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γ-Secretase

γ-Secretase

Inhibitory Selectivity

Catalog No.	Inhibitor Name	γ secretase	Aβ	Notch	Other
A10288	DAPT (GSI-IX)		*
A10802	RO4929097	***		***	Aβ40
A10836	Semagacestat		**	**
A10157	Avagacestat		****
A11174	Dibenzazepine	***		***
A11176	LY411575	****		****
A15899	L-685458	*
A13815	FLI-06			*
A13319	PF-03084014	**
A11194	MK-0752		***		Aβ40
A13544	LY3039478			****
A16152	IMR-1			*
A16223	IMR-1A			*
A11258	Begacestat (GSI-953)	**
A12444	BMS 299897
A13217	TC-E 5006	*
A15304	MRK 560	****
A15301	JLK 6
A16214	CHF5074	*
A16215	Z-Ile-Leu-aldehyde

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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