GNE-272 is a potent and selective in Vivo Probe for the Bromodomains of CBP/EP300 (CBP IC50 = 0.02 μM, EP300 IC50 = 0.03 μM, BRET IC50 = 0.41 μM, BRD4(1) C50 = 13 μM).GNE-272 showed a marked antiproliferative effect in hematologic cancer cell lines and modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model. CBP has also been implicated in neurological disorders where a CBP bromodomain inhibitor has been shown to reduce expression of a regulator of G-protein signaling (RGS4).
MedKoo Cat#: 406825
Name: GNE-272
CAS#: 1936428-93-1
Chemical Formula: C22H25FN6O2
Exact Mass: 424.2023
Molecular Weight: 424.48
Elemental Analysis: C, 62.25; H, 5.94; F, 4.48; N, 19.80; O, 7.54
The following data is based on the product molecular weight 424.48 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 | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
