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Compound E

Cat. No. M9505
Compound E Structure
Synonym:

GSI-XXI; γ-secretase inhibitor XXI

Size Price Availability Quantity
2mg USD 310  USD310 In stock
5mg USD 520  USD520 In stock
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Quality Control
Biological Activity

Compound E is a cell-permeable, potent, selective inhibitor of γ-secretase and Notch processing. Compound E bloks β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC50s of 0.24, 0.37, 0.32 nM, respectively. Compound E reduces the proliferation of T47D, and MCF-7 cell lines by less than 50% at a concentration of 50 μM.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 490.51
Formula C27H24F2N4O3
CAS Number 209986-17-4
Purity >99%
Solubility DMSO ≥ 60 mg/mL
Storage at -20°C
References

[1] Saenger AK. Clin Chem. Discovery of the wonder drug: from cows to cortisone. The effects of the adrenal cortical hormone 17-hydroxy-11-dehydrocorticosterone (Compound E) on the acute phase of rheumatic fever; preliminary report. Mayo Clin Proc 1949;24:277-97.

[2] Rasul S, et al. Br J Cancer. Inhibition of gamma-secretase induces G2/M arrest and triggers apoptosis in breast cancer cells.

[3] Beher D, et al. J Biol Chem. PharnacoIogicaI knock-down of the presenilin 1 heterodimer by a novel gamma -secretase inhibitor: implications for presenilin biology.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Compound E, GSI-XXI; γ-secretase inhibitor XXI supplier, Gamma-secretase, inhibitors

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