Referencia número: HY-108435

GNE-049

Name: GNE-049
Brand: MedChemExpress
SKU: HY-108435
Price: 190.00 USD
Availability: InStock
Rating: 5 (7 reviews)

7 Cited Publications

Revisión del cliente

Based on 7 publication(s) in Google Scholar

GNE-049 is a highly potent and selective CBP inhibitor with an IC₅₀ of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC₅₀s of 12 nM and 4200 nM, respectively.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza : 99.74%
No. CAS: 1936421-41-8
Fòrmula: C₂₇H₃₂F₂N₆O₂
Peso molecular:510.58

Almacenamiento:

-20°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

GNE-049 Chemical Structure

No. CAS: 1936421-41-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (7)
Solvente y solubilidad
- In Vitro
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

CBP/p300

Ver todos los productos específicos de isoformas Epigenetic Reader Domain :

Ver todos los productos específicos de isoformas Histone Acetyltransferase :

Cellular Effect

Cell Line	Type	Value	Description	References
CWR22R	IC₅₀	>1000 nM Compound: 1; GNE-049	Antiproliferative activity against AR positive human 22Rv1 cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay Antiproliferative activity against AR positive human 22Rv1 cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay	[PMID: 38530938]
CWR22R	IC₅₀	>1000 nM Compound: 3; GNE-049	Antiproliferative activity against human 22Rv1 cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay Antiproliferative activity against human 22Rv1 cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay	[PMID: 38477974]
HEK293	IC₅₀	12 nM Compound: 10	Inhibition of Halo-tagged histone H3.3 binding to NanoLuc luciferase conjugated human CBP expressed in HEK293 cells after overnight incubation by BRET assay Inhibition of Halo-tagged histone H3.3 binding to NanoLuc luciferase conjugated human CBP expressed in HEK293 cells after overnight incubation by BRET assay	[PMID: 28892380]
LNCaP	IC₅₀	>1000 nM Compound: 3; GNE-049	Antiproliferative activity against human LNCaP cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay Antiproliferative activity against human LNCaP cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay	[PMID: 38477974]
LNCaP	IC₅₀	7000 nM Compound: 1; GNE-049	Antiproliferative activity against AR positive human LNCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay Antiproliferative activity against AR positive human LNCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay	[PMID: 38530938]
VCaP	IC₅₀	>1000 nM Compound: 3; GNE-049	Antiproliferative activity against human VCaP cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay Antiproliferative activity against human VCaP cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay	[PMID: 38477974]
VCaP	IC₅₀	216 nM Compound: 1; GNE-049	Antiproliferative activity against AR positive human VCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay Antiproliferative activity against AR positive human VCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay	[PMID: 38530938]

In Vitro

GNE-049 is selected for further profiling as it has the best balance of liver microsomes (LM) stability, selectivity, and cellular potency GNE-049 has excellent potency in the BRET cellular assay and, in an orthogonal measure of the target engagement, GNE-049 is shown to inhibit the expression of MYC (MV4-11 cell line) with an EC₅₀ of 14 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GNE-049 demonstrates acceptable PK in mouse, rat, dog, and monkey. Determination of potency versus a selection of bromodomains revealed that GNE-049 is selective for CBP/P300 and, importantly, quite selective (3820-fold) over BRD4(1). GNE-049 is further evaluated in a rat single dose (30-250 mg/kg QD) toxicokinetic study. Adverse central nervous system (CNS)-related signs (e.g., marked hyperactivity and vocalization) are observed in several of the rats at the 250 mg/kg dose level. Furthermore, at the 250 mg/kg dose level, the ratio of the unbound drug concentration in brain to unbound drug concentration in plasma (K_p,uu) 3 h post dose is determined to be 0.43, indicating that GNE-049 is penetrating into the CNS and potentially resulting in the observed toxicity^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

No. CAS 1936421-41-8
Appearance Solid
Peso molecular 510.58
Fòrmula C₂₇H₃₂F₂N₆O₂
Color Light yellow to yellow
SMILES

CC(N1CCC(N(C2CCOCC2)N=C3N4CCCC5=C4C=C(C(F)F)C(C6=CN(C)N=C6)=C5)=C3C1)=O
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

-20°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Publications (7)

All Cell Proliferation/Viability AssayBio/Physico-chemical AssayCell Imaging/Staining

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Journal Impact Factor

Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Int J Biol Macromol

Lentinan attenuates histone deacetylation of SOCS1 promoter to remodel autophagy via JAK2/STAT3 pathway for the prevention of intervertebral disc degeneration. [Abstract]

2025 Sep;321(Pt 4):146457. PMID: 40749910
Mol Med

β-hydroxybutyrate resensitizes colorectal cancer cells to oxaliplatin by suppressing H3K79 methylation in vitro and in vivo. [Abstract]

2024 Jun 23;30(1):95. PMID: 38910244

GNE-049 purchased from MedChemExpress. Usage Cited in: Mol Med. 2024 Jun 23;30(1):95. [Abstract]

BHB significantly reduced the viability of HCT116-Oxa cells treated with GNE-049 (10 μM).

GNE-049 purchased from MedChemExpress. Usage Cited in: Mol Med. 2024 Jun 23;30(1):95. [Abstract]

BHB significantly reduced the proliferation ability of HCT116-Oxa cells treated with GNE-049 (10 μM).
ACS Chem Neurosci

Domain-Independent Inhibition of CBP/p300 Attenuates α-Synuclein Aggregation. [Abstract]

2021 Jul 7;12(13):2273-2279. PMID: 34110772

GNE-049 purchased from MedChemExpress. Usage Cited in: ACS Chem Neurosci. 2021 Jul 7;12(13):2273-2279. [Abstract]

GNE-049 at concentrations of 0.1, 1, and 10 μM added at DIV-12 to the PFF-pretreated primary dopaminergic cell culture significantly decreases formation of Lewy-body-like aggregates.

GNE-049 purchased from MedChemExpress. Usage Cited in: ACS Chem Neurosci. 2021 Jul 7;12(13):2273-2279. [Abstract]

Dopaminergic cell survival evaluated by the number of TH-positive cells was not affected by PFFs or by GNE-049 at concentrations of 0.1, 1 and 10 μM.

GNE-049 purchased from MedChemExpress. Usage Cited in: ACS Chem Neurosci. 2021 Jul 7;12(13):2273-2279. [Abstract]

Representative images of control- (top), PFF- (middle), and PFF-and-GNE-049-treated (bottom) groups. Arrowheads point at α-synuclein accumulations in TH-positive neurons.
bioRxiv

2025 Sep 7.
Patent

US20230255966A1.
bioRxiv

05 Oct 2021.

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (195.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9586 mL

9.7928 mL

19.5856 mL

5 mM

0.3917 mL

1.9586 mL

3.9171 mL

10 mM

0.1959 mL

0.9793 mL

1.9586 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Protocolo

Animal Administration^[1]

Mice^[1]
Twelve female CD-1 mice are used. All animals are 6-9 weeks old at the time of study and weighed between 20 and 35 g. Animals (n=3 per dosing route) are dosed with GNE-049 or GNE-781 at 1 mg/kg iv (in propyl ethylene glycol 400 (35% v/v) and water (65% v/v)) or 5 mg/kg po (suspended in 0.5% w/v methylcellulose, 0.2% w/v Tween 80). Food and water are available ad libitum to all animals. Serial blood samples (15 μL) are collected by tail nick at 0.033, 0.083, 0.25, 0.5, 1, 3, 8, and 24 h after the intravenous administration and 0.083, 0.25, 0.5, 1, 3, 8, and 24 h after the oral administration. All blood samples are diluted with 60 μL of water containing 1.7 mg/mL EDTA and kept at -80 °C until analysis^[1].
Rats^[1]
Twelve male Sprague-Dawley rats are used. All animals are 6-9 weeks old at the time of study and weighed between 200 and 300 g. Animals (n=3 per dosing route) are dosed with GNE-049 or GNE-781 at 1 mg/kg iv (in propyl ethylene glycol 400 (35% v/v) and water (65% v/v)) or 5 mg/kg po (suspended in 0.5% w/v methylcellulose, 0.2% w/v Tween 80). Food and water are available ad libitum to animals in the iv groups. Animals in po groups are fasted overnight and food withheld until 4 h postdose. Approximately 250 μL of blood are collected via the catheter at 0.033, 0.083, 0.25, 0.5, 1, 2, 4, 8, and 24 h after the intravenous or oral administration. All blood samples are collected into tubes containing 5 μL of 0.5 M K₂EDTA and processed for plasma. Samples are centrifuged (2500g for 15 min at 4°C) within 1 h of collection, and plasma samples are kept at -80 °C until analysis^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Romero FA, et al. GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP). J Med Chem. 2017 Nov 22;60(22):9162-9183. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9586 mL	9.7928 mL	19.5856 mL	48.9639 mL
	5 mM	0.3917 mL	1.9586 mL	3.9171 mL	9.7928 mL
	10 mM	0.1959 mL	0.9793 mL	1.9586 mL	4.8964 mL
	15 mM	0.1306 mL	0.6529 mL	1.3057 mL	3.2643 mL
	20 mM	0.0979 mL	0.4896 mL	0.9793 mL	2.4482 mL
	25 mM	0.0783 mL	0.3917 mL	0.7834 mL	1.9586 mL
	30 mM	0.0653 mL	0.3264 mL	0.6529 mL	1.6321 mL
	40 mM	0.0490 mL	0.2448 mL	0.4896 mL	1.2241 mL
	50 mM	0.0392 mL	0.1959 mL	0.3917 mL	0.9793 mL
	60 mM	0.0326 mL	0.1632 mL	0.3264 mL	0.8161 mL
	80 mM	0.0245 mL	0.1224 mL	0.2448 mL	0.6120 mL
	100 mM	0.0196 mL	0.0979 mL	0.1959 mL	0.4896 mL

Bioz

Keywords

GNE-049

7 Cited Publications

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GNE-049

Publications Citing Use of MedChemExpress (MCE) GNE-049

Ver todos los productos específicos de isoformas Epigenetic Reader Domain

Ver todos los productos específicos de isoformas Histone Acetyltransferase