DAPT
Based on 161 publication(s) in Google Scholar
DAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor with IC50s of 115 nM and 200 nM for total amyloid-β (Aβ) and Aβ42, respectively. DAPT inhibits the activation of Notch 1 signaling and induces cell differentiation. DAPT also induces autophagy and apoptosis. DAPT has neuroprotection activity and has the potential for autoimmune and lymphoproliferative diseases, degenerative disease and cancers treatment.
For research use only. We do not sell to patients.
- Purity: 99.97%
- CAS No.: 208255-80-5
- Formula: C23H26F2N2O4
- Molecular Weight:432.46
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) DAPT
More- Nature. 2026 Jan;649(8098):1032-1041. [Abstract]
- Science. 2022 Dec 2;378(6623):eabo5503. [Abstract]
- Nat Biotechnol. 2023 Sep;41(9):1287-1295. [Abstract]
- Nat Immunol. 2026 Mar 3. [Abstract]
- Mil Med Res. 2020 Sep 6;7(1):42. [Abstract]
- Adv Funct Mater. 2026 Jan 8.
- Hepatology. 2016 Jul;64(1):175-88. [Abstract]
- Nat Commun. 2025 Nov 26;16(1):10514. [Abstract]
- Nat Commun. 2025 May 14;16(1):4475. [Abstract]
- Nat Commun. 2023 Oct 20;14(1):6669. [Abstract]
- Acta Pharm Sin B. 2024 Jul;14(7):3049-3067. [Abstract]
- Adv Sci (Weinh). 2026 Jan 21:e18084. [Abstract]
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- Adv Sci (Weinh). 2022 Sep;9(26):e2202505. [Abstract]
- J Clin Invest. 2018 Jan 2;128(1):483-499. [Abstract]
- Neuro Oncol. 2023 Oct 3;25(10):1788-1801. [Abstract]
- Theranostics. 2022 Oct 17;12(17):7250-7266. [Abstract]
- Theranostics. 2021 Jan 1;11(6):2788-2805. [Abstract]
- Theranostics. 2019 Jul 9;9(16):4827-4840. [Abstract]
- J Adv Res. 2025 May 13:S2090-1232(25)00343-1. [Abstract]
- J Nanobiotechnology. 2026 Mar 6;24(1):345. [Abstract]
- Sci Adv. 2026 Mar 27;12(13):eaea8280. [Abstract]
- Sci Adv. 2026 Feb 20;12(8):eadz8405. [Abstract]
- Sci Adv. 2025 Dec 5;11(49):eady7272. [Abstract]
- Sci Adv. 2024 Jul 12;10(28):eadn2091. [Abstract]
- Sci Adv. 2021 Apr 14;7(16):eabb2213. [Abstract]
- J Biomed Sci. 2023 Jun 12;30(1):39. [Abstract]
- Brain. 2026 Feb 19:awag070. [Abstract]
- J Hazard Mater. 2025 Oct 17:499:140149. [Abstract]
- J Allergy Clin Immunol. 2017 Mar;139(3):987-996.e10. [Abstract]
- MedComm (2020). 2026 Feb 5;7(2):e70628. [Abstract]
- Cell Death Dis. 2019 Sep 12;10(9):681. [Abstract]
- Genes Dis. 2020 Nov 21;8(6):867-881. [Abstract]
- Proc Natl Acad Sci U S A. 2017 May 30;114(22):E4425-E4434. [Abstract]
- Cell Commun Signal. 2025 Oct 1;23(1):403. [Abstract]
- Dev Cell. 2025 Jun 25:S1534-5807(25)00362-4. [Abstract]
- Int J Biol Macromol. 2025 Jun 4;318(Pt 1):144963. [Abstract]
- Acta Pharmacol Sin. 2024 Dec;45(12):2553-2566. [Abstract]
- Phytomedicine. 2022 Dec:107:154466. [Abstract]
- Phytomedicine. 2022 Jan:95:153870. [Abstract]
- Phytomedicine. 2021 Mar:83:153488. [Abstract]
- Free Radic Biol Med. 2024 Aug 10:S0891-5849(24)00582-3. [Abstract]
- Sci Total Environ. 2020 Aug 20;731:139234. [Abstract]
- Biomed Pharmacother. 2025 Nov 6:193:118716. [Abstract]
- Biomed Pharmacother. 2018 Nov:107:1370-1376. [Abstract]
- Stem Cell Res Ther. 2025 Nov 5;16(1):617. [Abstract]
- Environ Pollut. 2025 Jun 16:126684. [Abstract]
- Stem Cell Res Ther. 2024 Dec 18;15(1):478. [Abstract]
- Aging Dis. 2019 Aug 1;10(4):719-730. [Abstract]
- Neural Regen Res. 2019 Mar;14(3):452-461. [Abstract]
- Mater Today Chem. aterials Today Chemistry 12 (2019) 78e84
- J Agric Food Chem. 2022 Jul 27;70(29):9166-9178. [Abstract]
- J Agric Food Chem. 2022 Mar 9;70(9):2889-2897. [Abstract]
- Ecotoxicol Environ Saf. 2024 Jan 1:269:115727. [Abstract]
- JCI Insight. 2022 Dec 8;7(23):e162402. [Abstract]
- Ecotoxicol Environ Saf. 2022 Nov:246:114183. [Abstract]
- Food Biosci. April 2022, 101571.
- J Mol Cell Biol. 2019 Jan 1;11(1):26-38. [Abstract]
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- Breast Cancer Res. 2025 May 26;27(1):92. [Abstract]
- Int J Mol Sci. 2024 May 21;25(11):5588. [Abstract]
- Cell Prolif. 2019 Nov;52(6):e12689. [Abstract]
- Inflamm Res. 2019 Sep;68(9):761-774. [Abstract]
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- Cells. 2026 Jun 17;15(12):1101. [Abstract]
- Cells. 2025 Apr 21;14(8):620. [Abstract]
- Microchem J. 2026 Jan 6;221:116840.
- Life Sci. 2023 Sep 1:328:121921. [Abstract]
- Drug Des Devel Ther. 2018 Nov 8:12:3847-3854. [Abstract]
- Immunology. 2022 Aug 29. [Abstract]
- Inflammation. 2019 Dec;42(6):1980-1989. [Abstract]
- Stem Cells Transl Med. 2024 Jan 12;13(1):83-99. [Abstract]
- Int J Mol Sci. 2023 Mar 27;24(7):6295. [Abstract]
- Biomolecules. 2026 Feb 20;16(2):328. [Abstract]
- Bioorg Chem. 2025 Sep 17:165:109010. [Abstract]
- Invest Ophthalmol Vis Sci. 2025 Jun 2;66(6):25. [Abstract]
- Int Immunopharmacol. 2023 Mar:116:109832. [Abstract]
- Eur J Pharmacol. 2022 Aug 5:928:175130. [Abstract]
- Int Immunopharmacol. 2020 Feb;79:106107. [Abstract]
- Int J Cancer. 2018 Aug 1;143(3):645-656. [Abstract]
- Toxicology. 2025 Jun 17:154216. [Abstract]
- Cancer Sci. 2024 Feb;115(2):412-426. [Abstract]
- Front Cell Dev Biol. 2020 Aug 6;8:744. [Abstract]
- FASEB J. 2025 Jan 15;39(1):e70304. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2022 Aug 1;1868(8):166413. [Abstract]
- Mediators Inflamm. 2021 Oct 4:2021:1791222. [Abstract]
- J Inflamm Res. 2025 Oct 10:18:14113-14129. [Abstract]
- iScience. 2025 Apr 3;28(5):112344. [Abstract]
- iScience. 2023 Apr 14;26(5):106670. [Abstract]
- Toxicol Sci. 2019 Sep 1;171(1):1-12. [Abstract]
- Oncol Res. 2019 Jun 21;27(6):643-651. [Abstract]
- iScience. 2019 Sep 27;19:1248-1259. [Abstract]
- Neurochem Int. 2025 May:185:105953. [Abstract]
- J Neurochem. 2023 Aug;166(4):747-762. [Abstract]
- Toxins. 2021 Aug 22;13(8):585. [Abstract]
- J Cell Physiol. 2018 Mar;233(3):2225-2237. [Abstract]
- J Biol Chem. 2026 Jan 20:111182. [Abstract]
- Sci Rep. 2025 Dec 18. [Abstract]
- Biomedicines. 2025 Oct 21;13(10):2574. [Abstract]
- Sci Rep. 2025 May 8;15(1):16133. [Abstract]
- Sci Rep. 2024 Nov 26;14(1):29286. [Abstract]
- Biomedicines. 2022 Apr 18;10(4):928. [Abstract]
- J Biol Chem. 2024 Jul 4:107530. [Abstract]
- Oncol Rep. 2020 Aug;44(2):438-448. [Abstract]
- ACS Chem Neurosci. 2018 Dec 19;9(12):3175-3185. [Abstract]
- Front Med. 2025 Dec 27. [Abstract]
- Food Chem Toxicol. 2024 May 9:114724. [Abstract]
- Front Med. 2021 Sep 23;8:746298. [Abstract]
- Exp Cell Res. 2020 Feb 15;387(2):111806. [Abstract]
- Microb Pathogenesis. 2020 Jan;138:103826. [Abstract]
- Mol Med Rep. 2019 Jun;19(6):5227-5236. [Abstract]
- Eur J Med Res. 2025 Sep 23;30(1):851. [Abstract]
- Andrology. 2022 Nov;10(8):1644-1659. [Abstract]
- Stem Cells Int. 2021 Apr 9:2021:8859071. [Abstract]
- J Cancer. 2022 Jan 1;13(2):527-540. [Abstract]
- Front Neurosci. 2021 Jan 28:15:579431. [Abstract]
- Kaohsiung J Med Sci. 2025 Jan 10:e12930. [Abstract]
- Oral Dis. 2023 Apr;29(3):913-922. [Abstract]
- J Biochem Mol Toxicol. 2025 Feb;39(2):e70129. [Abstract]
- Neuroscience. 2022 Nov 10:504:33-46. [Abstract]
- J Orthop Surg Res. 2021 Nov 6;16(1):660. [Abstract]
- J Cell Biochem. 2019 Feb;120(2):1903-1915. [Abstract]
- Animals (Basel). 2024 Feb 9;14(4):585. [Abstract]
- DNA Repair. 2023 Nov:131:103580. [Abstract]
- PLoS One. 2018 Feb 15;13(2):e0193037. [Abstract]
- Traffic. 2023 Jan;24(1):20-33. [Abstract]
- Toxicon. 2026 Jan:269:108660. [Abstract]
- Virology. 2025 Jun 27:610:110615. [Abstract]
- Biochem Biophys Res Commun. 2021 Apr 2:547:131-138. [Abstract]
- Int Arch Allergy Immunol. 2023;184(2):122-131. [Abstract]
- Biol Open. 2021 Mar 3;10(3):bio056432. [Abstract]
- J Matern Fetal Neonatal Med. 2023 Dec;36(2):2264447. [Abstract]
- Am J Transl Res. 2021 May 15;13(5):4835-4843. [Abstract]
- Neurol Res. 2019 Jul;41(7):658-664. [Abstract]
- J Vis Exp. 2025 Jan 31:(215). [Abstract]
- bioRxiv. 2026 Jun 3:2026.06.01.728985. [Abstract]
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- Res Sq. 2026 Feb 2.
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- bioRxiv. 2024 Aug 1:2024.08.01.606248. [Abstract]
- SSRN. 2024 May 30.
- Universidad de Navarra. 2024 Feb 28.
- Research Square Preprint. 2024 Jan 19.
- bioRxiv. 2023 Nov 5:2023.10.29.560483. [Abstract]
- Research Square Print. 2022 Nov 29.
- Research Square Preprint. 2022 Jul.
- Research Square Preprint. 2022 Feb.
- Methods Mol Biol. 2022:2454:811-827. [Abstract]
- Yale University. 2016 Jan.
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Cell Proliferation/Viability Assay
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WB
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WB
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Cell Proliferation/Viability Assay
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WB
Biological Activity
IC50: 115 nM (Aβ), 200 nM (Aβ42)[5]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
34200 nM
Compound: DAPT
|
Displacement of [3H]L685458 from human SPP expressed in HEK293 cells
Displacement of [3H]L685458 from human SPP expressed in HEK293 cells
|
[PMID: 17932033] |
| Hep 3B2 | IC50 |
5 μM
Compound: DAPT
|
Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by SRB assay
Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by SRB assay
|
[PMID: 30108693] |
| Huh-7 | IC50 |
5 μM
Compound: DAPT
|
Cytotoxicity against human HuH7 cells assessed as growth inhibition after 72 hrs by SRB assay
Cytotoxicity against human HuH7 cells assessed as growth inhibition after 72 hrs by SRB assay
|
[PMID: 30108693] |
| Mahlavu | IC50 |
5 μM
Compound: DAPT
|
Cytotoxicity against human Mahlavu cells assessed as growth inhibition after 72 hrs by SRB assay
Cytotoxicity against human Mahlavu cells assessed as growth inhibition after 72 hrs by SRB assay
|
[PMID: 30108693] |
| SNU-475 | IC50 |
0.6 μM
Compound: DAPT
|
Cytotoxicity against human SNU475 cells assessed as growth inhibition after 72 hrs by SRB assay
Cytotoxicity against human SNU475 cells assessed as growth inhibition after 72 hrs by SRB assay
|
[PMID: 30108693] |
| THP-1 | IC50 |
6.3 nM
Compound: DAPT
|
Displacement of [3H]IN973 from gamma-secretase in human THP1 cells
Displacement of [3H]IN973 from gamma-secretase in human THP1 cells
|
[PMID: 17932033] |
| THP-1 | IC50 |
>100000 nM
Compound: DAPT
|
Displacement of [3H]L685458 from gamma-secretase in human THP1 cells
Displacement of [3H]L685458 from gamma-secretase in human THP1 cells
|
[PMID: 17932033] |
DAPT inhibits Aβ production over 90%, effects only a modest reduction in APPβ in the culture media. Although APPβ is reduced by about 30% by DAPT treatment, this effect is not concentration-dependent and is reversed by the removal of DAPT[1].
CNE-2 cells are treated with increasing concentrations of DAPT (0, 25, 50 and 75 μM), and the γ-secretase-generated Notch 1 fragment Val1744-NICD is decreased after 48 h in a dose-dependent manner (P<0.01). The activation of γ-secretase is almost completely inhibited by DAPT at the concentration of 50 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
DAPT protects brain against cerebral ischemia by down-regulating the expression of Notch 1 and Nuclear factor kappa B in rats. Western blot analyses also show a significant decrease of Notch 1 and NF-κB expression in DAPT (0.03 mg/kg) group (P<0.05 vs. MCAO group)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 208255-80-5
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Appearance Solid
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Molecular Weight 432.46
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Formula C23H26F2N2O4
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Color White to off-white
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SMILES
FC1=CC(F)=CC(CC(N[C@H](C(N[C@H](C(OC(C)(C)C)=O)C2=CC=CC=C2)=O)C)=O)=C1
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Synonyms
GSI-IX
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (161)
-
Journal Impact Factor
-
Most Recent
-
Nature
2026 Jan;649(8098):1032-1041. PMID: 41299171 -
Science
2022 Dec 2;378(6623):eabo5503. PMID: 36454848 -
Nat Biotechnol
Tension-tuned receptors for synthetic mechanotransduction and intercellular force detection. [Abstract]2023 Sep;41(9):1287-1295. PMID: 36646932 -
Nat Immunol
Exclusion of Notch from the contact site during efferocytosis restricts anticancer immunity. [Abstract]2026 Mar 3. PMID: 41776100 -
Mil Med Res
Efficient and rapid conversion of human astrocytes and ALS mouse model spinal cord astrocytes into motor neuron-like cells by defined small molecules. [Abstract]2020 Sep 6;7(1):42. PMID: 32892745 -
-
Hepatology
Intrahepatic bile ducts are developed through formation of homogeneous continuous luminal network and its dynamic rearrangement in mice. [Abstract]2016 Jul;64(1):175-88. PMID: 26926046 -
Nat Commun
2025 Nov 26;16(1):10514. PMID: 41298370 -
Nat Commun
Macrophage-augmented intestinal organoids model virus-host interactions in enteric viral diseases and facilitate therapeutic development. [Abstract]2025 May 14;16(1):4475. PMID: 40368896 -
Nat Commun
Imaging and multi-omics datasets converge to define different neural progenitor origins for ATRT-SHH subgroups. [Abstract]2023 Oct 20;14(1):6669. PMID: 37863903
DAPT purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Oct 20;14(1):6669. [Abstract]
Dose response curve assessed as percentage of cell viability of two ATRT cell lines, upon treatment with DAPT.
DAPT purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Oct 20;14(1):6669. [Abstract]
Western blot analyses for Notch intracellular domain NICD in CHLA-02 and IC-032 cell lines treated with DAPT (10 µM; 7 days) NOTCH inhibitor or DMSO as a control.
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Acta Pharm Sin B
2024 Jul;14(7):3049-3067. PMID: 39027246 -
Adv Sci (Weinh)
Single-Cell Mitochondrial Lineage Tracing Decodes Fate Decision and Spatial Clonal Architecture in Human Hematopoietic Organoids. [Abstract]2026 Jan 21:e18084. PMID: 41560697 -
Adv Sci (Weinh)
Group 3 Innate Lymphoid Cells Exacerbate Lupus Nephritis by Promoting B Cell Activation in Kidney Ectopic Lymphoid Structures. [Abstract]2023 Dec;10(35):e2302804. PMID: 37915129 -
Adv Sci (Weinh)
Near-Infrared-Responded High Sensitivity Nanoprobe for Steady and Visualized Detection of Albumin in Hepatic Organoids and Mouse Liver. [Abstract]2022 Sep;9(26):e2202505. PMID: 35853243 -
J Clin Invest
2018 Jan 2;128(1):483-499. PMID: 29227285 -
Neuro Oncol
FAM129A promotes self-renewal and maintains invasive status via stabilizing the Notch intracellular domain in glioma stem cells. [Abstract]2023 Oct 3;25(10):1788-1801. PMID: 37083136 -
Theranostics
Fibroblast-specific activation of Rnd3 protects against cardiac remodeling in diabetic cardiomyopathy via suppression of Notch and TGF-β signaling. [Abstract]2022 Oct 17;12(17):7250-7266. PMID: 36438502 -
Theranostics
Lipin 1 deficiency causes adult-onset myasthenia with motor neuron dysfunction in humans and neuromuscular junction defects in zebrafish. [Abstract]2021 Jan 1;11(6):2788-2805. PMID: 33456573 -
Theranostics
Sulforaphane Inhibits the Acquisition of Tobacco Smoke-Induced Lung Cancer Stem Cell-Like Properties via the IL-6/ΔNp63α/Notch Axis. [Abstract]2019 Jul 9;9(16):4827-4840. PMID: 31367260 -
J Adv Res
An injectable nano-hydroxyapatite-incorporated hydrogel with sustained release of Notoginsenoside R1 enhances bone regeneration by promoting angiogenesis through Notch1/Akt signaling. [Abstract]2025 May 13:S2090-1232(25)00343-1. PMID: 40373960 -
J Nanobiotechnology
Matrix micro/nano-topography drives oncogenic signaling and drug response in a 3D osteosarcoma model. [Abstract]2026 Mar 6;24(1):345. PMID: 41787498 -
Sci Adv
Primary human intestinal organoids model enteric infection of monkeypox virus and enable scalable drug discovery. [Abstract]2026 Mar 27;12(13):eaea8280. PMID: 41894500 -
Sci Adv
12R-HETE acts as an endogenous ligand for Nur77 in the intestines and regulates NKp46+ ILC3 development. [Abstract]2026 Feb 20;12(8):eadz8405. PMID: 41719391 -
Sci Adv
Drosophila and mouse intestinal stem cells are spatiotemporally specified by Notch suppression and Wnt activation. [Abstract]2025 Dec 5;11(49):eady7272. PMID: 41337595 -
Sci Adv
Robust reprogramming of glia into neurons by inhibition of Notch signaling and nuclear factor I (NFI) factors in adult mammalian retina. [Abstract]2024 Jul 12;10(28):eadn2091. PMID: 38996013 -
Sci Adv
Chemical conversion of human epidermal stem cells into intestinal goblet cells for modeling mucus-microbe interaction and therapy. [Abstract]2021 Apr 14;7(16):eabb2213. PMID: 33853767 -
J Biomed Sci
Krüppel-like factor 10 modulates stem cell phenotypes of pancreatic adenocarcinoma by transcriptionally regulating notch receptors. [Abstract]2023 Jun 12;30(1):39. PMID: 37308977 -
Brain
BTK inhibition suppresses neuroinflammation and neurodegeneration in amyotrophic lateral sclerosis. [Abstract]2026 Feb 19:awag070. PMID: 41710977 -
J Hazard Mater
Environmental UV filters threaten human neurodevelopment: Disruption of central and peripheral nervous system lineage commitment via WNT signaling dysregulation. [Abstract]2025 Oct 17:499:140149. PMID: 41110322 -
J Allergy Clin Immunol
Pharmacologic inhibition of Notch signaling suppresses food antigen-induced mucosal mast cell hyperplasia. [Abstract]2017 Mar;139(3):987-996.e10. PMID: 27555456 -
MedComm (2020)
Nitrate Enhances Gastric Mucosa Defense and Repair Process in Ethanol-Induced Gastric Ulcer Rats via the Notch-Tff2 Pathway. [Abstract]2026 Feb 5;7(2):e70628. PMID: 41660303 -
Cell Death Dis
Vascular endothelial growth factor 165 inhibits pro-fibrotic differentiation of stromal cells via the DLL4/Notch4/smad7 pathway. [Abstract]2019 Sep 12;10(9):681. PMID: 31515487 -
Genes Dis
2020 Nov 21;8(6):867-881. PMID: 34522714 -
Proc Natl Acad Sci U S A
2017 May 30;114(22):E4425-E4434. PMID: 28507130 -
Cell Commun Signal
The aggressive colorectal cancer subtype marker HTR2B has a dual role depending on the tumor microenvironment. [Abstract]2025 Oct 1;23(1):403. PMID: 41034989 -
Dev Cell
Conserved signals control self-organization and symmetry breaking of murine bilayered epithelia during development and regeneration. [Abstract]2025 Jun 25:S1534-5807(25)00362-4. PMID: 40592344 -
Int J Biol Macromol
Regulation of shelterin proteins TERF2IP and TRF2 by the MLL2-H3K4me3-p65 axis drives hyperglycemia-dependent endothelial senescence. [Abstract]2025 Jun 4;318(Pt 1):144963. PMID: 40480577 -
Acta Pharmacol Sin
DLK1 promoted ischemic angiogenesis through notch1 signaling in endothelial progenitor cells. [Abstract]2024 Dec;45(12):2553-2566. PMID: 39060522 -
Phytomedicine
TKF, a mexicanolide-type limonoid derivative, suppressed hepatic stellate cells activation and liver fibrosis through inhibition of the YAP/Notch3 pathway. [Abstract]2022 Dec:107:154466. PMID: 36182796 -
Phytomedicine
Hibiscus syriacus L. cultivated in callus culture exerts cytotoxicity in colorectal cancer via Notch signaling-mediated cholesterol biosynthesis suppression. [Abstract]2022 Jan:95:153870. PMID: 34896899 -
Phytomedicine
Epiberberine ameliorated diabetic nephropathy by inactivating the angiotensinogen (Agt) to repress TGFβ/Smad2 pathway. [Abstract]2021 Mar:83:153488. PMID: 33571918 -
Free Radic Biol Med
The new pattern for dual NOTCH pathway involving nuclear transcription and mitochondrial regulation supports therapeutic mechanism of 4-butyl benzophenone derivatives against SIRS. [Abstract]2024 Aug 10:S0891-5849(24)00582-3. PMID: 39134162 -
Sci Total Environ
Endosulfan triggers epithelial-mesenchymal transition via PTP4A3-mediated TGF-β signaling pathway in prostate cancer cells. [Abstract]2020 Aug 20;731:139234. PMID: 32413665 -
Biomed Pharmacother
Drug target proteome profiling identifies HES1-driven mitotic catastrophe in ovarian serous carcinoma. [Abstract]2025 Nov 6:193:118716. PMID: 41202420 -
Biomed Pharmacother
FLI-06 suppresses proliferation, induces apoptosis and cell cycle arrest by targeting LSD1 and Notch pathway in esophageal squamous cell carcinoma cells. [Abstract]2018 Nov:107:1370-1376. PMID: 30257352
DAPT purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Nov:107:1370-1376. [Abstract]
ECa109 and EC9706 cells are treated with concentrations of GSI-DAPT (0, 10 and 20 μM) for 48 h. The expressions of Notch3, DTX1 and Hes1 are investigated by Western blotting.
DAPT purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Nov:107:1370-1376. [Abstract]
ECa109 and EC9706 cells are treated with concentrations of GSI-DAPT (0, 10 and 20 μM) for 48 h. The expressions of LSD1 and H3K4me2 are investigated by Western blotting.
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Stem Cell Res Ther
In vitro derivation of midbrain dopaminergic neurons from porcine embryonic stem cells in multi-dimensional conditions. [Abstract]2025 Nov 5;16(1):617. PMID: 41194288 -
Environ Pollut
Neburon induced cardiotoxicity in embryonic and adult male zebrafish via over-activation of the Ahr-Notch1 signaling pathway. [Abstract]2025 Jun 16:126684. PMID: 40532808 -
Stem Cell Res Ther
Transcriptomic and proteomic sequencing unveils the role of vitamin D and metabolic flux shifts in the induction of human hepatic organoids. [Abstract]2024 Dec 18;15(1):478. PMID: 39696644 -
Aging Dis
Salsalate Prevents β-Cell Dedifferentiation in OLETF Rats with Type 2 Diabetes through Notch1 Pathway. [Abstract]2019 Aug 1;10(4):719-730. PMID: 31440379 -
Neural Regen Res
Neuroprotective effect of Notch pathway inhibitor DAPT against focal cerebral ischemia/reperfusion 3 hours before model establishment. [Abstract]2019 Mar;14(3):452-461. PMID: 30539813
DAPT purchased from MedChemExpress. Usage Cited in: Neural Regen Res. 2019 Mar;14(3):452-461. [Abstract]
Western blot assay for Hes1 (left) and Hes5 (right) protein expression in the right prefrontal cortex of cerebral I/R mice following DAPT treatment.
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J Agric Food Chem
HDAC11 Regulates the Proliferation of Bovine Muscle Stem Cells through the Notch Signaling Pathway and Inhibits Muscle Regeneration. [Abstract]2022 Jul 27;70(29):9166-9178. PMID: 35837734 -
J Agric Food Chem
Lycopene Alleviates Chronic Stress-Induced Spleen Apoptosis and Immunosuppression via Inhibiting the Notch Signaling Pathway in Rats. [Abstract]2022 Mar 9;70(9):2889-2897. PMID: 35212537 -
Ecotoxicol Environ Saf
The role of estrogen receptors (ERs)-Notch pathway in thyroid toxicity induced by Di-2-ethylhexyl phthalate (DEHP) exposure: Population data and in vitro studies. [Abstract]2024 Jan 1:269:115727. PMID: 38042133 -
JCI Insight
Increased CHCHD2 expression promotes liver fibrosis in nonalcoholic steatohepatitis via Notch/osteopontin signaling. [Abstract]2022 Dec 8;7(23):e162402. PMID: 36477358 -
Ecotoxicol Environ Saf
Analysis of the roles of the Notch1 signalling pathway in modulating deoxynivalenol cytotoxicity. [Abstract]2022 Nov:246:114183. PMID: 36270035
DAPT purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2022 Nov:246:114183. [Abstract]
DAPT treatment enhances the protein expression of Bax and decreases the expression of Bcl2. And the expression of cleaved-caspase3 is upregulated after DAPT treatment (10 μM; for 24 h).
DAPT purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2022 Nov:246:114183. [Abstract]
Detection of cell viability after treatment with different concentrations of DAPT (5 μM, 10 μM, 15 μM, 20 μM; for 24 h).
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J Mol Cell Biol
β-catenin activation in hair follicle dermal stem cells induces ectopic hair outgrowth and skin fibrosis. [Abstract]2019 Jan 1;11(1):26-38. PMID: 29771334 -
J Invest Dermatol
Identification of Small-Molecule Inhibitors Targeting Different Signaling Pathways in Cancer-Associated Fibroblast Reprogramming Under Tumor-Stroma Interaction. [Abstract]2024 Jun 5:S0022-202X(24)00392-0. PMID: 38848988 -
Breast Cancer Res
NOTCH1 inhibition enhances immunogenicity and sensitizes triple-negative breast cancer to immune checkpoint inhibitors. [Abstract]2025 May 26;27(1):92. PMID: 40420289 -
Int J Mol Sci
Pin1 Downregulation Is Involved in Excess Retinoic Acid-Induced Failure of Neural Tube Closure. [Abstract]2024 May 21;25(11):5588. PMID: 38891776 -
Cell Prolif
GIT1 regulates angiogenic factor secretion in bone marrow mesenchymal stem cells via NF-κB/Notch signalling to promote angiogenesis. [Abstract]2019 Nov;52(6):e12689. PMID: 31502302 -
Inflamm Res
Activation of the Notch signaling pathway disturbs the CD4+/CD8+, Th17/Treg balance in rats with experimental autoimmune uveitis. [Abstract]2019 Sep;68(9):761-774. PMID: 31209505 -
World J Gastroenterol
Notch signaling mediated by TGF-β/Smad pathway in concanavalin A-induced liver fibrosis in rats. [Abstract]2017 Apr 7;23(13):2330-2336. PMID: 28428712
DAPT purchased from MedChemExpress. Usage Cited in: World J Gastroenterol. 2017 Apr 7;23(13):2330-2336. [Abstract]
Notch γ-secretase inhibitor attenuates notch and transforming growth factor-β signaling pathways in peripheral blood mononuclear cells of liver fibrosis rats. Western blot analysis of protein expression of Notch1, Hes1, Hes5, TGF-β and Smad3 and quantification in PBMCs (2 × 106) from rats treated with DAPT or DMSO for 24 h.
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Cells
Compensatory Intercellular Mitochondrial Transfer Improves Bioenergetics in P301L Tau-Affected Neuronal Cells. [Abstract]2026 Jun 17;15(12):1101. PMID: 42346128 -
Cells
LFA-1/ICAM-1 Interactions Between CD8+ and CD4+ T Cells Promote CD4+ Th1-Dominant Differentiation and CD8+ T Cell Cytotoxicity for Strong Antitumor Immunity After Cryo-Thermal Therapy. [Abstract]2025 Apr 21;14(8):620. PMID: 40277945 -
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Life Sci
Ferulic acid, ligustrazine, and tetrahydropalmatine display the anti-proliferative effect in endometriosis through regulating Notch pathway. [Abstract]2023 Sep 1:328:121921. PMID: 37429417 -
Drug Des Devel Ther
Notch inhibitor can attenuate apparent diffusion coefficient and improve neurological function through downregulating NOX2-ROS in severe traumatic brain injury. [Abstract]2018 Nov 8:12:3847-3854. PMID: 30510400
DAPT purchased from MedChemExpress. Usage Cited in: Drug Des Devel Ther. 2018 Nov 8:12:3847-3854. [Abstract]
Western anslysis of protein analysis of NOX2, NICD, Hes1, Hes5 in the treatment of TBI, TBI+vehicle, TBI+DAPT and TBI+DPI, respectively.
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Immunology
Notch1 signalling controls the differentiation and function of myeloid-derived suppressor cells in systemic lupus erythematosus. [Abstract]2022 Aug 29. PMID: 36038992 -
Inflammation
Protein Kinase C Theta Inhibition Attenuates Lipopolysaccharide-Induced Acute Lung Injury through Notch Signaling Pathway via Suppressing Th17 Cell Response in Mice. [Abstract]2019 Dec;42(6):1980-1989. PMID: 31297750 -
Stem Cells Transl Med
Sstr2 Defines the Cone Differentiation-Competent Late-Stage Retinal Progenitor Cells in the Developing Mouse Retina. [Abstract]2024 Jan 12;13(1):83-99. PMID: 37935630 -
Int J Mol Sci
Notch-RBPJ Pathway for the Differentiation of Bone Marrow Mesenchymal Stem Cells in Femoral Head Necrosis. [Abstract]2023 Mar 27;24(7):6295. PMID: 37047268 -
Biomolecules
Notch Signaling Exacerbates Pulmonary Fibrosis by Regulating the Differentiation of CD4+ Tissue-Resident Memory T Cells. [Abstract]2026 Feb 20;16(2):328. PMID: 41750395 -
Bioorg Chem
Usenamine A, an RGS2 inhibitor, exerts anti-NSCLC activity and enhances cytotoxicity of gemcitabine by inducing ER stress and Notch1-mediated autophagy. [Abstract]2025 Sep 17:165:109010. PMID: 40974657 -
Invest Ophthalmol Vis Sci
SLC6A6-Mediated Taurine Uptake Sustains Corneal Epithelial Stem/Progenitor Cell Function to Counteract Age-Related Dysfunction. [Abstract]2025 Jun 2;66(6):25. PMID: 40478558 -
Int Immunopharmacol
2023 Mar:116:109832. PMID: 36764280 -
Eur J Pharmacol
Notch signaling activation contributes to paclitaxel-induced neuropathic pain via activation of A1 astrocytes. [Abstract]2022 Aug 5:928:175130. PMID: 35777441 -
Int Immunopharmacol
DAPT reverses the Th17/Treg imbalance in experimental autoimmune uveitis in vitro via inhibiting Notch signaling pathway. [Abstract]2020 Feb;79:106107. PMID: 31863921 -
Int J Cancer
Pharmacological inhibition of the Notch pathway enhances the efficacy of androgen deprivation therapy for prostate cancer. [Abstract]2018 Aug 1;143(3):645-656. PMID: 29488214
DAPT purchased from MedChemExpress. Usage Cited in: Int J Cancer. 2018 Aug 1;143(3):645-656. [Abstract]
Evaluation of expression change of Notch downstream under the androgen-deprived condition with or without the treatment of DAPT by western blot assay.
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Toxicology
Effects of miR-200b-3p and miR-424-5p regulating notch signaling pathway on atherosclerosis induced by PM2.5in vitro. [Abstract]2025 Jun 17:154216. PMID: 40553880 -
Cancer Sci
NOTCH3 promotes docetaxel resistance of prostate cancer cells through regulating TUBB3 and MAPK signaling pathway. [Abstract]2024 Feb;115(2):412-426. PMID: 38115797 -
Front Cell Dev Biol
LncRNA Xist Contributes to Endogenous Neurological Repair After Chronic Compressive Spinal Cord Injury by Promoting Angiogenesis Through the miR-32-5p/Notch-1 Axis. [Abstract]2020 Aug 6;8:744. PMID: 32850853 -
FASEB J
Mechanosensitive Ca2+ channel TRPV1 activated by low-intensity pulsed ultrasound ameliorates acute kidney injury through Notch1-Akt-eNOS signaling. [Abstract]2025 Jan 15;39(1):e70304. PMID: 39785696 -
Biochim Biophys Acta Mol Basis Dis
The Annexin A2-Notch regulatory loop in hepatocytes promotes liver fibrosis in NAFLD by increasing osteopontin expression. [Abstract]2022 Aug 1;1868(8):166413. PMID: 35413401 -
Mediators Inflamm
Notch1 Signaling Contributes to Mechanical Allodynia Associated with Cyclophosphamide-Induced Cystitis by Promoting Microglia Activation and Neuroinflammation. [Abstract]2021 Oct 4:2021:1791222. PMID: 34646085 -
J Inflamm Res
The Pomegranate Peel Polyphenols Protects Acne Vulgaris by Regulating Inflammation Through Notch/NF-κB Signal Pathway. [Abstract]2025 Oct 10:18:14113-14129. PMID: 41098683 -
iScience
2025 Apr 3;28(5):112344. PMID: 40276762 -
iScience
Casein kinase 1α is required to maintain murine hypothalamic pro-opiomelanocortin expression. [Abstract]2023 Apr 14;26(5):106670. PMID: 37168577 -
Toxicol Sci
2019 Sep 1;171(1):1-12. PMID: 31241159 -
Oncol Res
Heme Oxygenase-1 Inhibits Tumor Metastasis Mediated by Notch1 Pathway in Murine Mammary Carcinoma. [Abstract]2019 Jun 21;27(6):643-651. PMID: 30764900 -
iScience
2019 Sep 27;19:1248-1259. PMID: 31353167 -
Neurochem Int
Kaempferol promotes angiogenesis through HIF-1α/VEGF-A/Notch1 pathway in ischemic stroke rats. [Abstract]2025 May:185:105953. PMID: 39988285 -
J Neurochem
2023 Aug;166(4):747-762. PMID: 37422446 -
Toxins
2021 Aug 22;13(8):585. PMID: 34437455 -
J Cell Physiol
Triptolide prevents extracellular matrix accumulation in experimental diabetic kidney disease by targeting microRNA-137/Notch1 pathway. [Abstract]2018 Mar;233(3):2225-2237. PMID: 28695984
DAPT purchased from MedChemExpress. Usage Cited in: J Cell Physiol. 2018 Mar;233(3):2225-2237. [Abstract]
DAPTprevents Nicd splitting from Notch1 and has been recognized as a Notch1 pathway inhibitor. Treatment with DAPT also inhibits the expression of Col IV and FN, resembling the effect of Notch1 siRNA.
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J Biol Chem
Andrographolide targets syndecan4 to impair its interaction with syntenin and inhibits the biogenesis of small extracellular vesicles. [Abstract]2026 Jan 20:111182. PMID: 41570990 -
Sci Rep
2025 Dec 18. PMID: 41413272 -
Biomedicines
Immunomodulatory Potential of a Composite Amniotic Membrane Hydrogel for Wound Healing: Effects on Macrophage Cytokine Secretion. [Abstract]2025 Oct 21;13(10):2574. PMID: 41153852 -
Sci Rep
Sciellin inhibits senescence and promotes pancreatic cancer progress by activating the notch signaling pathway. [Abstract]2025 May 8;15(1):16133. PMID: 40341648 -
Sci Rep
The neuroepithelial origin of ovarian carcinomas explained through an epithelial-mesenchymal-ectodermal transition enhanced by cisplatin. [Abstract]2024 Nov 26;14(1):29286. PMID: 39592661 -
Biomedicines
Generation of a Pure Culture of Neuron-like Cells with a Glutamatergic Phenotype from Mouse Astrocytes. [Abstract]2022 Apr 18;10(4):928. PMID: 35453678 -
J Biol Chem
MGST3 regulates BACE1 protein translation and amyloidogenesis by controlling the RGS4-mediated AKT signaling pathway. [Abstract]2024 Jul 4:107530. PMID: 38971310 -
Oncol Rep
miR‑1299/NOTCH3/TUG1 feedback loop contributes to the malignant proliferation of ovarian cancer. [Abstract]2020 Aug;44(2):438-448. PMID: 32468036 -
ACS Chem Neurosci
2018 Dec 19;9(12):3175-3185. PMID: 30091580 -
Front Med
ASPH interacts with RUVBL2 to promote tumor metastasis in lung adenocarcinoma via MAPK and Notch signaling pathways. [Abstract]2025 Dec 27. PMID: 41454078 -
Food Chem Toxicol
Activation of Notch Signaling Pathway is involved in Extracellular Matrix Degradation in human induced pluripotent stem cells chondrocytes induced by HT-2 toxin. [Abstract]2024 May 9:114724. PMID: 38734200 -
Front Med
Amnion-Derived Mesenchymal Stromal/Stem Cell Paracrine Signals Potentiate Human Liver Organoid Differentiation: Translational Implications for Liver Regeneration. [Abstract]2021 Sep 23;8:746298. PMID: 34631757 -
Exp Cell Res
GRWD1 promotes cell proliferation and migration in non-small cell lung cancer by activating the Notch pathway. [Abstract]2020 Feb 15;387(2):111806. PMID: 31891681 -
Microb Pathogenesis
Tangeretin attenuates lipopolysaccharide-induced acute lung injury through Notch signaling pathway via suppressing Th17 cell response in mice. [Abstract]2020 Jan;138:103826. PMID: 31676364 -
Mol Med Rep
miR‑125b‑mediated regulation of cell proliferation through the Jagged‑1/Notch signaling pathway by inhibiting BRD4 expression in psoriasis. [Abstract]2019 Jun;19(6):5227-5236. PMID: 31059052 -
Eur J Med Res
Targeting ANGPTL4 improves Treg/Th17 cell imbalance and alleviates inflammation in allergic rhinitis by suppressing the Notch signaling pathway. [Abstract]2025 Sep 23;30(1):851. PMID: 40988062 -
Andrology
2022 Nov;10(8):1644-1659. PMID: 36057850 -
Stem Cells Int
Inhibition of Notch Signaling Promotes the Differentiation of Epicardial Progenitor Cells into Adipocytes. [Abstract]2021 Apr 9:2021:8859071. PMID: 33897781 -
J Cancer
SIX1 Predicts Poor Prognosis and Facilitates the Progression of Non-small Lung Cancer via Activating the Notch Signaling Pathway. [Abstract]2022 Jan 1;13(2):527-540. PMID: 35069900 -
Front Neurosci
Pathophysiological Changes and the Role of Notch-1 Activation After Decompression in a Compressive Spinal Cord Injury Rat Model. [Abstract]2021 Jan 28:15:579431. PMID: 33584186 -
Kaohsiung J Med Sci
FOXA1 activates NOLC1 transcription through NOTCH pathway to promote cell stemness in lung adenocarcinoma. [Abstract]2025 Jan 10:e12930. PMID: 39789998 -
Oral Dis
Phenotype transition of fibroblasts incorporated into patient-derived oral carcinoma organoids. [Abstract]2023 Apr;29(3):913-922. PMID: 34741375 -
J Biochem Mol Toxicol
Estrogen Promotes the Proliferation and Migration of Endometrial Cancer Through the GPER-Mediated NOTCH Pathway. [Abstract]2025 Feb;39(2):e70129. PMID: 39878097 -
Neuroscience
DJ-1 Protein Inhibits Apoptosis in Cerebral Ischemia by Regulating the Notch1 and Nuclear Factor Erythroid2-Related Factor 2 Signaling Pathways. [Abstract]2022 Nov 10:504:33-46. PMID: 36167256 -
J Orthop Surg Res
Total glycosides from Eucommia ulmoides seed promoted osteogenic differentiation of adipose-derived mesenchymal stem cells and bone formation in ovariectomized rats through regulating Notch signaling pathway. [Abstract]2021 Nov 6;16(1):660. PMID: 34742334 -
J Cell Biochem
Gamma-secretase inhibitor suppressed Notch1 intracellular domain combination with p65 and resulted in the inhibition of the NF-κB signaling pathway induced by IL-1β and TNF-α in nucleus pulposus cells. [Abstract]2019 Feb;120(2):1903-1915. PMID: 30367520
DAPT purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2019 Feb;120(2):1903-1915. [Abstract]
The distribution of aggrecan is increased in the DAPT group.
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Animals (Basel)
NOTCH1 as a Negative Regulator of Avian Adipocyte Differentiation: Implications for Fat Deposition. [Abstract]2024 Feb 9;14(4):585. PMID: 38396553 -
DNA Repair
Presenilin-1, mutated in familial Alzheimer's disease, maintains genome stability via a γ-secretase dependent way. [Abstract]2023 Nov:131:103580. PMID: 37804602 -
PLoS One
2018 Feb 15;13(2):e0193037. PMID: 29447233
DAPT purchased from MedChemExpress. Usage Cited in: PLoS One. 2018 Feb 15;13(2):e0193037. [Abstract]
After DAPT treatment, the protein levels of Notch, Hes1 and Hes5 are downregulated in severe injury group. After DAPT treatment, the protein levels of Bcl-2 are upregulated while those of Bax, caspase-3 and caspase-9 are downregulated.
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Traffic
AP2S1 regulates APP degradation through late endosome-lysosome fusion in cells and APP/PS1 mice. [Abstract]2023 Jan;24(1):20-33. PMID: 36412210 -
Toxicon
Deoxynivalenol-induced anorexia is mediated by brain-gut peptides through CaSR-TRPM5 signaling axis. [Abstract]2026 Jan:269:108660. PMID: 41241198 -
Virology
Decoding the role of the intestinal epithelium in hepatitis E virus infection using a human organoid prototype of "gut-liver" axis. [Abstract]2025 Jun 27:610:110615. PMID: 40596796 -
Biochem Biophys Res Commun
Inhibition of Notch1 signaling reduces hepatocyte injury in nonalcoholic fatty liver disease via autophagy. [Abstract]2021 Apr 2:547:131-138. PMID: 33610041 -
Int Arch Allergy Immunol
B Lymphocytes Balance Th1/Th2 to Participate in Fibrotic Hypersensitivity Pneumonia Induced by Pigeon Shedding. [Abstract]2023;184(2):122-131. PMID: 36323228 -
Biol Open
Biophysical and biochemical properties of Deup1 self-assemblies: a potential driver for deuterosome formation during multiciliogenesis. [Abstract]2021 Mar 3;10(3):bio056432. PMID: 33658185 -
J Matern Fetal Neonatal Med
Periostin promotes extensive neovascularization in placenta accreta spectrum disorders via Notch signaling. [Abstract]2023 Dec;36(2):2264447. PMID: 37806775 -
Am J Transl Res
The protective role of the miR-25-mediated notch signaling pathway in the memory capacity and brain tissue of mice with central nervous system infections. [Abstract]2021 May 15;13(5):4835-4843. PMID: 34150065 -
Neurol Res
Rosuvastatin improves neurite extension in cortical neurons through the Notch 1/BDNF pathway. [Abstract]2019 Jul;41(7):658-664. PMID: 31023175 -
J Vis Exp
Two-dimensional Porcine Intestinal Organoids Reflecting the Physiological Properties of Native Gut. [Abstract]2025 Jan 31:(215). PMID: 39960208 -
bioRxiv
ProNotch converts extracellular protease activity into programmable transcriptional outputs. [Abstract]2026 Jun 3:2026.06.01.728985. PMID: 42282718 -
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bioRxiv
Graded Notch Signaling Functions as a Rheostat of Lineage Plasticity and Therapy Resistance in Prostate Cancer. [Abstract]2025 Nov 26:2025.11.23.690056. PMID: 41394651 -
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bioRxiv
Spatial 3D genome organization controls the activity of bivalent chromatin during human neurogenesis. [Abstract]2024 Aug 1:2024.08.01.606248. PMID: 39131314 -
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bioRxiv
Robust reprogramming of glia into neurons by inhibition of Notch signaling and NFI factors in adult mammalian retina. [Abstract]2023 Nov 5:2023.10.29.560483. PMID: 37961663 -
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Methods Mol Biol
Human Pluripotent Stem Cells for High-Throughput Drug Screening and Characterization of Small Molecules. [Abstract]2022:2454:811-827. PMID: 34128205 -
DAPT purchased from MedChemExpress. Usage Cited in: Yale University. 2016 Jan.
Treatment with DAPT does not markedly alter expression of p27Kip1 in bulk or CD133- cells, but dramatically enhances its expression in CD133+ cells.
Solvent & Solubility
DMSO : 62.5 mg/mL (144.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 10 mg/mL (23.12 mM; Need ultrasonic)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.78 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 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.78 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 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.
Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (2.31 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (10.0 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: Corn Oil
Solubility: 10 mg/mL (23.12 mM); Suspended solution; Need ultrasonic
Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 20 mg/mL (46.25 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
-
+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
Human embryonic kidney cells, 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. Cells are pre-treated for 2 h at 37°C with DAPT (0, 0.4, 2, 10, 50 and 250 nM), media are aspirated off and fresh compound solutions applied. After an additional 2-h treatment period, conditioned media are 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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
The three- to four-month-old heterozygous PDAPP transgenic mice overexpressing the APPV717F mutant form of the amyloid precursor protein. Each treatment group (n=10) consists of equal numbers of age-matched male and female animals that are fasted overnight prior to treatment. Both treatment and control groups are dosed at a volume of 10 mL/kg with DAPT or vehicle alone. Tissues are processed and all Aβ and APP measurements are made. After removal of the brain, the cortex from one hemisphere is homogenized, centrifuged, and the supernatant is used for Aβ measurements. Cortex from the other hemisphere is snap frozen for analysis of compound levels. Aβ levels are expressed as ng/g of wet tissue weight, and percentage reductions are calculated relative to the mean Aβ level of tissue from vehicle-treated control animals. Data are analyzed with Mann-Whitney non-parametric statistics to assess significance.
Rats[3]
Male Sprague-Dawley rats (260-290 g) are used. DAPT solution is stereotactically injected into the lateral cerebral ventricle (LV) immediately after MCAO. The stereotactic injections into the LVs are performed at coordinates −0.8 mm anteroposterior, ±1.5 mm mediolateral and −4.5 mm dorsoventral from the bregma. 30 rats are randomly assigned to three operating groups (10 rats in each group): sham-operated group that receive equal volume of PBS without MCAO operation; MCAO group that receive equal volume PBS after MCAO (MCAO); and DAPT group that receive DAPT as 0.03 mg/kg after MCAO. 24 h after operation the first neurological function is assessed and then 48 h after operation the second neurological function is assessed. Meanwhile, brain water content and infarction volume are measured and compared among different groups.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Dovey HF, et al. Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain. J Neurochem. 2001 Jan;76(1):173-81. [Content Brief]
[2]. Li S, et al. DAPT protects brain against cerebral ischemia by down-regulating the expression of Notch 1 and nuclear factor κB in rats. Neurol Sci. 2012 Dec;33(6):1257-64. [Content Brief]
[3]. Zhou JX, et al. γ-secretase inhibition combined with NSC 119875 enhances apoptosis of nasopharyngeal carcinoma cells.Exp Ther Med. 2012 Feb;3(2):357-361. [Content Brief]
[4]. Tanimizu N, et al. Intrahepatic bile ducts are developed through formation of homogeneous continuous luminal network and its dynamic rearrangement in mice. Hepatology. 2016 Jul;64(1):175-88. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 2.3124 mL | 11.5618 mL | 23.1235 mL | 57.8088 mL |
| 5 mM | 0.4625 mL | 2.3124 mL | 4.6247 mL | 11.5618 mL | |
| 10 mM | 0.2312 mL | 1.1562 mL | 2.3124 mL | 5.7809 mL | |
| 15 mM | 0.1542 mL | 0.7708 mL | 1.5416 mL | 3.8539 mL | |
| 20 mM | 0.1156 mL | 0.5781 mL | 1.1562 mL | 2.8904 mL | |
| DMSO | 25 mM | 0.0925 mL | 0.4625 mL | 0.9249 mL | 2.3124 mL |
| 30 mM | 0.0771 mL | 0.3854 mL | 0.7708 mL | 1.9270 mL | |
| 40 mM | 0.0578 mL | 0.2890 mL | 0.5781 mL | 1.4452 mL | |
| 50 mM | 0.0462 mL | 0.2312 mL | 0.4625 mL | 1.1562 mL | |
| 60 mM | 0.0385 mL | 0.1927 mL | 0.3854 mL | 0.9635 mL | |
| 80 mM | 0.0289 mL | 0.1445 mL | 0.2890 mL | 0.7226 mL | |
| 100 mM | 0.0231 mL | 0.1156 mL | 0.2312 mL | 0.5781 mL |