Compound E (Synonyms: γ-Secretase-IN-1)

Name: Compound E
Brand: MedChemExpress
SKU: HY-14176
Rating: 5.0 (6 reviews)

Cat. No.: HY-14176 Purity: 99.97%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Compound E is a γ-secretase inhibitor. Compound E bloks β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC₅₀s of 0.24, 0.37, 0.32 nM, respectively.

For research use only. We do not sell to patients.

Compound E Chemical Structure

CAS No. : 209986-17-4

Size	Price	Stock	Quantity
1 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 520	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 830	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1650	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2220	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2995	In-stock	Estimated Time of Arrival: December 31
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500 mg		Get quote

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Based on 6 publication(s) in Google Scholar

Other Forms of Compound E:

(1R,3S)-Compound E Get quote

6 Publications Citing Use of MCE Compound E

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Compound E is a γ-secretase inhibitor. Compound E bloks β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC₅₀s of 0.24, 0.37, 0.32 nM, respectively.

IC₅₀ & Target

IC50: 0.24 nM (β-amyloid(40)), 0.37 nM (β-amyloid(42)), 0.24 nM (Notch)^[1]

Cellular Effect

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]

In Vitro

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.

Molecular Weight

490.50

Formula

C₂₇H₂₄F₂N₄O₃

CAS No.

209986-17-4

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-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)

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0387 mL	10.1937 mL	20.3874 mL
5 mM	0.4077 mL	2.0387 mL	4.0775 mL
10 mM	0.2039 mL	1.0194 mL	2.0387 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.88 mg/mL (5.87 mM); Clear solution

This protocol yields a clear solution of ≥ 2.88 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (28.8 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 2

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.
Protocol 3

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.97%

Select Batch:

Data Sheet (278 KB) SDS (394 KB)

COA (254 KB) HNMR (139 KB) RP-HPLC (168 KB) LCMS (103 KB)

Handling Instructions (2659 KB)

References

[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]

Cell Assay
^[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[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

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 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Compound E209986-17-4γ-Secretase-IN-1γ-secretaseGamma secretaseInhibitorinhibitorinhibit

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Compound E (Synonyms: γ-Secretase-IN-1)

Customer Review

Other Forms of Compound E:

Compound E Related Antibodies

6 Publications Citing Use of MCE Compound E

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Compound E Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Compound E Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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