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Merck

565789

γ-Secretase Inhibitor XX

≥95% (HPLC), solid, γ-secretase inhibitor, Calbiochem®

Synonym(s):

γ-Secretase Inhibitor XX, (S,S)-2-[2-(3,5-Difluorophenyl)acetylamino]-N-(5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)propionamide, DBZ, Dibenzazepine

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About This Item

Empirical Formula (Hill Notation):
C26H23F2N3O3
CAS Number:
209984-56-5
Molecular Weight:
463.48
MDL number:
MFCD12828734
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

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Product Name

γ-Secretase Inhibitor XX, This γ-secretase inhibitor, CAS 209984-56-5, is a cell-permeable dibenzazepine compound that lowers both brain and plasma Aβ40 levels by ~72% in Tg2576 mutant APP transgenic mouse model.

InChI key

QSHGISMANBKLQL-OWJWWREXSA-N

SMILES string

Fc1cc(cc(c1)CC(=O)N[C@@H](C)C(=O)N[C@H]2c3c(cccc3)c4c(cccc4)N(C2=O)C)F

InChI

1S/C26H23F2N3O3/c1-15(29-23(32)13-16-11-17(27)14-18(28)12-16)25(33)30-24-21-9-4-3-7-19(21)20-8-5-6-10-22(20)31(2)26(24)34/h3-12,14-15,24H,13H2,1-2H3,(H,29,32)(H,30,33)/t15-,24-/m0/s1

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 10 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

100

Other Notes

Droy-Dupré, L., et al. 2012. Dis. Model Mech.5, 107.
van Es, J.H., et al. 2005. Nature435, 959.
Milano, J., et al. 2004. Toxicol. Sci.82, 341.

Packaging

Packaged under inert gas

Biochem/physiol Actions

Cell permeable: yes
Product does not compete with ATP.
Reversible: no
Target IC50: 1.7 nM inhibiting Notch processing in SupT1 cells

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable dibenzazepine (dbz) compound that acts as a potent γ-secretase inhibitor and significantly lowers both brain and plasma Aβ40 levels by ~72% in Tg2576 mutant APP transgenic mouse model (100 µmol/kg, b.i.d). Induces a heterogeneous reorganization of the crypt structural-proliferative units in the intestinal tract and of the stem cell niche in the colon. Also potently inhibits Notch processing (IC50 = 1.7 nM in SupT1 cells) and induces conversion of proliferative crypt cells to post-mitotic goblet cells in both the C57BL/6 and ApcMin mouse models (10 µmol/kg, i.p).
A cell-permeable, potent γ-secretase inhibitor that significantly lowers both brain and plasma Aβ40 levels by ~72% in Tg2576 mutant APP transgenic mouse model (100 µmol/kg, b.i.d). Induces a heterogeneous reorganization of the crypt structural-proliferative units in the intestinal tract and of the stem cell niche in the colon. Also potently inhibits Notch processing (IC50 = 1.7 nM in SupT1 cells) and induces conversion of proliferative crypt cells to post-mitotic goblet cells in both the C57BL/6 and ApcMin mouse models (10 µmol/kg, i.p).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

pictograms

Exclamation mark
GHS07

signalword

Warning

hcodes

H302,H317

Hazard Classifications

Acute Tox. 4 Oral - Skin Sens. 1A

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Anup K Nair et al.
Cells, 11(9) (2022-05-15)
The top genetic association signal for type 2 diabetes (T2D) in Southwestern American Indians maps to intron 15 of KCNQ1, an imprinted gene. We aim to understand the biology whereby variation at this locus affects T2D specifically in this genomic
Bahareh Rajaei et al.
Current protocols in human genetics, 100(1), e71-e71 (2018-10-20)
The International Diabetic Federation estimated that 415 million adults currently have diabetes and 318 million adults had impaired glucose tolerance, putting them at high risk of developing diabetes in the future. In Type 1 Diabetes (T1D), the β cells are
Siddharth Kishore et al.
Cell stem cell, 27(1), 137-146 (2020-05-23)
GATA6 is a critical regulator of pancreatic development, with heterozygous mutations in this transcription factor being the most common cause of pancreatic agenesis. To study the variability in disease phenotype among individuals harboring these mutations, a patient-induced pluripotent stem cell

Global Trade Item Number

SKUGTIN
565789-500UGCN04055977191844
565789-1MGCN04055977191837

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