2. Epigenetics
  3. Epigenetic Reader Domain Histone Acetyltransferase
  4. GNE-049

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.

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GNE-049

GNE-049 構造式

CAS 番号 : 1936421-41-8

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 213 在庫あり
Solution
10 mM * 1 mL in DMSO USD 213 在庫あり
Solid
5 mg $190 在庫あり
10 mg $304 在庫あり
25 mg $495 在庫あり
50 mg $690 在庫あり
100 mg $970 在庫あり
250 mg $1460 在庫あり
500 mg $2100 在庫あり
1 g $2950 在庫あり
5 g   お問い合わせ  
10 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 7 publication(s) in Google Scholar

Other Forms of GNE-049:

GNE-049 関連抗体

Top Publications Citing Use of Products

Histone Acetyltransferase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

  • 生物活性

  • プロトコル

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

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[1].

IC50 & Target

CBP/p300

 

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]
体外実験

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.

GNE-049 関連抗体
体内実験

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 (Kp,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.
分子量

510.58

分子式

C27H32F2N6O2
CAS 番号
Appearance

Solid

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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

-20°C, stored under nitrogen

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

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
純度とドキュメンテーション
参考文献
動物実験
[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) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

Complete Stock Solution Preparation Table

* 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.

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
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GNE-049 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GNE-0491936421-41-8GNE049GNE 049Epigenetic Reader DomainHistone AcetyltransferaseHATsHATInhibitorinhibitorinhibit

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製品名:
GNE-049
製品番号:
HY-108435
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