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Proteases

Proteases

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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

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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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YO-01027

Catalog No. A11174
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γ-secretase 抑制剂

YO-01027是一种二肽γ-secretase抑制剂，作用于APPL和Notch分裂，无细胞试验中IC50分别为2.6 nM和2.9 nM，一种抗阿尔茨海默氏病药物。了解更多

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LY-411575

Catalog No. A11176
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Gamma secretase 抑制剂

LY-411575是一种选择性的，细胞可渗透的小分子γ-secretase抑制剂。在表达APP或NΔE的HEK293细胞中IC50为0.078 nM/0.082 nM(基于膜/细胞)，也抑制Notch分裂，IC50为0.39 nM。了解更多

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- Wojciech J Szlachcic, .et al. SARS-CoV-2 infects an in vitro model of the human developing pancreas through endocytosis, iScience, 2022, Jul 15;25(7) PMID: 35756892
- Zhang ZH, .et al. Notch signaling suppresses CD14+ monocytes cells activity in patients with chronic hepatitis C, APMIS, 2019, Jul 5 PMID: 31274210
- Bo Pang, .et al. Elevated Notch1 enhances interleukin-22 production by CD4+ T cells via aryl hydrocarbon receptor in patients with lung adenocarcinoma, Biosci Rep, 2018, Dec 21; 38(6): BSR20181922 PMID: 30473538
- Shuo Li, .et al. Notch signaling pathway suppresses CD8+ T cells activity in patients with lung adenocarcinoma, Int Immunopharmacol, 2018, Oct;63:129-136 PMID: 30086535
- Jiang BC, .et al. Notch Signaling Regulates Circulating T Helper 22 Cells in Patients with Chronic Hepatitis C, Viral Immunol, 2017, Sep;30(7):522-532 PMID: 28410452
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Semagacestat (LY450139)

Catalog No. A10836
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Gamma-secretase 抑制剂

Semagacestat (LY450139)是一种针对Aβ42，Aβ40和Aβ38的γ-分泌酶阻滞剂，IC50分别为10.9 nM，12.1 nM和12.0 nM。 Semagacestat还抑制Notch信号传导，IC50为14.1 nM。了解更多

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- Yesuvadian R, .et al. Potent γ-secretase inhibitors/modulators interact with amyloid-β fibrils but do not inhibit fibrillation: a high-resolution NMR study., Biochem Biophys Res Commun., 2014, May 16;447(4):590-5 PMID: 24747079
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LY2811376

Catalog No. A11776
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BACE1 抑制剂

LY2811376是第一种可口服的非肽类BACE1抑制剂，可在动物体内产生显着的Aβ降低作用。了解更多

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BMS 433796

Catalog No. A11337
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γ-Secretase 抑制剂

BMS 433796是在阿尔茨海默病转基因小鼠模型中具有Aβ降低活性的γ分泌酶抑制剂。了解更多

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E 2012

Catalog No. A11393
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gamma-secretase modulator

E 2012是γ-secretase抑制剂。了解更多

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- Yesuvadian R, .et al. Potent γ-secretase inhibitors/modulators interact with amyloid-β fibrils but do not inhibit fibrillation: a high-resolution NMR study., Biochem Biophys Res Commun., 2014, May 16;447(4):590-5 PMID: 24747079
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BMS 299897

Catalog No. A12444
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γ-secretase 抑制剂

BMS 299897是一种有效的γ-分泌酶抑制剂（IC50 = 12 nM）。在体外抑制Aβ40和Aβ42的形成（IC50值分别为7.4和7.9 nM），并在体内降低脑，血浆和脑脊髓液中的Aβ。了解更多

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- Chao Liu, .et al. APP upregulation contributes to retinal ganglion cell degeneration via JNK3, Cell Death Differ, 2018, Apr; 25(4): 661-676 PMID: 29238071
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Flurizan

Catalog No. A12433
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gamma-secretase modulator

Flurizan是一种非甾体抗炎药（NSAID），可抑制γ-分泌酶的活性。了解更多

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FLI-06

Catalog No. A13815
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Gamma-secretase 抑制剂

FLI-06是一种Notch抑制剂和早期分泌途径抑制剂。FLI-06以不同于布雷菲德菌素A和杀真菌剂A的方式破坏高尔基体。了解更多

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- Tan YJ, .et al. Anticancer activities of a benzimidazole compound through sirtuin inhibition in colorectal cancer, Future Med Chem, 2018, Sep 1;10(17):2039-2057 PMID: 30066578
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LY3039478

Catalog No. A13544
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Notch 抑制剂

LY3039478是一种新型小分子Notch抑制剂，在大多数测试的肿瘤细胞系中，IC50约为1nM。了解更多

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LY-900009

Catalog No. A14088
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Notch 抑制剂

LY-900009是一种有效的Notch抑制剂，IC50值为0.27 nM。了解更多

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IMR-1

Catalog No. A16152
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Notch 抑制剂

IMR-1是一类新型的Notch抑制剂，靶向转录激活，IC50为6 umol/L。了解更多

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IMR-1A

Catalog No. A16223
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Notch 抑制剂

IMR-1A是IMR-1的代谢产物。IMR-1是一类新型的Notch抑制剂，靶向转录激活，IC50为6 umol/L。了解更多

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NGP-555

Catalog No. A17051
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γ-Secretase Modulator

NGP-555是一种γ-分泌酶调节剂，具有选择性机制，可减少Abeta 42，同时提高较短的Abeta形式，例如Abeta 37和38。了解更多

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BPN-15606

Catalog No. A18681
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γ-secretase modulator

BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. 了解更多

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AM 114

Catalog No. A14922
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20S proteasome 抑制剂

AM 114是硼查尔酮的衍生物，是一种有效的蛋白酶体小分子抑制剂，可抑制20S蛋白酶体的胰凝乳蛋白酶样活性，其50％抑制浓度的IC50值约为1 uM，导致大量积累泛素化的p53和其他细胞蛋白在整个细胞中的表达，而不会显着破坏p53与鼠类double minutes 2（mdm2）蛋白的相互作用。了解更多

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Epoxomicin

Catalog No. A12730
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Proteasome 抑制剂

Epoxomicin是从放线菌中分离出来的一种有效的抗肿瘤药，被用作20S蛋白酶体的选择性和不可逆抑制剂。了解更多

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VR23

Catalog No. A13650
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Proteasome 抑制剂?

VR23是一个小分子，可有效抑制胰蛋白酶样蛋白酶体（IC50 = 1 nM），胰凝乳蛋白酶样蛋白酶体（IC50 = 50-100 nM）和半胱天冬酶样蛋白酶体（IC50 = 3uM）的活性。了解更多

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ML604440

Catalog No. A18826
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proteasome β1i (LMP2) subunit inhibitor

ML604440 is a potent, specific and cell permeable proteasome β1i (LMP2) subunit inhibitor. 了解更多

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Proteasome-IN-1

Catalog No. A12254
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proteasome inhibitor

Proteasome-IN-1 is a proteasome inhibitor extracted from patent WO 2013142376 A1. 了解更多

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Ixazomib citrate

Catalog No. A18017
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20S proteasome inhibitor

Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM. 了解更多

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(R)-MG-132

Catalog No. A21980
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proteasome inhibitor

(R)-MG-132 ((S,R,S)-(-)-MG-132) is the enantiomer of MG-132. (R)-MG-132 is a proteasome inhibitor with weaker cell cytotoxicity than MG-132. (R)-MG-132 stereoisomer is a more potent proteasome inhibitor than MG-132. 了解更多

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MLN9708

Catalog No. A10602
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Proteasome 抑制剂

MLN9708是一种蛋白酶体抑制剂，可抑制蛋白酶体的活性，从而阻断通常由蛋白酶体进行的靶向蛋白水解。了解更多

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Bortezomib (Velcade)

Catalog No. A10160
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Proteasome 抑制剂

Bortezomib (Velcade)是26S蛋白酶体的高度选择性，可逆抑制剂。了解更多

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- Yoshitaka Sato, .et al. Epstein-Barr virus tegument protein BGLF2 in exosomes released from virus-producing cells facilitates de novo infection, Cell Commun Signal, 2022, Jun 21;20(1):95 PMID: 35729616
- Shin-Ichi Makino, .et al. Impairment of Proteasome Function in Podocytes Leads to CKD, J Am Soc Nephrol, 2021, Mar;32(3):597-613 PMID: 33510039
- Yusuke Yamashita, .et al. Targeting Adaptive IRE1α Signaling and PLK2 in Multiple Myeloma: Possible Anti-Tumor Mechanisms of KIRA8 and Nilotinib, Int J Mol Sci, 2020, Sep; 21(17): 6314 PMID: 32878237
- Nandini Verma, .et al. Synthetic lethal combination targeting BET uncovered intrinsic susceptibility of TNBC to ferroptosis, Sci Adv, 2020, 6 : eaba8968
- A Hayano, .et al. Cell-type-specific sensitivity of bortezomib in the methotrexate-resistant primary central nervous system lymphoma cells, Int J Clin Oncol, 2019, 1-10 PMID: 30993483
- Hiroshi Fukamachi, .et al. A subset of diffuse-type gastric cancer is susceptible to mTOR inhibitors and checkpoint inhibitors, J Exp Clin Cancer Res, 2019, 38:127 PMID: 30866995
- Y Sato, .et al. S-like phase CDKs stabilize the Epstein-Barr virus BDLF4 protein to temporally control late gene transcription, J Virol, 2019, Jan 30. pii: JVI.01707-18 PMID: 30700607
- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Wenhan Deng, .et al. Variable Responses of MYC Translocation Positive Lymphoma Cell Lines To Different Combinations of Novel Agents: Impact of BCL2 Family Protein Expression, Transl Oncol, 2018, Oct; 11(5): 1147-1154 PMID: 30055346
- 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
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Hokyung K. Chung, .et al. Tunable and reversible drug control of protein production via a self-excising degron, Nat Chem Biol, 2015, Sep; 11(9): 713-720 PMID: 26214256
- S Raz, .et al. Severe hypoxia induces complete antifolate resistance in carcinoma cells due to cell cycle arrest, Cell Death Dis., 2014, 5(2): e1067 PMID: 24556682
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MG-132

Catalog No. A11043
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Proteasome 抑制剂

MG-132是蛋白酶体（IC50 = 100 nM）和钙蛋白酶（IC50 = 1.2μM）的有效的细胞渗透抑制剂。了解更多

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- Vo Thi Anh Nguyet, .et al. Acquired resistance to severe ethanol stress-induced inhibition of proteasomal proteolysis in Saccharomyces cerevisiae, Biochim Biophys Acta Gen Subj, 2022, Sep 6;1866(12):130241 PMID: 36075516
- Jalila Chagraoui, .et al. UM171 Preserves Epigenetic Marks that Are Reduced in Ex Vivo Culture of Human HSCs via Potentiation of the CLR3-KBTBD4 Complex, Cell Stem Cell, 2021, Jan 7;28(1):48-62.e6 PMID: 33417871
- Eunsu Yoo, .et al. Anti-proliferative activity of A. Oxyphylla and its bioactive constituent nootkatone in colorectal cancer cells, BMC Cancer, 2020, Sep 14;20(1):881 PMID: 32928152
- 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
- Chi-Hung R Or, .et al. Obatoclax, a Pan-BCL-2 Inhibitor, Downregulates Survivin to Induce Apoptosis in Human Colorectal Carcinoma Cells Via Suppressing WNT/β-catenin Signaling, Int J Mol Sci, 2020, Mar 5;21(5):1773 PMID: 32150830
- Ghosh S, .et al. Interactions between Viperin, Vesicle-Associated Membrane Protein A, and Hepatitis C Virus Protein NS5A Modulate Viperin Activity and NS5A Degradation, Biochemistry, 2020, Feb 18;59(6):780-789 PMID: 31977203
- Kondo H, .et al. PITHD1 is a proteasome-interacting protein essential for male fertilization, J Biol Chem, 2020, Feb 7;295(6):1658-1672 PMID: 31915251
- Ohigashi I, .et al. Trans-omics Impact of Thymoproteasome in Cortical Thymic Epithelial Cells, Cell Rep, 2019, Nov 26;29(9):2901-2916 PMID: 31775054
- Paudel DB, .et al. Expression and antiviral function of ARGONAUTE 2 in Nicotiana benthamiana plants infected with two isolates of tomato ringspot virus with varying degrees of virulence, Virology, 2018, Nov;524:127-139 PMID: 30195250
- Ohkusu-Tsukada K, .et al. The Role of Proteasome Inhibitor MG132 in 2,4-Dinitrofluorobenzene-Induced Atopic Dermatitis in NC/Nga Mice, Int Arch Allergy Immunol, 2018, 176(2):91-100 PMID: 29669333
- Chi-Hung R. Or, .et al. Obatoclax, a Pan-BCL-2 Inhibitor, Targets Cyclin D1 for Degradation to Induce Antiproliferation in Human Colorectal Carcinoma Cells, Int J Mol Sci, 2016, Jan; 18(1): 44 PMID: 28035994
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MLN2238 (Ixazomib)

Catalog No. A10600
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Proteasome 抑制剂

MLN2238 (Ixazomib)是20S蛋白酶体抑制剂的有效可逆特异性β5位点，IC50值为3.4 nM。了解更多

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CEP-18770 (Delanzomib)

Catalog No. A11145
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Proteasome 抑制剂

CEP-18770 (Delanzomib)是一种新型口服活性蛋白酶体抑制剂，IC50为3.8 nM，具有良好的肿瘤选择性，可用于治疗对蛋白酶体抑制有反应的MM和其他恶性肿瘤。了解更多

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PR-171 (Carfilzomib)

Catalog No. A11278
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Proteasome 抑制剂

PR-171 (Carfilzomib)是四肽环氧酮和选择性蛋白酶体抑制剂。它是环氧霉素的类似物。了解更多

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- Ori Kalid, .et al. PTX80, A Novel Compound Targeting the Autophagy Receptor p62/SQSTM1 for Treatment of Cancer, Chem Biol Drug Des, 2022, Mar 24 PMID: 35322538
- Abbas Rahdar, .et al. Pluronic F127/carfilzomib-based nanomicelles as promising nanocarriers: synthesis, characterization, biological, and in silico evaluations, Journal of Molecular Liquids, 2022, 346: 118271
- Sadegh Zarei, .et al. Carfilzomib Induces Drug Resistance in A2780 Ovarian Cancer Cells Through p53-Dependent and Caspase-3 Independent Pathways, J Appl Biotechnol Rep, 2019, June;6(2):45-49
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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ONX-0914

Catalog No. A12653
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Immunoproteasome 抑制剂

ONX 0914是有效，选择性的免疫蛋白酶体亚基LMP7的抑制剂，在自身免疫性疾病（如类风湿性关节炎，炎性肠病和狼疮）中具有潜在的治疗应用。ONX 0914被设计为一种有效的免疫蛋白酶抑制剂，对组成型蛋白酶体的交叉反应最小。了解更多

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- Yuki Sasaki, .et al. Blockade of the CXCR3/CXCL10 axis ameliorates inflammation caused by immunoproteasome dysfunction, JCI Insight, 2022, Apr 8;7(7) PMID: 35393946
- Ming-Shu Mo, .et al. Dopaminergic neurons show increased low-molecular-mass protein 7 activity induced by 6-hydroxydopamine in vitro and in vivo, Transl Neurodegener, 2018, 7: 19 PMID: 30128145
- Ohkusu-Tsukada K, .et al. The Role of Proteasome Inhibitor MG132 in 2,4-Dinitrofluorobenzene-Induced Atopic Dermatitis in NC/Nga Mice, Int Arch Allergy Immunol, 2018, 176(2):91-100 PMID: 29669333
- Arimochi H, .et al. Differentiation of preadipocytes and mature adipocytes requires PSMB8, Sci Rep, 2016, May 26;6:26791 PMID: 27225296
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Lactacystin

Catalog No. A12768
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proteasome 抑制剂

Lactacystin是一种细胞可渗透的，有效的和选择性的蛋白酶体抑制剂。了解更多

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Gliotoxin

Catalog No. A13711
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20S proteasome 抑制剂

Gliotoxin是由曲霉菌和其他真菌的致病菌株产生的一种免疫抑制性真菌毒素。了解更多

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PSI

Catalog No. A14048
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Proteasome 抑制剂

PSI是蛋白酶体抑制剂，其抑制蛋白酶体的胰凝乳蛋白酶样活性。了解更多

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ONX 0912 (Oprozomib)

Catalog No. A14181
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Proteasome 抑制剂

ONX 0912 (Oprozomib)是一种三肽环氧酮，可抑制对常规和硼替佐米治疗耐药的MM细胞的生长并诱导其凋亡。了解更多

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PI-1840

Catalog No. A14146
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reversible proteasome 抑制剂

PI-1840是一种具有抗肿瘤活性的新型非共价快速可逆蛋白酶体抑制剂。了解更多

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Marizomib (NPI-0052, salinosporamide A)

Catalog No. A13853
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Proteasome 抑制剂

Marizomib (NPI-0052,salinosporamide A)是一种天然存在的salinosporamide，从海洋放线菌Salinospora tropica中分离出来，具有潜在的抗肿瘤活性。了解更多

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- Tarantelli C, .et al. PQR309 Is a Novel Dual PI3K/mTOR Inhibitor with Preclinical Antitumor Activity in Lymphomas as a Single Agent and in Combination Therapy, Clin Cancer Res, 2018, Jan 1;24(1):120-129 PMID: 29066507
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Aclacinomycin A

Catalog No. A14910
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20S proteasome 抑制剂

Aclacinomycin A是一种蒽环类药物，是20S蛋白酶体胰凝乳蛋白酶样活性的特异性抑制剂。了解更多

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Dihydroeponemycin

Catalog No. A14932
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Proteasome 抑制剂

Dihydroeponemycin是蛋白酶体和抗肿瘤剂的抑制剂。了解更多

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