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| Targets |
GNE-375 targets BRD9, a bromodomain-containing protein involved in epigenetic regulation. It inhibits BRD9 with an IC₅₀ of 5 nM and shows >100-fold selectivity over BRD4, TAF1, and CECR2. The compound decreases BRD9 binding to chromatin and decreases expression of ALDH1A1, a gene important in drug tolerance.
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| ln Vitro |
In vitro, GNE-375 inhibits BRD9 binding to chromatin. It decreases expression of ALDH1A1, a gene previously shown to be important in drug tolerance. The compound can be used to study epigenetic resistance mechanisms. It shows potent activity in BRD9-dependent cellular assays.
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| ln Vivo |
In vivo, GNE-375 has been studied for its potential to modulate epigenetic regulation. As a selective BRD9 inhibitor, it may have therapeutic applications in diseases where BRD9 plays a role.
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| Enzyme Assay |
BRD9 binding assays: BRD9 protein is incubated with GNE-375 at various concentrations (typically 0.1-100 nM) and binding affinity is measured using fluorescence polarization, surface plasmon resonance, or AlphaScreen assays. IC₅₀ values are calculated from dose-response curves. Selectivity is assessed by testing against other bromodomain-containing proteins (BRD4, TAF1, CECR2).
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| Cell Assay |
Cells expressing BRD9-dependent genes are cultured in appropriate media at 37°C with 5% CO₂. Cells are treated with GNE-375 at various concentrations. BRD9 chromatin binding is assessed by ChIP-qPCR. Gene expression changes (e.g., ALDH1A1) are measured by qRT-PCR. Cell viability and proliferation are assessed by MTT or CellTiter-Glo assays.
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| Animal Protocol |
In vivo studies are conducted in animal models relevant to BRD9 function. GNE-375 is administered orally or via other routes at specified doses. Target engagement is assessed by analyzing BRD9 binding to chromatin in tissues. Pharmacodynamic markers such as ALDH1A1 expression are measured.
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| ADME/Pharmacokinetics |
GNE-375 has molecular weight 451.51 and formula C₂₅H₂₉N₃O₅. It is soluble in DMSO (30 mg/mL, 66.44 mM). Density is 1.246 g/cm³ (predicted). Purity is ≥98%. The compound is a selective and potent BRD9 inhibitor.
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| References | |
| Additional Infomation |
GNE-375 is a potent and highly selective BRD9 inhibitor with an IC₅₀ of 5 nM. It shows >100-fold selectivity for BRD9 over BRD4, TAF1, and CECR2. The compound decreases BRD9 binding to chromatin and decreases expression of ALDH1A1, a gene important in drug tolerance. It can be used to study epigenetic resistance and BRD9 function.
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| Molecular Formula |
C24H27N3O5
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| Molecular Weight |
437.48828625679
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| Exact Mass |
437.1951
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| CAS # |
1926989-06-1
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| Appearance |
Off-white to pink solid powder
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| SMILES |
O1CCN(C(C2=CC(=C(C=C2OC)C2=CN(C/C=C/C)C(C3=C2C=CN3)=O)OC)=O)CC1
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| Synonyms |
GNE375; GNE 375; GNE-375
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~110.74 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2858 mL | 11.4288 mL | 22.8577 mL | |
| 5 mM | 0.4572 mL | 2.2858 mL | 4.5715 mL | |
| 10 mM | 0.2286 mL | 1.1429 mL | 2.2858 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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