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Submit ReviewCompound E
Description: γ-secretase inhibitor; induces neuronal differentiation
Chemical Name: N-[(1S)-2-[[(3S)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluorobenzeneacetamide
Purity: ≥98% (HPLC)
Biological Activity
γ-secretase inhibitor. Enhances growth inhibition, differentiation and migration of neuroblastoma cells when used in a combination with DAPT (Cat. No. 2634) and 13-cis RA. In combination with hLIF, CHIR 99021 (Cat. No. 4423) and SB 431542 (Cat.No. 1614), accelerates the induction of a homogeneous, self-renewing primitive neuroepithelium population from hESCs. Active in vitro and in vivo.
Technical Data
| M. Wt | 490.5 |
| Formula | C27H24F2N4O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 209986-17-4 |
| PubChem ID | 11306390 |
| InChI Key | JNGZXGGOCLZBFB-IVCQMTBJSA-N |
| Smiles | C[C@@H](C(N[C@H]1N=C(C2=CC=CC=C2N(C1=O)C)C3=CC=CC=C3)=O)NC(CC4=CC(F)=CC(F)=C4)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 49.05 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 490.5. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.04 mL | 10.19 mL | 20.39 mL |
| 5 mM | 0.41 mL | 2.04 mL | 4.08 mL |
| 10 mM | 0.2 mL | 1.02 mL | 2.04 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.41 mL |
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References
References are publications that support the biological activity of the product.
Li et al (2011) Rapid induction and long-term self-renewal of primitive neural precursors from human embryonic stem cells by small molecule inhibitors. Proc.Natl.Acad.Sci.USA 108 8299 PMID: 21525408
Ferrari-Toninelli et al (2010) Targeting Notch pathway induces growth inhibition and differentiation of neuroblastoma cells. Neuro.Oncol. 12 1231 PMID: 20716592
Beher et al (2001) Pharmacological knock-down of the presenilin 1 heterodimer by a novel gamma -secretase inhibitor: implications for presenilin biology. J.Biol.Chem. 276 45394 PMID: 11574530
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Keywords: Compound E, Compound E supplier, gamma-secretase, g-secretase, inhibitors, inhibits, secretases, neuronal, differentiation, neurons, self, renewal, Gamma-Secretase, 6476, Tocris Bioscience
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