AB142164

Compound E, gamma;-secretase inhibitor

Name: Compound E, gamma;-secretase inhibitor (CAS 209986-17-4) | Abcam
Brand: Abcam Limited
SKU: AB142164
Price: 225 USD
Availability: InStock

Be the first to review this product! Submit a review

(11 Publications)

Cell-permeable, selective, non-competitive, potent γ-secretase inhibitor (IC₅₀ = 0.3 nM). MW 490.5.

- Active in vitro and in vivo
- Available in different sizes to fit your experimental needs

View Alternative Names

6530402N02Rik, AD3, AD3L, AD3LP, AD4, AD5, AL138795.3, APH1A gamma secretase subunit, APH1A_HUMAN, APH1B_HUMAN, Ad3h, Alzheimer disease 4, Anterior Pharynx Defective 1, Anterior pharynx defective 1 homolog A, Anterior pharynx defective 1 homolog B, Anterior pharynx defective 1 homolog B (C. elegans), Anterior pharynx defective 1B like, Anterior pharynx defective 1b short splicing variant, Aph-1alpha, Aph-1beta, CGI 78, CMD1V, DKFZp564D0372, E5-1, FAD, Gamma Secretase Subunit PEN2, Gamma secretase sununit, Gamma-secretase subunit APH-1A, Gamma-secretase subunit Aph-1b, Gamma-secretase subunit PEN-2, Hematopoietic stem/progenitor cells protein MDS033, Homo Sapiens Clone CC44 Senilin 1, Likely ortholog of C. elegans anterior pharynx defective 1A, MDS033, MSTP064, OTTHUMP00000035671, OTTHUMP00000035672, OTTHUMP00000228286, OTTHUMP00000228288, PEN2_HUMAN, PRO 1328, PS-1, PS-2, PS1-CTF12, PSEN1, PSEN2, PSF, PSFL, PSN1_HUMAN, PSN2_HUMAN, PSNL1, PSNL2, Presenilin 2, Presenilin 2 (Alzheimer disease 4), Presenilin Enhancer 2, Presenilin enhancer 2 homolog, Presenilin enhancer protein 2, Presenilin stabilisation factor like, Presenilin-1 CTF12, Presenilin-2 CTF subunit, Presenilin-stabilization factor, Presenilin-stabilization factor-like, Protein S182, S182, STM-2, TAAV 688, UNQ579/PRO1141, psenen

2 Images

Chemical Structure - Compound E, gamma;-secretase inhibitor (AB142164)

Chemical Structure

Lab

Chemical Structure - Compound E, gamma;-secretase inhibitor (AB142164)

2D chemical structure image of ab142164, Compound E, gamma;-secretase inhibitor

Functional Studies - Compound E, gamma;-secretase inhibitor (AB142164)

FuncS

Collaborator6479473****

Functional Studies - Compound E, gamma;-secretase inhibitor (AB142164)

Kc167 cells were treated with varying concentrations of compound E (ab142164) in DMSO for 16hr at 25°C; DMSO only was used as the negative control. The cells were further incubated for 30 minutes with 4mM EGTA in PBS (in the presence of compound E), and were then lysed for analysis. To measure Notch activity, Notch targets E(spl)mβ-HLH and E(spl)m3-HLH mRNA levels were assayed. Data shows the fold change of mRNA levels of E(spl)mβ-HLH and E(spl)m3-HLH under different conditions, normalised to DMSO treatment (negative control). Notch activation by EGTA is abrogated by treatment with compound E.

This image is courtesy of an Abreview submitted by a verified customer

Key facts

CAS number

209986-17-4

Purity

>99%

Form

Solid

form

Molecular weight

490.5 Da

Molecular formula

C27H24F2N4O3

PubChem

11306390

Nature

Synthetic

Solubility

Soluble in DMSO to 100 mM

Biochemical name

gamma-Secretase Inhibitor XXI

Biological description

Cell-permeable, selective, non-competitive, potent γ-secretase inhibitor (IC₅₀ = 0.3 nM). Active in vitro and in vivo.

Canonical smiles

CC(C(=O)NC1C(=O)N(C2=CC=CC=C2C(=N1)C3=CC=CC=C3)C)NC(=O)CC4=CC(=CC(=C4)F)F

Isomeric smiles

C[C@@H](C(=O)N[C@@H]1C(=O)N(C2=CC=CC=C2C(=N1)C3=CC=CC=C3)C)NC(=O)CC4=CC(=CC(=C4)F)F

InChi

InChI=1S/C27H24F2N4O3/c1-16(30-23(34)14-17-12-19(28)15-20(29)13-17)26(35)32-25-27(36)33(2)22-11-7-6-10-21(22)24(31-25)18-8-4-3-5-9-18/h3-13,15-16,25H,14H2,1-2H3,(H,30,34)(H,32,35)/t16-,25+/m0/s1

InChiKey

JNGZXGGOCLZBFB-IVCQMTBJSA-N

IUPAC Name

(2S)-2-[[2-(3,5-difluorophenyl)acetyl]amino]-N-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]propanamide

style

left-column

Product details

Check out our range of gamma secretase inhibitor biochemicals here

style

left-column

Properties and storage information

Shipped at conditions

Ambient - Can Ship with Ice

Appropriate short-term storage conditions

-20°C

Appropriate long-term storage conditions

-20°C

Storage information

Store under desiccating conditions|The product can be stored for up to 12 months

style

left-column

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

PS-1 and PS-2 have strong associations with Alzheimer's disease and familial early-onset Alzheimer's patients. Mutations in the presenilin genes lead to altered gamma-secretase activity resulting in increased production of amyloid-beta 42 a toxic form that is more prone to aggregation. These malfunctions are often observed in people with Alzheimer's and highlight the pathogenic role of altered presenilin activity alongside the amyloid precursor protein and tau another protein commonly associated with Alzheimer-related neurodegeneration.

Pathways

PS-1 and PS-2 are central to the Notch signaling pathway and amyloid precursor protein processing. Within these pathways gamma-secretase plays an essential role in cleaving substrates which allows for proper signaling and cellular communication. Here APP and Notch are critical substrates processed by this proteolytic activity. Other related proteins include the ligands for Notch signaling which presenilins help process through their enzymatic function in the gamma-secretase complex.

Biological function summary

Presenilins are important for the intramembrane proteolysis of various type 1 transmembrane proteins. They function as part of the gamma-secretase complex to facilitate the cleavage of amyloid precursor protein (APP) which is an essential process for generating amyloid-beta peptides. These peptides can aggregate and form plaques linked to neurodegeneration. The gamma-secretase complex includes other important proteins like PEN2 Aph1a and Aph1b which together with presenilins execute the proteolytic process.

Presenilin 1 (PS-1) and Presenilin 2 (PS-2) also known as AD5 are integral membrane proteins that act mechanically as the catalytic core of the gamma-secretase complex. PS-1 has a molecular mass of about 467 amino acids while PS-2 is 448 amino acids. These proteins are expressed primarily in the endoplasmic reticulum and the Golgi apparatus across many tissues including neurons. They form a complex with accessory proteins such as PEN2 and either Aph1a or Aph1b which are necessary for the gamma-secretase activity.

style

left-column

style

left-column

Product protocols

Visit the General protocols
Visit the Troubleshooting

style

left-column

Publications (11)

Recent publications for all applications. Explore the full list and refine your search

Nature communications 16:460 PubMed39779681

2025

A high-fidelity CRISPR-Cas13 system improves abnormalities associated with C9ORF72-linked ALS/FTD.

Applications

Unspecified application

Species

Unspecified reactive species

Tristan X McCallister,Colin K W Lim,Mayuri Singh,Sijia Zhang,Najah S Ahsan,William M Terpstra,Alisha Y Xiong,M Alejandra Zeballos C,Jackson E Powell,Jenny Drnevich,Yifei Kang,Thomas Gaj

Scientific reports 14:21912 PubMed39300145

2024

Notch1 Phase Separation Coupled Percolation facilitates target gene expression and enhancer looping.

Applications

Unspecified application

Species

Unspecified reactive species

Gregory Foran,Ryan Douglas Hallam,Marvel Megaly,Anel Turgambayeva,Daniel Antfolk,Yifeng Li,Vincent C Luca,Aleksandar Necakov

Brain communications 6:fcae244 PubMed39144751

2024

Inhibition of expression in human superoxide dismutase 1-mutant amyotrophic lateral sclerosis astrocytes protects against neurotoxicity.

Applications

Unspecified application

Species

Unspecified reactive species

Kornélia Szebényi,Ingrid Vargová,Veselina Petrova,Jana Turečková,George M Gibbons,Monika Řehořová,Mai Abdelgawad,Alexandra Sándor,Dana Marekova,Jessica C F Kwok,Pavla Jendelová,James W Fawcett,András Lakatos

Nature cell biology 26:353-365 PubMed38443567

2024

Distinct pathways drive anterior hypoblast specification in the implanting human embryo.

Applications

Unspecified application

Species

Unspecified reactive species

Bailey A T Weatherbee,Antonia Weberling,Carlos W Gantner,Lisa K Iwamoto-Stohl,Zoe Barnikel,Amy Barrie,Alison Campbell,Paula Cunningham,Cath Drezet,Panagiota Efstathiou,Simon Fishel,Sandra Gutiérrez Vindel,Megan Lockwood,Rebecca Oakley,Catherine Pretty,Nabiha Chowdhury,Lucy Richardson,Anastasia Mania,Lauren Weavers,Leila Christie,Kay Elder,Phillip Snell,Magdalena Zernicka-Goetz

Frontiers in cellular neuroscience 16:866020 PubMed35685988

2022

MicroRNA-582-5p Contributes to the Maintenance of Neural Stem Cells Through Inhibiting Secretory Protein FAM19A1.

Applications

Unspecified application

Species

Unspecified reactive species

Yu-Fei Zhang,Xin-Xin Li,Xiu-Li Cao,Chen-Chen Ji,Xiang-Yu Gao,Dan Gao,Hua Han,Fei Yu,Min-Hua Zheng

eLife 11: PubMed35438077

2022

Notch controls the cell cycle to define leader versus follower identities during collective cell migration.

Applications

Unspecified application

Species

Unspecified reactive species

Zain Alhashem,Dylan Feldner-Busztin,Christopher Revell,Macarena Alvarez-Garcillan Portillo,Karen Camargo-Sosa,Joanna Richardson,Manuel Rocha,Anton Gauert,Tatianna Corbeaux,Martina Milanetto,Francesco Argenton,Natascia Tiso,Robert N Kelsh,Victoria E Prince,Katie Bentley,Claudia Linker

Journal of visualized experiments : JoVE : PubMed34515684

2021

Establishment of an Electrophysiological Platform for Modeling ALS with Regionally-Specific Human Pluripotent Stem Cell-Derived Astrocytes and Neurons.

Applications

Unspecified application

Species

Unspecified reactive species

Arens Taga,Christa W Habela,Alexandra Johns,Shiyu Liu,Mollie O'Brien,Nicholas J Maragakis

Cell reports 25:2563-2576.e9 PubMed30485820

2018

Improving Cell Survival in Injected Embryos Allows Primed Pluripotent Stem Cells to Generate Chimeric Cynomolgus Monkeys.

Applications

Unspecified application

Species

Unspecified reactive species

Yu Kang,Zongyong Ai,Kui Duan,Chenyang Si,Yong Wang,Yun Zheng,Jingjing He,Yu Yin,Shumei Zhao,Baohua Niu,Xiaoqing Zhu,Li Liu,Lifeng Xiang,Linming Zhang,Yuyu Niu,Weizhi Ji,Tianqing Li

eLife 7: PubMed30394875

2018

A novel mechanism of gland formation in zebrafish involving transdifferentiation of renal epithelial cells and live cell extrusion.

Applications

Unspecified application

Species

Unspecified reactive species

Richard W Naylor,Hao-Han G Chang,Sarah Qubisi,Alan J Davidson

Experimental and therapeutic medicine 16:4623-4631 PubMed30542413

2018

BMP9 overexpressing adipose-derived mesenchymal stem cells promote cartilage repair in osteoarthritis-affected knee joint via the Notch1/Jagged1 signaling pathway.

Applications

Unspecified application

Species

Unspecified reactive species

Xinwei Liu,Mingchang Du,Yu Wang,Songbo Liu,Xianmin Liu

View all publications

style

left-column

style

left-column

style

right-column

Product promise

We are committed to supporting your work with high-quality reagents, and we're here for you every step of the way. In the unlikely event that one of our products does not perform as expected, you're protected by our Product Promise.

For full details, please see our Terms & Conditions

Please note: All products are 'FOR RESEARCH USE ONLY. NOT FOR USE IN DIAGNOSTIC OR THERAPEUTIC PROCEDURES'.

For licensing inquiries, please contact partnerships@abcam.com

Compound E, gamma;-secretase inhibitor

Chemical Structure - Compound E, gamma;-secretase inhibitor (AB142164)

Functional Studies - Compound E, gamma;-secretase inhibitor (AB142164)

Key facts

CAS number

Purity

Form

Molecular weight

Molecular formula

PubChem

Nature

Solubility

Biochemical name

Biological description

Canonical smiles

Isomeric smiles

InChi

InChiKey

IUPAC Name

Product details

Properties and storage information

Shipped at conditions

Appropriate short-term storage conditions

Appropriate long-term storage conditions

Storage information

Supplementary information

Pathways

Biological function summary

Product protocols

Publications (11)

Complementary Products

Secondary Antibodies

Biochemicals

Primary Antibodies

Biochemicals

Product promise