BRD3308

製品コードS8962 バッチS896201

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
化学式

C15H14FN3O2

分子量 287.29 CAS No. 1550053-02-5
Solubility (25°C)* 体外 DMSO 57 mg/mL (198.4 mM)
Water Insoluble
Ethanol Insoluble
体内 (毎回新しく調製した物を用意してください)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
2.85mg/ml 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 95% Corn oil
0.35mg/ml 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. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 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. BRD3308 activates HIV-1 transcription. BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines (glucolipotoxic stress) and increases functional insulin release.
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 BRD3308 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. HDAC3 treatment in vivo prevents pancreatic islet infiltration and protects β-cells from apoptosis. β-cell proliferation is increased in animals treated with BRD3308. HDAC3 treatment in vivo prevents white adipose tissue infiltration in NOD mice.[2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 2D10 cells, J89 cells, THP89 cells, J-Lat 6.3 cells
濃度 5 μM, 10 μM, 15 μM, 30 μM
反応時間 6 h, 12 h, 18 h, 24 h
実験の流れ

BRD3308 (15 μM) is added to aliquots of resting CD4+ T cells which are then plated in limiting dilution replicates of 2.5 or 1 million, 0.5 million, and 0.1 million cells and incubated at 37℃ under 5% CO2. BRD3308 is removed from the cultures after 24 hours.

動物実験 動物モデル Female NOD/ShiLTJ (NOD) mice
投薬量 0.1 mg/kg, 1 mg/kg, 10 mg/kg
投与方法 IP

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。