1. Epigenetics
  2. Epigenetic Reader Domain
    Histone Acetyltransferase
  3. GNE-207

GNE-207 

Cat. No.: HY-120028 Purity: 98.10%
Handling Instructions

GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells.

For research use only. We do not sell to patients.

GNE-207 Chemical Structure

GNE-207 Chemical Structure

CAS No. : 2158266-58-9

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 1101 In-stock
Estimated Time of Arrival: December 31
1 mg USD 550 In-stock
Estimated Time of Arrival: December 31
5 mg USD 980 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells[1].

IC50 & Target[1]

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].

Molecular Weight

510.59

Formula

C₂₉H₃₀N₆O₃

CAS No.

2158266-58-9

SMILES

O=C(NC)C1=NC=C(C2=CC3=C(C=N2)C(C4=NN(C5CCOCC5)C6=C4CN(C(C)=O)CC6)=CC=C3)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (391.70 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9585 mL 9.7926 mL 19.5852 mL
5 mM 0.3917 mL 1.9585 mL 3.9170 mL
10 mM 0.1959 mL 0.9793 mL 1.9585 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 5 mg/mL (9.79 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 5 mg/mL (9.79 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (9.79 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

GNE-207GNE207GNE 207Epigenetic Reader DomainHistone AcetyltransferaseHATsHATInhibitorinhibitorinhibit

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GNE-207
Cat. No.:
HY-120028
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