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BRD3308 HDAC inhibitor

Name: BRD3308
Brand: Selleck Chemicals
SKU: S8962
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S8962

BRD3308 is a potant and highly selective inhibitor of HDAC3 with IC50 of 54 nM, 1.26 μM and 1.34 μM for HDAC3, HDAC1 and HDAC2, respectively. This compound activates HIV-1 transcription. It suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines (glucolipotoxic stress) and increases functional insulin release.

Chemical Structure

Molecular Weight: 287.29

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S896201 DMSO]57 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 98.19%

98.19

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Chemical Information, Storage & Stability

Molecular Weight	287.29	Formula	C₁₅H₁₄FN₃O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1550053-02-5	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(=O)NC1=CC=C(C=C1)C(=O)NC2=C(C=C(C=C2)F)N

Solubility

In vitro
Batch:

DMSO : 57 mg/mL (198.4 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.850mg/ml (9.92mM)	Taking the 1 mL working solution as an example, add 50 μL of 57 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.350mg/ml (1.22mM)	Taking the 1 mL working solution as an example, add 50 μL of 7 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	HDAC3 ^[1] (Cell-free assay) 54 nM HDAC1 ^[1] (Cell-free assay) 1.26 μM HDAC2 ^[1] (Cell-free assay) 1.34 μM
In vitro	BRD3308 is a derivative of the ortho-aminoanilide HDAC inhibitor CI-994 and is developed to be highly selective for inhibition of HDAC3 with an IC50 value that is 23-fold lower for HDAC3 than for HDAC1 or 22. HDAC3 selective inhibition induces expression of HIV and exposure to this compound allows the recovery of latent HIV-1 from patient cells.^[1]
In vivo	Selective inhibition of HDAC3 by BRD3308 prevents diabetes onset in female NOD mice. This compound treatment in vivo prevents pancreatic islet infiltration and protects β-cells from apoptosis. β-cell proliferation is increased in animals treated with this chemical. This compound treatment in vivo prevents white adipose tissue infiltration in NOD mice.^[2]
References	[1] https://pubmed.ncbi.nlm.nih.gov/25136952/ [2] https://pubmed.ncbi.nlm.nih.gov/28860191/

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Handling Instructions

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