Compound E
Based on 18 publication(s) in Google Scholar
Compound E is a γ-secretase inhibitor. Compound E blocks β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC50s of 0.24, 0.37, 0.32 nM, respectively.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.97%
- CAS 番号: 209986-17-4
- 分子式: C27H24F2N4O3
- 分子量:490.50
-
保管条件:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Compound E
More- Immunity. 2025 Mar 21:S1074-7613(25)00093-7. [Abstract]
- Cell Stem Cell. 2026 Jan 8;33(1):44-57.e7. [Abstract]
- Mol Neurodegener. 2025 Aug 28;20(1):94. [Abstract]
- Nat Commun. 2022 Jul 18;13(1):4148. [Abstract]
- Sci Adv. 2022 Feb 25;8(8):eabk1826. [Abstract]
- Chem Eng J. 1 January 2023, 138737.
- Cell Rep. 2021 Dec 7;37(10):110102. [Abstract]
- Fundam Res. 2026 Jan 10.
- Fundam Res. 2024 Mar 19.
- Front Cell Dev Biol. 2021 Jul 12:9:703338. [Abstract]
- Front Cell Dev Biol. 2021 Jun 21:9:671704. [Abstract]
- bioRxiv. 2026 Jun 3:2026.06.01.728985. [Abstract]
- Northwestern University. 2026.
- bioRxiv. 2025 Dec 9:2025.12.05.692670. [Abstract]
- Seoul National University. 2032.
- bioRxiv. 2025 Aug 19.
- Heinrich Heine University Dusseldorf. 2025.
- bioRxiv. 2024 November 15.
Customer Validation & Images
-
2D/3D Cell Culture and Differentiation
-
In Vivo Efficacy Study
-
WB
生物活性
IC50: 0.24 nM (β-amyloid(40)), 0.37 nM (β-amyloid(42)), 0.24 nM (Notch)[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| SH-SY5Y | IC50 |
1 nM
Compound: 66
|
Displacement of [3H]5-chloro-N-((2S,3R)-5,5,5-trifluoro-1-hydroxy-3-methylpentan-2-yl)thiophene-2-sulfonamide from gamma secretase in human SH-SY5Y cells by competitive binding assay
Displacement of [3H]5-chloro-N-((2S,3R)-5,5,5-trifluoro-1-hydroxy-3-methylpentan-2-yl)thiophene-2-sulfonamide from gamma secretase in human SH-SY5Y cells by competitive binding assay
|
[PMID: 19694467] |
| SH-SY5Y | IC50 |
2.7 nM
Compound: 66
|
Inhibition of gamma secretase-mediated amyloid beta (1 to 40) production in human SH-SY5Y cells
Inhibition of gamma secretase-mediated amyloid beta (1 to 40) production in human SH-SY5Y cells
|
[PMID: 19694467] |
Compound E reduces the proliferation of T47D, and MCF-7 cell lines by less than 50% at a concentration of 50 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 209986-17-4
-
性状 Solid
-
分子量 490.50
-
分子式 C27H24F2N4O3
-
Color White to light yellow
-
SMILES
FC1=CC(CC(N[C@@H](C)C(N[C@@H]2C(N(C)C(C=CC=C3)=C3C(C4=CC=CC=C4)=N2)=O)=O)=O)=CC(F)=C1
-
別名
γ-Secretase-IN-1
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (18)
-
Journal Impact Factor
-
Most Recent
-
Immunity
The transcription factor MEF2C restrains microglial overactivation by inhibiting kinase CDK2. [Abstract]2025 Mar 21:S1074-7613(25)00093-7. PMID: 40139186 -
Cell Stem Cell
Transcriptional code for circuit integration in the injured brain by transplanted human neurons. [Abstract]2026 Jan 8;33(1):44-57.e7. PMID: 41512834 -
Mol Neurodegener
MS4A6A/Ms4a6d deficiency disrupts neuroprotective microglia functions and promotes inflammation in Alzheimer's disease model. [Abstract]2025 Aug 28;20(1):94. PMID: 40877951
Compound E purchased from MedChemExpress. Usage Cited in: Mol Neurodegener. 2025 Aug 28;20(1):94. [Abstract]
ISF Aβ1-x obtained by microdialysis from 1-month-old APP/PS1:Ms4a6d +/+ mice (blue) and APP/PS1:Ms4a6d +/− mice (magenta). Baseline Aβ1-x levels were defined as the mean concentration from hours 3–5 after probe insertion. Aβ1-x values after γ-secretase inhibitor Compound E (6.7 mg/kg; i.p.) treatment at each time point were expressed as percentage of baseline mean (% baseline). Raw data were fitted with linear trend lines.
-
Nat Commun
N6-methyladenosine modification-mediated mRNA metabolism is essential for human pancreatic lineage specification and islet organogenesis. [Abstract]2022 Jul 18;13(1):4148. PMID: 35851388 -
Sci Adv
2022 Feb 25;8(8):eabk1826. PMID: 35196077 -
-
Cell Rep
Aberrant role of pyruvate kinase M2 in the regulation of gamma-secretase and memory deficits in Alzheimer's disease. [Abstract]2021 Dec 7;37(10):110102. PMID: 34879266 -
Compound E purchased from MedChemExpress. Usage Cited in: Fundam Res. 2026 Jan 10.
Schematic representation of structural morphogenesis of human post-implantation embryoids from hESCs in 3D culture. H9 human embryonic stem cell (hESC) clusters embedded in 100% Matrigel to promote cell adhesion tension. The embedded hESC clusters were then supplemented with CHIR99021, FGF2, LDN193189 and Compound E (2 μM; 3 d) in an N2/B27 basal medium to induce post-implantation embryoid formation.
-
-
Front Cell Dev Biol
Genome-Wide Analysis Identifies Rag1 and Rag2 as Novel Notch1 Transcriptional Targets in Thymocytes. [Abstract]2021 Jul 12:9:703338. PMID: 34322489 -
Front Cell Dev Biol
HIF-1α Affects the Neural Stem Cell Differentiation of Human Induced Pluripotent Stem Cells via MFN2-Mediated Wnt/β-Catenin Signaling. [Abstract]2021 Jun 21:9:671704. PMID: 34235146 -
bioRxiv
ProNotch converts extracellular protease activity into programmable transcriptional outputs. [Abstract]2026 Jun 3:2026.06.01.728985. PMID: 42282718 -
-
bioRxiv
Astrocyte cell-surface proteomics identified CD44 as an OPN/SPP1 receptor regulating lipid metabolism and glial crosstalk in Alzheimer's disease. [Abstract]2025 Dec 9:2025.12.05.692670. PMID: 41427315 -
-
Compound E purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Aug 19.
Efects of protease inhibitors on extracellular and intracellular HO-1 protein levels in cultured rat astrocytes. Astrocytes were incubated with NH4Cl (5 mM) for 48 h before cysteine protease inhibitors (Compound E, 5 µM; E64d, 50 µM) or the ER-associated degradation (ERAD) inhibitor eeyarestatin 1 (ESI, 20 µM) were added and cells were incubated for another 24 h. Fulllength and truncated HO-1 protein were analyzed in cell culture supernatants and cellular lysates by Western blot and quantified by densitometry.
-
-
溶剤 & 溶解度
DMSO : 100 mg/mL (203.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.10 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.10 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
The breast cancer cell lines MDA-MB-231, T47D, and MCF-7 are treated with Compound E at concentrations in the range 0.01-50 μM for 48 h and their viability is determined using a Coulter counter[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
-
データシート (278 KB)
-
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Beher D, et al. Pharmacological knock-down of the presenilin 1 heterodimer by a novel gamma -secretase inhibitor: implications for presenilin biology. J Biol Chem. 2001 Nov 30;276(48):45394-402. [Content Brief]
[2]. Rasul S, et al. Inhibition of gamma-secretase induces G2/M arrest and triggers apoptosis in breast cancer cells. Br J Cancer. 2009 Jun 16;100(12):1879-88. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0387 mL | 10.1937 mL | 20.3874 mL | 50.9684 mL |
| 5 mM | 0.4077 mL | 2.0387 mL | 4.0775 mL | 10.1937 mL | |
| 10 mM | 0.2039 mL | 1.0194 mL | 2.0387 mL | 5.0968 mL | |
| 15 mM | 0.1359 mL | 0.6796 mL | 1.3592 mL | 3.3979 mL | |
| 20 mM | 0.1019 mL | 0.5097 mL | 1.0194 mL | 2.5484 mL | |
| 25 mM | 0.0815 mL | 0.4077 mL | 0.8155 mL | 2.0387 mL | |
| 30 mM | 0.0680 mL | 0.3398 mL | 0.6796 mL | 1.6989 mL | |
| 40 mM | 0.0510 mL | 0.2548 mL | 0.5097 mL | 1.2742 mL | |
| 50 mM | 0.0408 mL | 0.2039 mL | 0.4077 mL | 1.0194 mL | |
| 60 mM | 0.0340 mL | 0.1699 mL | 0.3398 mL | 0.8495 mL | |
| 80 mM | 0.0255 mL | 0.1274 mL | 0.2548 mL | 0.6371 mL | |
| 100 mM | 0.0204 mL | 0.1019 mL | 0.2039 mL | 0.5097 mL |
Compound E 関連分類
HY-14176 関連分類
Powered by Bioz