Home Tools

DAPT

Catalog No. T6202 CAS 208255-80-5

Synonyms: LY-374973, GSI-IX

DAPT (LY-374973) is a γ-secretase inhibitor that inhibits total Aβ and Aβ42 (IC50=115/200 nM) and is orally active. DAPT is also a Notch inhibitor. DAPT induces cell differentiation, autophagy and apoptosis.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

DAPT, CAS 208255-80-5

Pack Size	Availability	Price/USD
5 mg	In stock	$ 53.00
10 mg	In stock	$ 90.00
25 mg	In stock	$ 168.00
50 mg	In stock	$ 293.00
100 mg	In stock	$ 436.00
200 mg	In stock	$ 545.00
500 mg	In stock	$ 878.00
1 mL * 10 mM (in DMSO)	In stock	$ 54.00

Bulk Inquiry

Select Batch

Purity: 99.81%

Purity: 99.79%

Purity: 99.2%

Purity: 98.06%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	DAPT (LY-374973) is a γ-secretase inhibitor that inhibits total Aβ and Aβ42 (IC50=115/200 nM) and is orally active. DAPT is also a Notch inhibitor. DAPT induces cell differentiation, autophagy and apoptosis.
Targets&IC50	Aβ42:200 nM (in human primary neuronal cultures), β-Amyloid:115 nM (in human primary neuronal cultures), β-Amyloid:20 nM (HEK 293 cells)
In vitro	METHODS: Ovarian tumor stem cells (OCSC) HO8910 and SKOV3 were treated with DAPT (1-20 μg/mL) for 24-72 h. Cell viability was measured by MTT. RESULTS: A significant decrease in cell self-renewal and proliferation was observed after incubation with DAPT.DAPT induced a concentration-dependent antiproliferative effect on HO8910 and SKOV3 OCSC-like cells. [1] METHODS: Tumor cells GH3 and primary GHoma were treated with DAPT (20-100 nM) for 24 h. Cell migration was monitored using Transwell. RESULTS: DAPT inhibited the migration of GH3 cells and primary GHoma cells. [2]
In vivo	METHODS: To test the anti-tumor activity in vivo, DAPT (1-5 mg/kg) was injected intraperitoneally into an athymic immune-deficient nude mouse model harboring rat pituitary tumor GH3 one day a day for fifteen days. RESULTS: DAPT treatment significantly inhibited tumor growth, and the expression of Notch2 and DLL3 was down-regulated in DAPT-treated tumors, with no difference in the expression of DLL4 and VEGF. [2] METHODS: To investigate the effect on cisplatin-induced renal injury, DAPT (15 mg/kg in 20% Captisol) was administered intraperitoneally once daily for five days to a cisplatin-induced renal injury model in C57BL/6J mice. RESULTS: DAPT attenuated cisplatin-induced tubular injury and decreased glomerular filtration rate, and the Notch signaling pathway may be a potential therapeutic target for alleviating cisplatin chemotherapy-associated renal complications. [3]
Kinase Assay	water content was 78.83 ± 0.35%. In DAPT group
Cell Research	Human embryonic kidney cells, transfected with the gene for APP751 (HEK 293) were used for routine Ab reduction assays. The Ab peptides secreted from these cells have been characterized previously. Cells were plated in 96-well plates and allowed to adhere overnight in Dulbecco's modified Eagle medium (DMEM) supplemented with 10% heat-inactivated fetal bovine serum. For compound screening and dose±response testing, compounds were diluted from stock solutions in DMSO to yield a final concentration equal to 0.1% DMSO in media. Cells were pre-treated for 2 h at 378C with compounds, media were aspirated off and fresh compound solutions applied. After an additional 2-h treatment period, conditioned media were drawn off and analyzed by a sandwich ELISA (266±3D6) specific for total Ab. Reduction of Ab production was measured relative to control cells treated with 0.1% DMSO and expressed as percentage inhibition. Data from at least six doses in duplicate were fitted to a four-parameter logistical model using XLfit software in order to determine potency [1].
Animal Research	All studies were conducted with three- to four-month-old heterozygous PDAPP transgenic mice overexpressing the APPV717F a mutant form of the amyloid precursor protein. These animals have been previously shown to exhibit many of the neuropathological features of AD and to produce high levels of Ab in a regionally specific manner. Each treatment group (n=10) consisted of equal numbers of age-matched male and female animals that were fasted overnight prior to treatment. Both treatment and control groups were dosed at a volume of 10 mL/kg with compound formulated in corn oil, 5% (v/v) ethanol or vehicle alone. Tissues were processed and all Ab and APP measurements were made as described previously. After removal of the brain, the cortex from one hemisphere was homogenized, extracted with 5 M guanidine, 50 mM Tris ± pH 8.0, centrifuged, and the supernatant was used for Ab measurements. Cortex from the other hemisphere was snap frozen for analysis of compound levels. Ab levels were expressed as ng/g of wet tissue weight, and percentage reductions were calculated relative to the mean Ab level of tissue from vehicle-treated control animals. Data were analyzed with Mann± Whitney non-parametric statistics to assess significance [1].

Synonyms	LY-374973, GSI-IX
Molecular Weight	432.46
Formula	C23H26F2N2O4
CAS No.	208255-80-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: Insoluble

DMSO: 43.2 mg/mL (100 mM)

References and Literature

1. Jiang LY, et al. γ-Secretase Inhibitor, DAPT Inhibits Self-renewal and Stemness Maintenance of Ovarian Cancer Stem-like Cells In Vitro. Chin J Cancer Res. 2011 Jun;23(2):140-6. 2. Feng J, et al. DAPT, a γ-Secretase Inhibitor, Suppresses Tumorigenesis, and Progression of Growth Hormone-Producing Adenomas by Targeting Notch Signaling. Front Oncol. 2019 Aug 27;9:809. 3. Soni H, et al. γ-secretase inhibitor DAPT mitigates cisplatin-induced acute kidney injury by suppressing Notch1 signaling. J Cell Mol Med. 2019 Jan;23(1):260-270. 6. Majumder S, et al. Shifts in podocyte histone H3K27me3 regulate mouse and human glomerular disease. J Clin Invest. 2018 Jan 2;128(1):483-499. 7. Yixin Tao, et al. β-catenin activation in hair follicle dermal stem cells induces ectopic hair outgrowth and skin fibrosis. J Mol Cell Biol. 2018 May 16. 8. Zhou Y, Li X. LxA4 Inhibits LPS Induced Proinflammatory Response and Microglia Polarization through Notch Signaling Pathway[J]. Revista Argentina de Clínica Psicológica. 2021, 30(1): 330. 9. Huang C, Yan T, Xu Z, et al. Hypoxia Enhances Fusion of Oral Squamous Carcinoma Cells and Epithelial Cells Partly via the Epithelial–Mesenchymal Transition of Epithelial Cells[J]. BioMed research international. 2018 Feb 8;2018:5015203. 10. Zhenyu Wang, Weijian Li, Hongshu Jing, Ming Ding, Gong-Bo Fu, Tianjie Yuan, Weijian Huang, Mengjun Dai, Dan Tang, Min Zheng, Yi Chen, Hongdan Zhang, Yuan Peng, Qigen Li, Weifeng Yu, Hexin Yan, Bo Zhai . Generation of hepatic spheroids using human hepatocyte-derived liver progenitor-like cells for hepatotoxicity screening. Theranostics.

Citations

1. Wang Z, Li W, Jing H, et al. Generation of hepatic spheroids using human hepatocyte-derived liver progenitor-like cells for hepatotoxicity screening. Theranostics. 2019, 9(22): 6690 2. Cai N, Xu B, Li X, et al. Roflumilast, a cyclic nucleotide phosphodiesterase 4 inhibitor, protects against cerebrovascular endothelial injury following cerebral ischemia/reperfusion by activating the Notch1/Hes1 pathway. European Journal of Pharmacology. 2022: 175027 3. Huang C, Yan T, Xu Z, et al. Hypoxia Enhances Fusion of Oral Squamous Carcinoma Cells and Epithelial Cells Partly via the Epithelial–Mesenchymal Transition of Epithelial Cells. BioMed Research International. 2018 Feb 8;2018:5015203 4. Yang L, Wang X, Zhao G, et al.Leveraging temporal Wnt signal for efficient differentiation of intestinal stem cells in an organoid model.Stem Cells and Development.2023 (ja). 5. Qu R, Peng Y, Zhou M, et al.MiR-223-3p attenuates M1 macrophage polarization via suppressing the Notch signaling pathway and NLRP3-mediated pyroptosis in experimental autoimmune uveitis.European Journal of Pharmacology.2023, 960: 176139.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Neurodegenerative Disease Compound Library Anti-Alzheimer's Disease Compound Library Autophagy Compound Library Human Metabolite Library Neuronal Differentiation Compound Library Orally Active Compound Library Bioactive Compounds Library Max NO PAINS Compound Library Stem Cell Differentiation Compound Library

Related Products

Related compounds with same targets

Cardanol (C15:1) Antitumor agent-112 Trigonelline Selonsertib XX-650-23 ASP3026 Simmiparib Tauroursodeoxycholate sodium

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

DAPT 208255-80-5 Apoptosis Autophagy Neuroscience Proteases/Proteasome Stem Cells Beta Amyloid Gamma-secretase Gamma secretase Amyloid-β Inhibitor LY-374973 LY374973 Abeta LY 374973 Notch γ-secretase inhibit β-amyloid peptide GSI-IX inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.