902118
- Schneider D, .et al. The E3 ubiquitin ligase RNF40 suppresses apoptosis in colorectal cancer cells, Clin Epigenetics, 2019, Jul 2;11(1):98 PMID: 31266541
- Fujiki K, .et al. Blockade of ALK4/5 signaling suppresses cadmium- and erastin-induced cell death in renal proximal tubular epithelial cells via distinct signaling mechanisms, Cell Death Differ, 2019, Feb 25 PMID: 30804470
- T Yamamoto, .et al. Mycoplasma pneumoniae protects infected epithelial cells from hydrogen peroxide-induced cell detachment, Cell Microbiol, 2019, 2019 PMID: 30702185
- Maeda N, .et al. Glucocorticoids potentiate the inhibitory capacity of programmed cell death 1 by up-regulating its expression on T cells, J Biol Chem, 2019, Nov 13. pii: jbc.RA119.010379 PMID: 31723031
- Miyazawa S, .et al. Vitamin K2 induces non-apoptotic cell death along with autophagosome formation in breast cancer cell lines, Breast Cancer, 2019, Oct 17 PMID: 31625014
- Yeh HT, .et al. Flavopereirine induces cell cycle arrest and apoptosis via the AKT/p38 MAPK/ERK1/2 signaling pathway in human breast cancer cells, Eur J Pharmacol, 2019, Sep 10;863:172658 PMID: 31518562
- D. Bosc, .et al. A new quinoline-based chemical probe inhibits the autophagy-related cysteine protease ATG4B, Sci Rep, 2018, 8: 11653 PMID: 30076329
- Tsukamoto H, .et al. Lipopolysaccharide (LPS)-binding protein stimulates CD14-dependent Toll-like receptor 4 internalization and LPS-induced TBK1-IKKε-IRF3 axis activation, J Biol Chem, 2018, Jun 29;293(26):10186-10201 PMID: 29760187
- Hiroshi Kuribayashi, .et al. Roles of Nmnat1 in the survival of retinal progenitors through the regulation of pro-apoptotic gene expression via histone acetylation, Cell Death Dis, 2018, Sep; 9(9): 891 PMID: 30166529
- Matsuo J, .et al. Activation of caspase-3 during Chlamydia trachomatis-induced apoptosis at a late stage, Can J Microbiol, 2018, Oct 18:1-9 PMID: 30336068
- Orly Ravid, .et al. Blood-Brain Barrier Cellular Responses Toward Organophosphates: Natural Compensatory Processes and Exogenous Interventions to Rescue Barrier Properties, Front Cell Neurosci, 2018, 12: 359 PMID: 30459557
- Im E, .et al. Luteolin induces caspase-dependent apoptosis via inhibiting the AKT/osteopontin pathway in human hepatocellular carcinoma SK-Hep-1 cells, Life Sci, 2018, Sep 15;209:259-266 PMID: 30107166
- Szalai P, .et al. Nonlinear relationship between ER Ca2+ depletion versus induction of the unfolded protein response, autophagy inhibition, and cell death, Cell Calcium, 2018, Dec;76:48-61 PMID: 30261424
- Im E, .et al. Dihydroartemisinin induced caspase-dependent apoptosis through inhibiting the specificity protein 1 pathway in hepatocellular carcinoma SK-Hep-1 cells, Life Sci, 2018, Jan 1;192:286-292 PMID: 29128513
- Iriyama N, .et al. The cyclin-dependent kinase 4/6 inhibitor, abemaciclib, exerts dose-dependent cytostatic and cytocidal effects and induces autophagy in multiple myeloma cells, Leuk Lymphoma, 2018, Jun;59(6):1439-1450 PMID: 28918692
- Birte Plitzko, .et al. The natural product mensacarcin induces mitochondrial toxicity and apoptosis in melanoma cells, J Biol Chem, 2017, Dec 22; 292(51): 21102-21116 PMID: 29074620
- Akashi E, .et al. Effects of galectin-9 on apoptosis, cell cycle and autophagy in human esophageal adenocarcinoma cells, Oncol Rep, 2017, Jul;38(1):506-514 PMID: 28586026
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Nivocasan (GS-9450)

Catalog No. A14100
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Caspase 抑制剂

Nivocasan (GS-9450)是一种新型的caspase抑制剂，已在纤维化/凋亡动物模型中证明了其肝保护活性。了解更多

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Z-DEVD-FMK

Catalog No. A13503
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Caspase-3 抑制剂

Z-DEVD-FMK是一种特殊的不可逆的Caspase-3抑制剂。了解更多

Product Citations (4)

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- Roi Ankawa, .et al. Apoptotic cells represent a dynamic stem cell niche governing proliferation and tissue regeneration, Dev Cell, 2021, Jul 12;56(13):1900-1916 PMID: 34197726
- Yosefzon Y, .et al. Caspase-3 Regulates YAP-Dependent Cell Proliferation and Organ Size, Mol Cell, 2018, May 17;70(4):573-587.e4 PMID: 29775577
- Akashi E, .et al. Effects of galectin-9 on apoptosis, cell cycle and autophagy in human esophageal adenocarcinoma cells, Oncol Rep, 2017, Jul;38(1):506-514 PMID: 28586026
- Wenquan Liang, .et al. Shikonin induces mitochondria-mediated apoptosis and enhances chemotherapeutic sensitivity of gastric cancer through reactive oxygen species, Sci Rep, 2016, 6: 38267 PMID: 27905569
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Z-LEHD-FMK

Catalog No. A14358
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Caspase-9 抑制剂

Z-LEHD-FMK是一种不可逆抑制caspase-9和相关caspase活性的合成肽。了解更多

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- Wenquan Liang, .et al. Shikonin induces mitochondria-mediated apoptosis and enhances chemotherapeutic sensitivity of gastric cancer through reactive oxygen species, Sci Rep, 2016, 6: 38267 PMID: 27905569
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Q-VD-OPh hydrate

Catalog No. A14915
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Caspase 抑制剂

Q-VD-OPh hydrate是一种选择性，脑和细胞可渗透的，高效且不可逆的caspase-3（IC50 = 25nm），caspase-1（IC50 = 50nM），caspase-8（IC50 = 100nM）和caspase-9抑制剂（IC50 ＝ 430nM）。了解更多

Product Citations (4)

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- Anna L Koessinger, .et al. Increased apoptotic sensitivity of glioblastoma enables therapeutic targeting by BH3-mimetics, Cell Death Differ, 2022, Apr 26 PMID: 35473984
- Florian J Bock, .et al. Apoptotic stress-induced FGF signalling promotes non-cell autonomous resistance to cell death, Nat Commun, 2021, Nov 12;12(1):6572 PMID: 34772930
- Davide Pradella, .et al. A ligand-insensitive UNC5B splicing isoform regulates angiogenesis by promoting apoptosis, Nat Commun, 2021, 12: 4872 PMID: 34381052
- Haschka MD, .et al. MARCH5-dependent degradation of MCL1/NOXA complexes defines susceptibility to antimitotic drug treatment, Cell Death Differ, 2020, Feb 3 PMID: 32015503
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Z-WEHD-FMK

Catalog No. A14916
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Caspase 抑制剂

Z-WEHD-FMK是不可逆抑制caspase-5和相关caspase活性的合成肽。了解更多

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Caspase-3/7 Inhibitor I

Catalog No. A14919
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Caspase-3/7 抑制剂

Caspase-3/7 Inhibitor I是caspase-3（Ki = 60 nM）和caspase-7（Ki = 170 nM）的有效，细胞可渗透且可逆的有效抑制剂。了解更多

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AZ 10417808

Catalog No. A15294
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Caspase-3 抑制剂

AZ 10417808，caspase-3的选择性非肽抑制剂（Ki = 247 nM）；相对于半胱氨酸蛋白酶1、2、6、7和8（Ki> 10 uM）显示的选择性> 40倍。了解更多

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Ivachtin

Catalog No. A15300
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Caspase-3 抑制剂

Ivachtin是一种有效的，细胞可渗透的，可逆的，非竞争性的Caspase-3抑制剂（IC50 = 23 nM）。了解更多

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- Yosefzon Y, .et al. Caspase-3 Regulates YAP-Dependent Cell Proliferation and Organ Size, Mol Cell, 2018, May 17;70(4):573-587.e4 PMID: 29775577
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Ac-DEVD-CHO

Catalog No. A15816
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Caspase 抑制剂

Ac-DEVD-CHO是醛肽和CPP32/Apopain抑制剂。了解更多

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Z-VEID-FMK

Catalog No. A12611
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Caspase-6 抑制剂

Z-VEID-FMK是caspase-6 / Mch2的特异性识别序列。 Z-VEID-FMK是不可逆地抑制VEID依赖性胱天蛋白酶（例如caspase-6）活性的合成肽。抑制剂被设计为甲酯，以促进细胞渗透性。了解更多

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Z-VDVAD-FMK

Catalog No. A12637
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Caspase-2 抑制剂

Z-VDVAD-FMK是caspase-2的细胞渗透性不可逆抑制剂。半胱天冬酶抑制剂在研究生物学过程中起重要作用。了解更多

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Z-DQMD-FMK

Catalog No. A12697
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Caspase-3 抑制剂

Z-DQMD-FMK是不可逆地抑制Caspase-3活性的合成肽。了解更多

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Z-IETD-FMK

Catalog No. A12800
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caspase 8 抑制剂

Z-IETD-FMK是caspase 8的特异性抑制剂。了解更多

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- Liqun Zhao, .et al. Rictor, an essential component of mTOR complex 2, undergoes caspase-mediated cleavage during apoptosis induced by multiple stimuli, Apoptosis, 2021, Apr 27 PMID: 33905036
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EP1013

Catalog No. A11212
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caspase inhibitor

EP1013 is a broad-spectrum caspase selective inhibitor, used in the research of type 1 diabetes. 了解更多

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BOC-D-FMK

Catalog No. A11356
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caspase inhibitor

Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor; inhibits apoptosis stimulated by TNF-α with an IC50 of 39 ?M. 了解更多

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ML132

Catalog No. A21557
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caspase 1 inhibitor

ML132 (NCGC 00185682) is a potent and selective caspase 1 inhibitor with an IC50 of 0.316 nM. 了解更多

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Z-FA-FMK

Catalog No. A14284
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Irreversible Cysteine Protease 抑制剂

Z-FA-FMK是不可逆的半胱氨酸蛋白酶抑制剂。了解更多

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Boc-D-FMK

Catalog No. A15392
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Caspase 抑制剂

BOC-D-FMK是Caspase-3的新型抑制剂。了解更多

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Emricasan

Catalog No. A11394
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Caspase inhibitor

Emricasan is a first-in-class caspase inhibitor in clinical trials for the treatment of liver diseases. 了解更多

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Z-YVAD-FMK

Catalog No. A16317
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Caspase-1 抑制剂

Z-YVAD-FMK是有效的细胞渗透性和caspase-1不可逆抑制剂。了解更多

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Z-VAD(OH)-FMK

Catalog No. A16340
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Caspase 抑制剂

Z-VAD(OH)-FMK是所有胱天蛋白酶的不可逆三肽抑制剂。了解更多

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Z-FA-FMK

Catalog No. A16381
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Cysteine protease 抑制剂

Z-FA-FMK是半胱氨酸蛋白酶的不可逆抑制剂。了解更多

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MX1013

Catalog No. A17218
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pan-caspase inhibitor

MX1013 is a dipeptide pan-caspase inhibitor that inhibits caspase-1, caspase-3, and caspase-6, 7, 8, and 9. 了解更多

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LY2886721

Catalog No. A10543
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BACE1 抑制剂

LY2886721是一种有效的，选择性的，口服活性的β位淀粉样蛋白前体蛋白裂解酶 1 (BACE1) 抑制剂。LY2886721是一种新型强效药物，用于治疗阿尔茨海默病的研究。了解更多

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- Naomi Ito, .et al. miR-15b mediates oxaliplatin-induced chronic neuropathic pain through BACE1 down-regulation, Br J Pharmacol, 2017, Mar; 174(5): 386-395 PMID: 28012171
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AZD3839

Catalog No. A12825
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BACE1 抑制剂

AZD3839是人类BACE1的有效选择性抑制剂，Ki为26.1 nM。了解更多

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AMG-8718

Catalog No. A14407
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BACE1 抑制剂

AMG-8718是一种有效的BACE1抑制剂。了解更多

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Timosaponin b-II

Catalog No. A14591
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BACE1 抑制剂

Timosaponin B-II是知母草（Liliaceae，根茎）的主要活性成分，对脑缺血性损伤具有保护作用。了解更多

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JLK 6

Catalog No. A15301
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γ-secretase 抑制剂

JLK 6是γ-分泌酶的抑制剂，可选择性抑制APP裂解而不影响其他γ-分泌酶介导的途径。了解更多

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MRK 560

Catalog No. A15304
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γ-secretase 抑制剂

MRK 560是一种可用的γ-分泌酶抑制剂，能够显着减少大鼠脑和CSF中的Abeta肽，并证实该大鼠可用于评估γ-分泌酶抑制剂对中枢神经系统Abeta的作用（40）体内水平。了解更多

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PF-03084014

Catalog No. A11259
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γ-secretase 抑制剂

PF-03084014是一种可逆和选择性的γ-分泌酶抑制剂，IC50值为6.2 nM。了解更多

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Flurbiprofen Axetil

Catalog No. A13662
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gamma-secretase 抑制剂

Flurbiprofen Axetil是非甾体抗炎药(NSAID)。了解更多

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L-685458

Catalog No. A15899
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γ-secretase 抑制剂

L-685458是一种有效的A beta PPγ-分泌酶抑制剂，Ki为17 nM。了解更多

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Begacestat (GSI-953)

Catalog No. A11258
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γ-secretase 抑制剂

Begacestat (GSI-953)是一种新型的选择性淀粉样前体蛋白γ-分泌酶的噻吩磺酰胺抑制剂。了解更多

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Verubecestat (MK-8931)

Catalog No. A16113
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β-secretase/BACE1 抑制剂

Verubecestat (MK-8931)是一种有效的选择性β-分泌酶抑制剂，是BACE1蛋白抑制剂或Beta-site APP裂解酶1抑制剂。了解更多

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Z-Ile-Leu-aldehyde

Catalog No. A16215
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γ-Secretase 抑制剂

Z-Ile-Leu-aldehyde是一种有效的γ-分泌酶抑制剂；Notch信号抑制剂。了解更多

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BACE1-IN-4

Catalog No. A18462
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BACE1 inhibitor

BACE1-IN-4 is a potent and highly selective BACE1 inhibitor, with an IC50 of 3.8 nM and a Ki of 1.9 nM, more selective at BACE1 over BACE2. Anti-Alzheimer??s disease. 了解更多

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PF-06751979

Catalog No. A20066
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BACE1 inhibitor

PF-06751979 is a potent, brain penetrant, β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 7.3 nM in BACE1 binding assay. 了解更多

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Umibecestat (CNP520)

Catalog No. A18987
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BACE-1 inhibitor

Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively. 了解更多

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Lanabecestat

Catalog No. A12282
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BACE1 inhibitor

Lanabecestat (AZD3293) is a potent, highly permeable, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM. 了解更多

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BACE1-IN-1

Catalog No. A12183
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BACE1 inhibitor

BACE1-IN-1 is a potent and highly brain penetrant BACE1 inhibitor with IC50s of 32 and 47 nM for human BACE1 and BACE2, respectively. 了解更多

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BMS-906024

Catalog No. A21172
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gamma secretase inhibitor

BMS-906024 is an oral and selective gamma secretase inhibitor (GSI) that is a small molecule Notch inhibitor. 了解更多

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Compound E

Catalog No. A21292
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γ-secretase inhibitor

Compound E is a γ-secretase inhibitor. 了解更多

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β-Secretase Inhibitor IV

Catalog No. A21346
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BACE-1 inhibitor

β-Secretase Inhibitor IV is a potent, cell-active BACE-1 inhibitor with IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively. 了解更多

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AZD3839 free base

Catalog No. A21606
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BACE1 inhibitor

AZD3839 (free base) is a potent and selective BACE1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, also a β-secretase enzyme inhibitor. 了解更多

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RO4929097

Catalog No. A10802
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Gamma-secretase 抑制剂

RO4929097是一种γ secretase抑制剂，无细胞试验中IC50为4 nM。抑制Aβ40和Notch的细胞加工，EC50分别为14 nM和5 nM。了解更多

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- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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BMS-708163 (Avagacestat)

Catalog No. A10157
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Gamma-secretase 抑制剂

BMS-708163 (Avagacestat)是口服生物有效的，选择性的γ-分泌酶抑制剂，作用于Aβ40和Aβ42时，IC50分别为0.3 nM和0.27 nM。了解更多

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MK-0752

Catalog No. A11194
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Gamma-secretase 抑制剂

MK-0752抑制Notch信号通路，这可能会导致Notch信号通路被过度激活的肿瘤细胞诱导生长停滞和凋亡。了解更多

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DAPT (GSI-IX)

Catalog No. A10288
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Gamma secretase 抑制剂

DAPT (GSI-IX)是一种γ-分泌酶抑制剂，可导致人原代神经元培养物中Aβ40和Aβ42水平降低，总Aβ和Aβ42的IC50值分别为115和200 nM。了解更多

Product Citations (2)

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- Paul Mark Medina, .et al. Revealing the anticancer potential of candidate drugs in vivo using Caenorhabditis elegans mutant strains, Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
- Tatsuya Usui, .et al. Hedgehog Signals Mediate Anti-Cancer Drug Resistance in Three-Dimensional Primary Colorectal Cancer Organoid Culture, Int J Mol Sci, 2018, Apr; 19(4): 1098 PMID: 29642386

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