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DAPT

Cat. No. M1746
DAPT Structure
Synonym:

GSI-IX

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 55  USD55 In stock
5mg USD 50  USD50 In stock
10mg USD 85  USD85 In stock
50mg USD 250  USD250 In stock
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Quality Control & Documentation
Biological Activity

DAPT (GSI-IX) is a γ-secretase inhibitor with IC50 values of 115 and 200 nM for total Aβ and Aβ42 respectively. DAPT (GSI-IX) may be useful in the study of β-amyloid (Aβ) formation. As an inhibitor of Notch, DAPT may advance studies of autoimmune and lymphoproliferative diseases, such as ALPS and lupus erythematosus (SLE). Other γ-secretase substrates include LDL receptor-related protein, E-cadherin and ErbB-4.

Product Citations
Customer Product Validations & Biological Datas
Source Oncol Lett (2017). Figure 6. DAPT (AbMole BioScience, Shanghai, China)
Method Co‑IP assay
Cell Lines SMMC‑7721 cells
Concentrations 1 μM
Incubation Time
Results The interaction between Jagged1 and Notch1 in SMMC‑7721 cells was also significantly reduced after adding DAPT compared with that of the normal serum group (P<0.01) (Fig. 6).
Source Oncol Lett (2017). Figure 5. DAPT (AbMole BioScience, Shanghai, China)
Method Western blot
Cell Lines SMMC‑7721 cells
Concentrations 1 μM
Incubation Time
Results The levels of Jagged1 and Notch1 were decreased after adding the Notch inhibitor, DAPT, indicating that DAPT successfully inhibited the Jagged1/Notch signaling pathway. In addition, the expression of VEGF protein was reduced after adding DAPT (Fig. 5).
Source Circ Res (2017). Figure 2. DATP (Abmole Bioscience)
Method Retina dissection and whole mount staining
Cell Lines mice
Concentrations 100 mg/kg
Incubation Time
Results DAPT treatment resulted in a large increase in vessel density and expansion of the vascular plexus in the postnatal retina of control mice (Fig. 2A, C, E, G). DAPT completely rescued the defect in SENP1-ecKO pups (Fig. 2B, D, F, H), which resulted in vascular length, vascular coverage, and tip sprouts growth comparable to the control group (Fig. 2I-K).
Source Sci adv (2015). Figure 5. The DAPT g-secretase inhibitor was obtained from AbMole BioScience.
Method Immunohistochemistry
Cell Lines
Concentrations 100 mg/kg, daily
Incubation Time
Results "The PlGF-modulated opposing vascular effects in relation to Dll4-Notch inhibition alter tumor growth by changing the microenvironment, tumor cell proliferation, and apoptosis."
Source Sci adv (2015). Figure 4. The DAPT g-secretase inhibitor was obtained from AbMole BioScience.
Method human tumor models, Immunohistochemistry
Cell Lines
Concentrations 100 mg/kg, daily
Incubation Time
Results PlGF mediates opposing vascular effects in nontreated and Dll4-Notch inhibitor–treated mouse tumors.
Source Sci adv (2015). Figure 3. The DAPT g-secretase inhibitor was obtained from AbMole BioScience.
Method Immunohistochemistry
Cell Lines Human JE-3, BeWo, MDA-MB-231 cells
Concentrations 100 mg/kg, daily
Incubation Time
Results "Both terminal deoxynucleotidyl transferase–mediated deoxyuridine triphosphate nick end labeling (TUNEL) staining and measurements of the activated or cleaved caspase 3 showed reductions of apoptotic cells in Dll4-Notch inhibitor–treated JE-3 and BeWo tumors. In contrast, treatment of PlGF-negative MDAMB-231 tumors with DAPT and Dll4 blockade showed completely opposite effects on cell proliferation and apoptosis, tipping the balance toward an apoptotic phenotype."
Source Sci adv (2015). Figure 1. The DAPT g-secretase inhibitor was obtained from AbMole BioScience.
Method Immunohistochemistry
Cell Lines Human JE-3, BeWo, MDA-MB-231 cells
Concentrations 100 mg/kg, daily
Incubation Time
Results "PlGF expression determines opposing effects of Dll4-Notch inhibition on human tumor growth and vascular remodeling."
Protocol (for reference only)
Cell Experiment
Cell lines SK-MES-1
Preparation 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.
Concentrations 2.5 ~ 160 μM
Incubation time 72 h
Animal Experiment
Animal models three‐ to four‐month‐old heterozygous PDAPP transgenic mice overexpressing the APPV717F mutant form of the amyloid precursor protein
Formulation formulated in corn oil, 5% (v/v) ethanol
Dosages 100 mg/kg
Administration s.c.
Chemical Information
Molecular Weight 432.46
Formula C23H26F2N2O4
CAS Number 208255-80-5
Solubility (25°C) DMSO 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Kim BK et al. J Am Coll Cardiol. A New Strategy for Discontinuation of Dual Antiplatelet Therapy: The RESET Trial (REal Safety and Efficacy of 3-month dual antiplatelet Therapy following Endeavor zotarolimus-eluting stent implantation).

[2] Kedhi E et al. EuroIntervention. Stent thrombosis: insights on outcomes, predictors and impact of dual antiplatelet therapy interruption from the SPIRIT II, SPIRIT III, SPIRIT IV and COMPARE trials.

[3] Oikawa et al. Neurosci Lett. The γ-secretase inhibitor DAPT increases the levels of gangliosides at neuritic terminals of differentiating PC12 cells.

[4] Zou et al. Clin Exp Med. Gamma-secretase inhibitor DAPT suppresses glioblastoma growth via uncoupling of tumor vessel density from vessel function.

[5] H F Dovey, et al. J Neurochem. Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain

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Keywords: DAPT, GSI-IX supplier, Gamma-secretase/Beta-secretase, inhibitors, activators


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