2. Epigenetics
  3. Epigenetic Reader Domain
  4. GNE-064

GNE-064 (compound 5) is a selective, orally active and highly soluble inhibitor of SMARCA4, SMARCA2 and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC50 of 0.035 μM and inhibits SMARCA2 with an EC50 of 0.10 μM. GNE-064 possess Kds with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of agent synthesis.

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

GNE-064 Chemical Structure

GNE-064 Chemical Structure

CAS No. : 1997321-20-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 330 In-stock
Solution
10 mM * 1 mL in DMSO USD 330 In-stock
Solid
5 mg USD 300 In-stock
10 mg USD 480 In-stock
25 mg USD 950 In-stock
50 mg USD 1450 In-stock
100 mg USD 2250 In-stock
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Based on 1 publication(s) in Google Scholar

GNE-064 Related Antibodies

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Description

GNE-064 (compound 5) is a selective, orally active and highly soluble inhibitor of SMARCA4, SMARCA2 and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC50 of 0.035 μM and inhibits SMARCA2 with an EC50 of 0.10 μM. GNE-064 possess Kds with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of agent synthesis[1].

IC50 & Target

IC50: 0.035 μM (SMARCA4)[1]
In Vitro

GNE-064 (0-0.5 μM; 1 h) inhibits SMARCA2 in ZsGreen-SMARCA2 BD-expressing U2OS cells[1].

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

GNE-064 Related Antibodies

Cell Viability Assay[1]

Cell Line: ZsGreen-SMARCA2 BD-expressing U2OS cells
Concentration: 0-0.5 μM
Incubation Time: 1 hour
Result: Inhibited SMARCA2 in ZsGreen-SMARCA2 BD-expressing U2OS cells with an EC50 of 0.1 μM.
In Vivo

GNE-064 (compound 5) (0.5 and 1.0 mg/kg; i.v. and p.o. once ) exibits ideal pharmacokinetics value in female CD-1 mice [1].

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

Animal Model: Female CD-1 mice[1]
Dosage: 0.5 mg/kg (i.v.) and 1.0 mg/kg (p.o.)
Administration: Intravenous injection and oral gavage; 0.5 mg/kg and 1.0 mg/kg once
Result: Showed a low unbound plasma clearance with 16 mL/min/kg, a reasonable half-life of 1.1 h and good oral bioavailability of 59%.
Molecular Weight

327.38

Formula

C17H21N5O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(N1[C@H](C)CN(C2=CC(C3=CC=CC=C3O)=NN=C2N)CC1)=O
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 : ≥ 125 mg/mL (381.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0546 mL 15.2728 mL 30.5455 mL
5 mM 0.6109 mL 3.0546 mL 6.1091 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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. 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 3.0546 mL 15.2728 mL 30.5455 mL 76.3639 mL
5 mM 0.6109 mL 3.0546 mL 6.1091 mL 15.2728 mL
10 mM 0.3055 mL 1.5273 mL 3.0546 mL 7.6364 mL
15 mM 0.2036 mL 1.0182 mL 2.0364 mL 5.0909 mL
20 mM 0.1527 mL 0.7636 mL 1.5273 mL 3.8182 mL
25 mM 0.1222 mL 0.6109 mL 1.2218 mL 3.0546 mL
30 mM 0.1018 mL 0.5091 mL 1.0182 mL 2.5455 mL
40 mM 0.0764 mL 0.3818 mL 0.7636 mL 1.9091 mL
50 mM 0.0611 mL 0.3055 mL 0.6109 mL 1.5273 mL
60 mM 0.0509 mL 0.2545 mL 0.5091 mL 1.2727 mL
80 mM 0.0382 mL 0.1909 mL 0.3818 mL 0.9545 mL
100 mM 0.0305 mL 0.1527 mL 0.3055 mL 0.7636 mL
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GNE-064 Related Classifications

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-0641997321-20-6GNE064GNE 064Epigenetic Reader Domainoralchemical probebromodomainsmall moleculeInhibitorinhibitorinhibit

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