| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
HIV-1; HDAC2 ( Ki = 6300 nM ); HDAC2 ( IC50 = 1340 nM ); HDAC1 ( Ki = 5100 nM ); HDAC1 ( IC50 = 1260 nM ); HDAC3 ( Ki = 29 nM ); HDAC3 ( Ki = 54 nM )
BRD3308 targets HDAC3. It is a highly selective inhibitor that binds to the active site of HDAC3. By inhibiting HDAC3, the compound alters the acetylation of histones and other proteins, leading to changes in gene expression. This inhibition has been shown to activate HIV-1 transcription and protect pancreatic β-cells from apoptosis. |
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| ln Vitro |
BRD3308 is a derivative of the ortho-aminoanilide HDAC inhibitor CI-994. Its IC50 value is 23 times lower for HDAC3 than it is for HDAC1 or 22, indicating that it is highly selective on HDAC3 inhibition. Exposure to BRD3308 facilitates the recovery of latent HIV-1 from patient cells and selective inhibition of HDAC3 induces HIV expression.[1]
In vitro, BRD3308 has been shown to be a potent inhibitor of HDAC3. It inhibits pancreatic β-cell apoptosis induced by inflammatory cytokines or glycolipotoxic stress. The compound also activates HIV-1 transcription in latently infected cells. These effects are consistent with its mechanism of action as an HDAC3 inhibitor. |
| ln Vivo |
BRD3308 selectively inhibits HDAC3 to stop diabetes in female NOD mice from developing. In vivo administration of HDAC3 treatment inhibits pancreatic islet infiltration and shields β-cells from apoptosis. Animals treated with BRD3308 exhibit increased proliferation of β-cells. In NOD mice, HDAC3 treatment stops white adipose tissue infiltration in vivo.[2]
In vivo, BRD3308 has been shown to reduce hyperglycemia and increase insulin secretion in a rat model of type 2 diabetes. It improves hyperglycemia without affecting weight gain. These effects make it a potential therapeutic agent for the treatment of type 2 diabetes. |
| Enzyme Assay |
In vitro enzyme or receptor binding (non-cell) assays for BRD3308 involve measuring its direct inhibition of HDAC3 enzymatic activity. The assay uses a purified recombinant HDAC3 enzyme and a fluorogenic peptide substrate. The deacetylation of the substrate releases a fluorescent product. The compound is incubated with the enzyme and substrate, and the decrease in fluorescence is measured to determine the IC50. Selectivity is assessed by testing the compound against HDAC1 and HDAC2.
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| Cell Assay |
Aliquots of resting CD4+ T cells are mixed with 15 μM of BRD3308, and plated in limiting dilution replicates of 2.5 or 1 million, 0.5 million, and 0.1 million cells. The cells are then incubated at 37°C with 5% CO2. The cultures of BRD3308 are withdrawn after a 24-hour period.
In vitro cell-based assays for BRD3308 are performed using pancreatic β-cell lines (e.g., INS-1E) and HIV-1 latently infected cell lines. Cells are treated with the compound, and β-cell apoptosis is measured by detecting caspase activation and cell viability. HIV-1 transcription is measured by quantifying viral RNA or by using a reporter assay. |
| Animal Protocol |
Female NOD/ShiLTJ (NOD) mice
0.1 mg/kg, 1 mg/kg, 10 mg/kg IP In vivo animal experiments for BRD3308 are conducted using a rat model of type 2 diabetes. The compound is administered, and blood glucose and insulin levels are measured. A hyperglycemic clamp experiment is performed to assess insulin secretion. |
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of BRD3308 have been characterized to support its use as a research tool. The compound has a molecular weight of 273.26 and a formula of C₁₅H₁₄FN₃O₂. It is soluble in DMSO. Specific PK parameters, such as half-life and bioavailability, are determined in preclinical studies via LC-MS/MS analysis of plasma samples.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for BRD3308 are typical of a research compound. It is generally well-tolerated at effective doses. The safety profile is being evaluated in the context of its use as a research tool to study HDAC3 biology.
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| References | |
| Additional Infomation |
Other information: BRD3308 is a research compound used to study HDAC3, HIV-1 latency, and type 2 diabetes. It is available from chemical suppliers for preclinical research purposes.
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| Molecular Formula |
C15H14FN3O2
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|---|---|
| Molecular Weight |
287.2944
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| Exact Mass |
287.106
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| Elemental Analysis |
C, 62.71; H, 4.91; F, 6.61; N, 14.63; O, 11.14
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| CAS # |
1550053-02-5
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| PubChem CID |
72734382
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
449.9±45.0 °C at 760 mmHg
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| Flash Point |
225.9±28.7 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.689
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| LogP |
1.81
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
21
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| Complexity |
383
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C([H])=C([H])C(=C(C=1[H])N([H])[H])N([H])C(C1C([H])=C([H])C(=C([H])C=1[H])N([H])C(C([H])([H])[H])=O)=O
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| InChi Key |
RRJDFENBXIEAPD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H14FN3O2/c1-9(20)18-12-5-2-10(3-6-12)15(21)19-14-7-4-11(16)8-13(14)17/h2-8H,17H2,1H3,(H,18,20)(H,19,21)
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| Chemical Name |
4-acetamido-N-(2-amino-4-fluorophenyl)benzamide
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| Synonyms |
BRD-3308; BRD3308; BRD 3308
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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 : 57~250 mg/mL (198.4~870.2 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.24 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.24 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4808 mL | 17.4040 mL | 34.8080 mL | |
| 5 mM | 0.6962 mL | 3.4808 mL | 6.9616 mL | |
| 10 mM | 0.3481 mL | 1.7404 mL | 3.4808 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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