EMAIL THIS PAGE TO A FRIEND
D5942 Sigma

DAPT

≥98% (HPLC), solid

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

Purchase

Properties

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)

Description

Frequently Asked Questions

Live Chat and Frequently Asked Questions are available for this Product.

Packaging

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

This compound is a featured product for Neuroscience research. Click here to discover more featured Neuroscience products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

This compound was developed by Eli Lilly. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Price and Availability


DISCOVER Bioactive Small Molecules
Safety & Documentation

Safety Information

WGK Germany 
3

Documents

Certificate of Analysis

Certificate of Origin

Protocols & Articles

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

References

Set your institution to view full text papers.

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

Loading...


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)

Loading...


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)

Loading...


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

Loading...


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)

Loading...


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

Loading...


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)

Loading...


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

Loading...


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

Loading...


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

Loading...


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)

Loading...


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)

Loading...


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)

Loading...


Short- versus long-term dual antiplatelet therapy after drug-eluting stent implantation: an individual patient data pairwise and network meta-analysis. Palmerini T, Sangiorgi D, Valgimigli M, et al. J. Am. Coll. Cardiol. 65(11), 1092-102, (2015)

Loading...


The immunoregulator soluble TACI is released by ADAM10 and reflects B cell activation in autoimmunity. Hoffmann FS, Kuhn PH, Laurent SA, et al. J. Immunol. 194(2), 542-52, (2015)

Loading...


F-box protein FBXW7 inhibits cancer metastasis in a non-cell-autonomous manner. Yumimoto K, Akiyoshi S, Ueo H, et al. J. Clin. Invest. 125(2), 621-35, (2015)

Loading...


New ischemic stroke and outcomes with vorapaxar versus placebo: results from the TRA 2 °P-TIMI 50 trial. Bonaca MP, Scirica BM, Braunwald E, et al. J. Am. Coll. Cardiol. 64(22), 2318-26, (2014)

Loading...


iPSC-derived neurons from GBA1-associated Parkinson's disease patients show autophagic defects and impaired calcium homeostasis. Schöndorf DC, Aureli M, McAllister FE, et al. Nat. Commun. 5, 4028, (2014)

Loading...


KSHV viral cyclin interferes with T-cell development and induces lymphoma through Cdk6 and Notch activation in vivo. Pekkonen P, Järviluoma A, Zinovkina N, et al. Cell Cycle 13(23), 3670-84, (2015)

Loading...


Notch and NF-kB signaling pathways regulate miR-223/FBXW7 axis in T cell acute lymphoblastic leukemia. Kumar V, Palermo R, Talora C, et al. Leukemia, doi:10.1038/leu.2014.133, (2014)

Loading...


Prasugrel plus aspirin beyond 12 months is associated with improved outcomes after TAXUS Liberté paclitaxel-eluting coronary stent placement. Garratt KN, Weaver WD, Jenkins RG, et al. Circulation 131(1), 62-73, (2015)

Loading...


Notch inhibition induces mitotically generated hair cells in mammalian cochleae via activating the Wnt pathway. Li W, Wu J, Yang J, et al. Proc. Natl. Acad. Sci. U. S. A. 112(1), 166-71, (2015)

Loading...


Loss of the Notch effector RBPJ promotes tumorigenesis. Kulic I, Robertson G, Chang L, et al. J. Exp. Med. 212(1), 37-52, (2015)

Loading...


Coronary stent thrombosis with vorapaxar versus placebo: results from the TRA 2° P-TIMI 50 trial. Bonaca MP, Scirica BM, Braunwald E, et al. J. Am. Coll. Cardiol. 64(22), 2309-17, (2014)

Loading...


A randomized comparison of novel biodegradable polymer- and durable polymer-coated cobalt-chromium sirolimus-eluting stents. Han Y, Xu B, Jing Q, et al. JACC Cardiovasc. Interv. 7(12), 1352-60, (2014)

Loading...


Notch2 controls prolactin and insulin-like growth factor binding protein-1 expression in decidualizing human stromal cells of early pregnancy. Otti GR, Saleh L, Velicky P, et al. PLoS ONE 9(11), e112723, (2014)

Loading...


ID4 controls mammary stem cells and marks breast cancers with a stem cell-like phenotype. Junankar S, Baker LA, Roden DL, et al. Nat. Commun. 6, 6548, (2015)

Loading...


Duration of dual antiplatelet therapy after drug-eluting stent implantation: a systematic review and meta-analysis of randomized controlled trials. Giustino G, Baber U, Sartori S, et al. J. Am. Coll. Cardiol. 65(13), 1298-310, (2015)

Loading...


Differentiation of hypothalamic-like neurons from human pluripotent stem cells. Wang L, Meece K, Williams DJ, et al. J. Clin. Invest. 125(2), 796-808, (2015)

Loading...


Bmi1 regulates murine intestinal stem cell proliferation and self-renewal downstream of Notch. López-Arribillaga E, Rodilla V, Pellegrinet L, et al. Development 142(1), 41-50, (2014)

Loading...


Identification of Cdca7 as a novel Notch transcriptional target involved in hematopoietic stem cell emergence. Guiu J, Bergen DJ, De Pater E, et al. J. Exp. Med. 211(12), 2411-23, (2014)

Loading...


Crucial role of the Rap G protein signal in Notch activation and leukemogenicity of T-cell acute lymphoblastic leukemia. Doi K, Imai T, Kressler C, et al. Sci. Rep. 5, 7978, (2015)

Loading...


Notch3-Jagged signaling controls the pool of undifferentiated airway progenitors. Mori M, Mahoney JE, Stupnikov MR, et al. Development 142(2), 258-67, (2015)

Loading...


Comparison of the gene expression profiles of human fetal cortical astrocytes with pluripotent stem cell derived neural stem cells identifies human astrocyte markers and signaling pathways and transcription factors active in human astrocytes. Malik N, Wang X, Shah S, et al. PLoS ONE 9(5), e96139, (2014)

Loading...


Submersion and hypoxia inhibit ciliated cell differentiation in a notch-dependent manner. Gerovac BJ, Valencia M, Baumlin N, et al. Am. J. Respir. Cell. Mol. Biol. 51(4), 516-25, (2014)

Loading...


VEGFR3 does not sustain retinal angiogenesis without VEGFR2. Zarkada G, Heinolainen K, Makinen T, et al. Proc. Natl. Acad. Sci. U. S. A. 112(3), 761-6, (2015)

Loading...


Decidualization induces a secretome switch in perivascular niche cells of the human endometrium. Murakami K, Lee YH, Lucas ES, et al. Endocrinology 155(11), 4542-53, (2014)

Loading...


The complex interplay between ERK1/2, TGF?/Smad, and Jagged/Notch signaling pathways in the regulation of epithelial-mesenchymal transition in retinal pigment epithelium cells. Chen X, Xiao W, Wang W, et al. PLoS ONE 9(5), e96365, (2014)

Loading...


The Notch Delta-4 ligand helps to maintain the quiescence and the short-term reconstitutive potential of haematopoietic progenitor cells through activation of a key gene network. Catelain C, Michelet F, Hattabi A, et al. Stem Cell Res. 13(3 Pt A), 431-41, (2015)

Loading...


Cell cycle-linked MeCP2 phosphorylation modulates adult neurogenesis involving the Notch signalling pathway. Li H, Zhong X, Chau KF, et al. Nat. Commun. 5, 5601, (2014)

Loading...


Shedding of glycan-modifying enzymes by signal peptide peptidase-like 3 (SPPL3) regulates cellular N-glycosylation. Voss M, Künzel U, Higel F, et al. EMBO J. 33(24), 2890-905, (2014)

Loading...


ADAM10 and ADAM17 have opposite roles during sprouting angiogenesis. Caolo V, Swennen G, Chalaris A, et al. Angiogenesis 18(1), 13-22, (2014)

Loading...


EpCAM is overexpressed in local and metastatic prostate cancer, suppressed by chemotherapy and modulated by MET-associated miRNA-200c/205. Massoner P, Thomm T, Mack B, et al. Br. J. Cancer 111(5), 955-64, (2014)

Loading...


Visfatin promotes cell and tumor growth by upregulating Notch1 in breast cancer. Park HJ, Kim SR, Kim SS, et al. Oncotarget 5(13), 5087-99, (2014)

Loading...


Notch prevents transforming growth factor-beta-assisted epithelial-mesenchymal transition in cultured limbal progenitor cells through the induction of Smad7. Tsai TH, Sun MH, Ho TC, et al. Mol. Vis. 20, 522-34, (2014)

Loading...


Analysing human neural stem cell ontogeny by consecutive isolation of Notch active neural progenitors. Edri R, Yaffe Y, Ziller MJ, et al. Nat. Commun. 6, 6500, (2015)

Loading...


Generation of a ciliary margin-like stem cell niche from self-organizing human retinal tissue. Kuwahara A, Ozone C, Nakano T, et al. Nat. Commun. 6, 6286, (2015)

Loading...


An evolutionary-conserved function of mammalian notch family members as cell adhesion molecules. Murata A, Yoshino M, Hikosaka M, et al. PLoS ONE 9(9), e108535, (2014)

Loading...


A protease storm cleaves a cell-cell adhesion molecule in cancer: multiple proteases converge to regulate PTPmu in glioma cells. Phillips-Mason PJ, Craig SE, Brady-Kalnay SM, et al. J. Cell. Biochem. 115(9), 1609-23, (2014)

Loading...


Related Products

Technical Service:

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Bulk Ordering & Pricing:

Need larger quantities for your development, manufacturing or research applications?