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DAPT γ-Secretase inhibitor

Cat.No.S2215

DAPT is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells. DAPT enhances the apoptosis of human tongue carcinoma cells and regulates autophagy.

DAPT Secretase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 432.46

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	HDAC Caspase Proteasome MMP HCV Protease Cysteine Protease Tyrosinase HIV Protease DPP Serine Protease
Other Secretase Inhibitors	RO4929097 (RG-4733) LY411575 Nirogacestat (PF-03084014) Dibenzazepine (YO-01027) MK-0752 Semagacestat (LY450139) Avagacestat (BMS-708163) MDL-28170 L-685,458 Itanapraced (CHF 5074)

Solubility in DMSO or Water

In vitro
Batch:

DMSO : 86 mg/mL (198.86 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 41 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 86 mg/mL (198.86 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 39 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 86 mg/mL (198.86 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 86 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 86 mg/mL (198.86 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 43 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 86 mg/mL (198.86 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 43 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.550mg/ml (1.27mM)	Taking the 1 mL working solution as an example, add 50 μL of 11 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.000mg/ml (4.62mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/mL clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify; add 50 μL of Tween-80 to the above system, mix evenly to clarify; Then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Read more about DAPT solubility in DMSO or water

Working Concentrations for Cell Culture Treatment

Read more about DAPT working concentrations for cell culture treatment

Working Concentrations for Animal Model Treatment

Mechanism of Action

Information	DAPT is a potent and cell-permeable γ-secretase inhibitor. It affects Notch and amyloid precursor protein (APP) signaling by blocking the proteolytic cleavage of Notch receptors and APP, effectively inhibiting amyloid-beta (Aβ) production and downstream Notch pathway activation.
Read more about DAPT IC50 for cell-based and cell-free assays
Primary Applications and Mechanism of Action

Read more about DAPT Mechanism of Action

Chemical Information, Storage & Stability

Molecular Weight	432.46	Formula	C₂₃H₂₆F₂N₂O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	208255-80-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	GSI-IX, LY-374973			Smiles	CC(C(=O)NC(C1=CC=CC=C1)C(=O)OC(C)(C)C)NC(=O)CC2=CC(=CC(=C2)F)F

Read more about storage & stability

DAPT Combination Database

Read more comparative analysis about DAPT

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
I would like to ask if you would recommend it used in endothelial cells (e.g. both murine and human endothelial cells).

Answer:
I think this compound can be used in endothelial cells from both human and mouse, please see the following reference: http://www.ncbi.nlm.nih.gov/pubmed/19481797; http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2615564/

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions

Concentration (start):

Dilution-folds:

Computed Result

C1=C0/X	C1:		LOG(C1):
C2=C1/X	C2:		LOG(C2):
C3=C2/X	C3:		LOG(C3):
C4=C3/X	C4:		LOG(C4):
C5=C4/X	C5:		LOG(C5):
C6=C5/X	C6:		LOG(C6):
C7=C6/X	C7:		LOG(C7):
C8=C7/X	C8:		LOG(C8):