D5942 Sigma


≥98% (HPLC), solid

Synonym: GSI-IX, LY-374973, N-[N-(3,5-Difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl ester



Related Categories Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Biochemicals and Reagents, Cell Biology,
assay   ≥98% (HPLC)
form   solid
color   white
solubility   DMSO: ~18 mg/mL
originator   Eli Lilly
storage temp.   2-8°C
Gene Information   human ... APH1A(51107), APH1B(83464), NCSTN(23385), NOTCH1(4851), NOTCH2(4853), NOTCH3(4854), NOTCH4(4855), PSEN1(5663), PSEN2(5664), PSENEN(55851)
mouse ... Aph1a(226548), Aph1b(208117), Ncstn(59287), Notch1(18128), Notch2(18129), Notch3(18131), Notch4(18132), Psen1(19164), Psen2(19165), Psenen(66340)
rat ... Aph1a(365872), Aph1b(300802), Ncstn(289231), Notch1(25496), Notch2(29492), Notch3(56761), Notch4(406162), Psen1(29192), Psen2(81751), Psenen(292788)


Frequently Asked Questions

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25 mg in poly bottle

5 mg in glass bottle

Biochem/physiol Actions

DAPT is a γ-secretase inhibitor and indirectly an inhibitor of Notch, a γ-secretase substrate. Other γ-secretase substrates include LDL receptor-related protein, E-cadherin and ErbB-4. As an inhibitor of γ-secretase, DAPT may be useful in the study of β-amyloid (Aβ) formation. DAPT has been shown to inhibit Notch signaling in studies of autoimmune and lymphoproliferative diseases, such as ALPS and lupus erythematosus (SLE), as well as in cancer cell growth, angiogenesis, and differentiation of human induced pluripotent stem cells (hIPSC).

Features and Benefits

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Safety & Documentation

Safety Information

WGK Germany 


Certificate of Analysis

Certificate of Origin

Protocols & Articles


Discover Bioactive Small Molecules for Neuroscience

The nervous system, comprised of the brain and spinal cord (central nervous system, or CNS) and network of nerves that connects the CNS to the rest of the body (peripheral nervous system, or PNS) is ...
Keywords: Bioactive small molecules, Central Nervous System, Diseases, Metabolism, Neurodegenerative Diseases, Neuroscience, Neurotransmission, Neurotransmitters

The Cancer Stem Cell Hypothesis

Traditionally, cancer has been viewed as a disease in which environmental or endogenous events induce mutations to critical oncogenes and tumor suppressor genes within a normal cell. The clinical man...
Vicki Caligur
BioFiles 2008, 3.5, 4.
Keywords: Angiogenesis, Apoptosis, Asymmetric synthesis, Cancer, Catalysis, Cell culture, Cell division, Cell proliferation, Clinical, DNA replication, Degradations, Eliminations, Environmental, Events, Gastrointestinal, Gene expression, Growth factors, Ligands, Metabolic Pathways, Phosphorylations, Poisons, Transcription, Transfection, transformation

Peer-Reviewed Papers


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In vitro expansion of single Lgr5+ liver stem cells induced by Wnt-driven regeneration. Huch, M., et al. Nature 494, 247-50, (2013)


A helix-to-coil transition at the epsilon-cut site in the transmembrane dimer of the amyloid precursor protein is required for proteolysis. Sato T, et. al. Proc. Natl. Acad. Sci. U. S. A., 1421-6, (2009)


Presenilin-dependent intramembrane proteolysis of CD44 leads to the liberation of its intracellular domain and the secretion of an Abeta-like peptide. Lammich, S., et al. J. Biol. Chem. 277, 44754-44759, (2002)


Requirement for Pdx1 in specification of latent endocrine progenitors in zebrafish. Robin A Kimmel et al BMC Biol. 9, 75, (2011)


Gastric cancer cell growth and epithelial-mesenchymal transition are inhibited by γ-secretase inhibitor DAPT. Li LC, Peng Y, Liu YM, et al. Oncol. Lett. 7(6), 2160-2164, (2014)


γ-Secretase/presenilin inhibitors for Alzheimer's disease phenocopy Notch mutations in Drosophila. Micchelli, C.A., et al. FASEB J. 17, 79-81, (2003)


Targeting Notch1 signaling pathway positively affects the sensitivity of osteosarcoma to cisplatin by regulating the expression and/or activity of Caspase family. Wang L, Jin F, Qin A, et al. Mol. Cancer 13(1), 139, (2014)

Targeting Notch signaling in autoimmune and lymphoproliferative disease Teachey DT, et al. Blood 111, 705-714, (2008)


Functional γ-secretase inhibitors reduce β-amyloid peptide levels in brain. Dovey, H.F., et al. J. Neurochem. 76, 173-181, (2001)


Suppression Of Notch Signaling In The Neonatal Mouse Ovary Decreases Primordial Follicle Formation. Trombly, D.J., et al. Endocrinology 150, 1014-24, (2009)


Notch Signaling Is Involved In Ovarian Follicle Development By Regulating Granulosa Cell Proliferation. Zhang, C.P., et al. Endocrinology 152, 2437-47, (2011)


The Notch signaling inhibitor DAPT down-regulates cdk5 activity and modulates the distribution of neuronal cytoskeletal proteins Kanungo J, et al. J. Neurochem. 106, 2236-2248, (2008)


The COX-2 selective inhibitor-independent COX-2 effect on colon carcinoma cells is associated with the Delta1/Notch1 pathway Zhang H, et al. Dig. Dis. Sci. 53, 2195-2203, (2008)


Inhibition of Notch signaling facilitates the differentiation of human-induced pluripotent stem cells into neural stem cells. Chen CY, Liao W, Lou YL, et al. Mol. Cell Biochem., (2014)


Monomeric C-reactive protein and Notch-3 co-operatively increase angiogenesis through PI3K signalling pathway. Boras E, Slevin M, Alexander MY, et al. Cytokine 69(2), 165-179, (2014)


In vivo notch signaling blockade induces abnormal spermatogenesis in the mouse. Murta D, Batista M, Trindade A, et al. PLoS ONE 9(11), e113365, (2014)


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