For research use only.

Catalog No.S2215 Synonyms: LY-374973

232 publications

DAPT (GSI-IX) Chemical Structure

CAS No. 208255-80-5

DAPT (GSI-IX, LY-374973) 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.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 112 In stock
USD 70 In stock
USD 120 In stock
USD 210 In stock
USD 370 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's DAPT (GSI-IX) has been cited by 232 publications

Purity & Quality Control

Choose Selective Gamma-secretase Inhibitors

Biological Activity

Description DAPT (GSI-IX, LY-374973) 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.
γ secretase(Aβ) [1]
(HEK 293 cells)
20 nM
In vitro

In human primary neuronal cultures, DAPT also shows inhibitory effects on Aβ production with IC50 of 115 nM and 200 nM respectively for Aβ total and Aβ42, which is 5-10-fold lower than is observed in HEK 293 cells. [1] A recent study shows that DAPT inhibits the proliferation of SK-MES-1 cells in a concentration-dependent manner with IC50 of 11.3 μM. In addition, DAPT also induces caspase-dependent and caspase-independent apoptosis in lung squamous cell carcinoma cells by inhibiting Notch receptor signaling pathway. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 CD133− NWDFd2k5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLIN2UzKM7:TR?= M1HsR|Q5KGh? M2TqeIVvcGGwY3XzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iaX7keYNm\CCkeTDDSGRR NHLXfngzPDVyMkm0PS=>
A549 CD133+ MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV:yJO69VQ>? NGnIOnI1QCCq NHKzUXFmdmijbnPld{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIHnu[JVk\WRiYomgR2RFWA>? M1XDWFI1PTB{OUS5
HT29  NXTwXGtLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13kSFAvPS15NTFOwG0> MWOxNk8zPC92ODDo MojGSG1UVw>? MljQbY5pcWKrdIOgeIhmKGOnbHyg[5Jwf3SqIHnuJIEh[2:wY3XueJJifGmxbjDtZY5v\XJ? NE\PSVkzPTJ3N{m0OS=>
SHG-44 NF\lb2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn2wNE42NTFyIN88US=> NHn1fnQyNTViZB?= MW\pcohq[mm2czD0bIUh[2WubDD2bYFjcWyrdImgZZQhfGinIH;weIlu[WxiY3;uZ4VvfHKjdHnvckBw\iBzIN88US=> Mn\kNlUxPjN{OEW=
MG63 NWXROHlMTnWwY4Tpc44hSXO|YYm= M2XzSFExOCEQvF2= MVKyOEBp M2XudGROW09? NXHtcI4x\GW|ZX7zbZRqgmW|IITo[UBk\WyuIHzpcoUhfG9iY3nzdIxifGmwIITy[YF1dWWwdB?= M17ZbVI1QDl2Mkm3
Saos-2 MnLqSpVv[3Srb36gRZN{[Xl? NEL2bmEyODBizszN M4PCOlI1KGh? MXPEUXNQ NF7zNpRl\XOnboPpeIl7\XNidHjlJINmdGxibHnu[UB1dyClaYPwcIF1cW5idILlZZRu\W62 MVyyOFg6PDJ7Nx?=
U251 NWftSpllT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHJNkDPxE1? M2TKNVQ5KGh? NIHrO4lFVVOR M1PROZN1emWwZ4To[Y5{yqC2LVHVR2IucW6mdXPl[EBk\WyuIHfyc5d1cCC|dYDwdoV{e2mxbh?= M{f1OlI1Pzl|M{Gz
U87  MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPvU2dKOiEQvF2= NI\WXIk1QCCq M{TN[mROW09? MnfMd5Rz\W6pdHjlcpPDqHRvQWXDRk1qdmS3Y3XkJINmdGxiZ4Lve5RpKHO3cIDy[ZN{cW:w NFS5SmwzPDd7M{OxNy=>
U251 NH22NmhHfW6ldHnvckBCe3OjeR?= MXeyJO69VQ>? MlToOFghcA>? M1Hj[2ROW09? Mk\YZoxw[2u|wrD0MWFWS0JvaX7keYNm\CCjY4TpeoF1cW:wIH;mJJRp\SCyM{igUWFRUy:PQWDLRXBMOi:Kc4CyO{Bx[XSqd3H5JIFv\CCrbnjpZol1eyCneIDy[ZN{cW:wIH;mJG5KS0Rz NXnUTVBbOjR5OUOzNVM>
U87  NV7iVIl2TnWwY4Tpc44hSXO|YYm= NEfnR5QzKM7:TR?= MoTFOFghcA>? MU\EUXNQ MWPicI9kc3QEoIStRXVESi2rbnT1Z4VlKGGldHn2ZZRqd25ib3[geIhmKHB|ODDNRXBMN02DUFvBVGszN0i|cEK3JJBifGi5YYmgZY5lKGmwaHnibZR{KGW6cILld5Nqd25ib3[gUmlETDF? MmnrNlQ4QTN|MUO=
A549  MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nvOlExKM7:TR?= MUGyOIg> MYLk[YNz\WG|ZYOgeIhmKGOnbHygeoli[mmuaYT5JINwdWKrbnXkJJdqfGhiUGTF MX6yN|Y4OTZzOR?=
GC-B  M1fRRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TJblYvOjVvMUCwJO69VQ>? M{KyNFI1KGh? NV3YOJRCTE2VTx?= NE\JUIhqdmirYnn0d{B1cGViY3XscEBoem:5dHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NFj6UJQyQTV2MkS0Oi=>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
Snail / N-cadherin / Vimentin / E-cadherin; 

PubMed: 24932308     

EMT markers were analyzed in AGS and MKN45 cells by immunoblotting following treatment with DAPT or the DMSO control.

Bax / caspase-3 / Bcl-2; 

PubMed: 29487808     

Western blot analysis of Bax, caspase-3, and Bcl-2 protein expression.

NICD / Pax7 / Pax3 / MyoD / Myogenin / p21; 

PubMed: 18957511     

(A) Primary myoblasts, incubated in GM until 90–100% confluency, were transferred to DM and were incubated for 1 day in the presence of DMSO or 5 μM GM6001, a metalloproteinase inhibitor (left), or in the presence of DMSO or 1 μM DAPT, a γ-secretase inhibitor (right). The levels of NICD, Pax7, Pax3, MyoD, myogenin, and p21 were determined by Western blotting, tubulin is a gel-loading control. A representative experiment out of three is shown.

24932308 29487808 18957511
Growth inhibition assay
Cell viability; 

PubMed: 27118928     

Cell viability of CPH036 or CPH047 cells following 7 days of treatment with iressa, DAPT or a combination in the indicated doses (mean ± SEM, n = 5). *p < 0.05, **p < 0.01, ***p < 0.001.


PubMed: 18662245     

Fixed E18 rat embryonic cortical neurons cells were immunostained for cdk5 (a, e) and p35 (b, f). Nuclei are stained with DAPI (c, g). Immunostaining for cdk5, p35 and DAPI are merged (d, h).

In vivo DAPT administration (100mg/kg) leads to a robust and sustained pharmacodynamic effect in PDAPP mice that DAPT levels in the brain exceeds 100 ng/g within 1 hour and persists up to 18 hours after administration, with peak levels of 490 ng/g observed after 3 hour. And during the period, DAPT (100 mg/kg) also reduces the cortical total Aβ and Aβ42 in a dose-dependent manner with a 50% reduction. [1] In rat cerebral cortexes, DAPT (40 mg/kg) suppresses the LPS-induced activity of γ-secretase and increases the cell apoptosis with the prolonged neuroinflammation. [3]


Kinase Assay:[1]
- Collapse

In vitro Aβ reduction assays :

Human embryonic kidney cells (American Type Culture Collection CRL-1573), transfected with the gene for APP751 (HEK 293) are used for routine Aβ reduction assays. Cells are 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. DAPT are diluted from stock solutions in dimethylsulfoxide (DMSO) to yield a final concentration equal to 0.1% DMSO in media. Cells are pre-treated for 2 hours at 37 °C with DAPT, media are aspirated off and fresh compound solutions applied. After an additional 2-hour treatment period, conditioned media is drawn off and analyzed by a sandwich ELISA (266–3D6) specific for total Aβ. Reduction of Aβ production is measured relative to control cells treated with 0.1% DMSO and expressed as a percentage inhibition. Data from at least six doses in duplicate are fitted to a four-parameter logistical model using XLfit software in order to determine potency. Human and PDAPP mouse neuronal cultures are grown in serum-free media to enhance their neuronal characteristics, and appeared to be greater than 90% neurons after maturation prior to use. Conditioned media to establish baseline Aβ values are collected by adding fresh media to each well and incubated for 24 hours at 37 °C in the absence of DAPT. Cultures are then treated with fresh media containing DAPT at the desired range of concentrations for an additional 24 hours at 37 °C, and conditioned media collected. For the measurement of total Aβ, samples are analyzed with the same ELISA (266–3D6) as used for the HEK 293 cell assays. Analyses of samples for Aβ42 production are performed by a separate ELISA (21F12–3D6) that utilizes a capture antibody specific for the Aβ42 C-terminus. Inhibition of production for both total Aβ and Aβ42 are determined by the difference between the values for the compound treatment and baseline periods. After plotting percentage inhibition versus DAPT concentration, data are analyzed with XLfit software, as above, to determine potency.
Cell Research:[2]
- Collapse
  • Cell lines: SK-MES-1
  • Concentrations: 2.5 μM to 160 μM
  • Incubation Time: 72 hours
  • Method: Cells are seeded into 96-well plates and exposed to 0.1% DMSO or DAPT at concentrations in the range of 2.5 μM–160 μM for 72 hours. Cytotoxicity is determined with 3-(4, 5)-dimethylthiahiazo-(-z-y1)-3, 5-di-phenytetrazoliumromide (MTT) dye reduction assay with minor modifications. Briefly, after incubation with DAPT, 20 μL MTT solution (5 mg/mL in PBS) is added to 180 μL medium in each well and plates are incubated for 4 hours at 37 °C, and subsequently 150 μL DMSO is added to each well, and mixed by shaking at room temperature for 15 minutes. Absorption is measured by an enzyme-linked immunosorbent assay at 490 nm to determine absorbance values. α-MEM supplemented with the same amount of MTT solution and solvent is used as blank solution. The IC50 value is calculated using PROBIT program in SPSS.
    (Only for Reference)
Animal Research:[1]
- Collapse
  • Animal Models: Heterozygous PDAPP transgenic mice overexpressing the APPV717F mutant form of the amyloid precursor protein.
  • Dosages: ≤100 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 86 mg/mL (198.86 mM)
Water Insoluble
Ethanol '50 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+corn oil
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 432.46


CAS No. 208255-80-5
Storage powder
in solvent
Synonyms 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

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 ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Molecular Weight

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

Dilution Calculator

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 )

  • C1

* 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

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

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 in 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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04470934 Not yet recruiting Device: SeQuent® SCB drug-coated balloon catheter Coronary Artery Disease|Myocardial Ischaemia B. Braun Melsungen AG November 2020 --
NCT04475536 Not yet recruiting Device: TANSEI stent Ischemic Heart Disease|Coronary Artery Disease Fundación EPIC September 1 2020 --

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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

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

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    Could you please help test the formulation of S2215 for in vivo studies?

  • Answer:

    S2215 DAPT in 30% PEG400+0.5% Tween80+5% Propylene glycol at 10 mg/ml is a suspension. We tried to add some EtOH, and it dissolved clearly in organice solvents, but when water added, the precipitation went out immediately. Then we tried other vehicles, and found S2215 can be dissolved in 4% DMSO+corn oil at 10 mg/ml clearly.

  • Question 2:

    I would like to ask if you would recommend this product used in endothelial cells (e.g. both murine and human endothelial cells).

  • Answer:

    I think DAPT 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/

Gamma-secretase Signaling Pathway Map

Gamma-secretase Inhibitors with Unique Features

Related Gamma-secretase Products

Tags: buy DAPT (GSI-IX) | DAPT (GSI-IX) supplier | purchase DAPT (GSI-IX) | DAPT (GSI-IX) cost | DAPT (GSI-IX) manufacturer | order DAPT (GSI-IX) | DAPT (GSI-IX) distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID