2158266-58-9
2158266-58-9 structure
- Name: GNE-207
- Chemical Name: GNE-207
- CAS Number: 2158266-58-9
- Molecular Formula: C29H30N6O3
- Molecular Weight: 510.59
- Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
- Create Date: 2019-02-11 16:01:29
- Modify Date: 2024-01-14 19:08:53
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GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, a selectively index of >2500-fold against BRD4 (1) (IC50, 3.1 μM)[1]. GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells[1].
| Name | GNE-207 |
|---|
| Description | GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, a selectively index of >2500-fold against BRD4 (1) (IC50, 3.1 μM)[1]. GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells[1]. |
|---|---|
| Related Catalog | |
| Target |
CBP:1 nM (IC50) BRD4(1):3.1 μM (IC50) |
| In Vitro | GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, a selectively index of >2500-fold against BRD4 (1) (IC50, 3.1 μM)[1]. GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells[1]. |
| In Vivo | GNE-207 (5 mg/kg) shows moderate clearance in PK, with acceptable oral bioavailability[1]. |
| References |
| Molecular Formula | C29H30N6O3 |
|---|---|
| Molecular Weight | 510.59 |