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Gamma Secretase

DAPT (GSI-IX) (208255-80-5)

DAPT (GSI-IX) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells.

Not Intended for Therapeutic Use. For research use only.

CAS: 208255-80-5 Category

DAPT (GSI-IX) (208255-80-5) Description:

DAPT, also known GSI-IX, is a potent and selective γ-secretase inhibitor. DAPT is a non-transition-state analogue GSI and is the compound most widely evaluated in experimental models. DAPT causes a reduction in Aβ levels in human primary neuronal cell cultures with IC50 values = 115−200 nM. DAPT blocks Notch signaling in a cell-based assay measuring the activation of the Notch pathway reporter gene with an IC50 = 500 nM. As an inhibitor of Notch, DAPT has also been used in the study of autoimmune and lymphoproliferative diseases.

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).

DAPT (GSI-IX) (208255-80-5) Specifications:

Product Name DAPT
Synonyms DAPT;DAPT peptide; GSI-IX; GSI IX; N-(2FPhAc)Ala-phenyl-Gly t-butyl ester.
Chemical Names tert-butyl (S)-2-((S)-2-(2-(3,5-difluorophenyl)acetamido)propanamido)-2-phenylacetate
Purity >98% (or refer to the Certificate of Analysis)
CAS Number 1208255-80-5
Molecular Formula C23H26F2N2O4
Molecular Weight 432.4678
Monoisotopic Mass 432.186 g/mol
MDL number MFCD04974585
InChIKey DWJXYEABWRJFSP-XOBRGWDASA-N
InChi Code InChI=1S/C23H26F2N2O4/c1-14(26-19(28)12-15-10-17(24)13-18(25)11-15)21(29)27-20(16-8-6-5-7-9-16)22(30)31-23(2,3)4/h5-11,13-14,20H,12H2,1-4H3,(H,26,28)(H,27,29)/t14-,20-/m0/s1
SMILES O=C(OC(C)(C)C)[[email protected]](C1=CC=CC=C1)NC([[email protected]](C)NC(CC2=CC(F)=CC(F)=C2)=O)=O
Form Powder
Color white
Solubility  Soluble in DMSO, not in water
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >2 years if stored properly
Handling Protect from air and light
Application DAPT is a γ-secretase inhibitor with IC50s of 115 and 200 nM for total Aβ and Aβ42, respectively.

 


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RIDADR NONH for all modes of transport

References:

  • 1: Panaccione A, Chang MT, Carbone BE, Guo Y, Moskaluk CA, Virk RK, Chiriboga L, Prasad ML, Judson B, Mehra S, Yarbrough WG, Ivanov SV. NOTCH1 and SOX10 are Essential for Proliferation and Radiation Resistance of Cancer Stem-Like Cells in Adenoid Cystic Carcinoma. Clin Cancer Res. 2016 Apr 15;22(8):2083-95. doi: 10.1158/1078-0432.CCR-15-2208. PubMed PMID: 27084744.
  • 2: Zhou J, Jain S, Azad AK, Xu X, Yu HC, Xu Z, Godbout R, Fu Y. Notch and TGFβ form a positive regulatory loop and regulate EMT in epithelial ovarian cancer cells. Cell Signal. 2016 Apr 10. pii: S0898-6568(16)30076-6. doi: 10.1016/j.cellsig.2016.03.016. [Epub ahead of print] PubMed PMID: 27075926.
  • 3: Li P, Lin X, Zhang JR, Li Y, Lu J, Huang FC, Zheng CH, Xie JW, Wang JB, Huang CM. The expression of presenilin 1 enhances carcinogenesis and metastasis in gastric cancer. Oncotarget. 2016 Mar 1;7(9):10650-62. doi: 10.18632/oncotarget.7298. PubMed PMID: 26872378.
  • 4: Tang Z, Wei J, Yu Y, Zhang J, Liu L, Tang W, Long J, Zheng X, Jing W. γ-Secretase inhibitor reverts the Notch signaling attenuation of osteogenic differentiation in aged bone marrow mesenchymal stem cells. Cell Biol Int. 2016 Apr;40(4):439-47. doi: 10.1002/cbin.10583. Epub 2016 Feb 4. PubMed PMID: 26801333.
  • 5: Campbell DP, Chrysostomou E, Doetzlhofer A. Canonical Notch signaling plays an instructive role in auditory supporting cell development. Sci Rep. 2016 Jan 20;6:19484. doi: 10.1038/srep19484. PubMed PMID: 26786414; PubMed Central PMCID: PMC4726253.

1 review for DAPT (GSI-IX) (208255-80-5)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The DAPT (GSI-IX) (208255-80-5) is high purity,also customer service is pretty nice !gotta try!!

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