Molibresib (I-BET-762)

製品コード:S7189 別名:GSK525762, GSK525762A

For research use only.

Molibresib (I-BET-762, GSK525762, GSK525762A) is an inhibitor for BET proteins with IC50 of ~35 nM in a cell-free assay, suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation, highly selective over other bromodomain-containing proteins.

Molibresib (I-BET-762)化学構造

CAS No. 1260907-17-2

サイズ 価格(税別)
10mM (1mL in DMSO) JPY 53400
JPY 34600
JPY 80000

代表番号: 03-5615-9297|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(26)

製品安全説明書

Epigenetic Reader Domain阻害剤の選択性比較

生物活性

製品説明 Molibresib (I-BET-762, GSK525762, GSK525762A) is an inhibitor for BET proteins with IC50 of ~35 nM in a cell-free assay, suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation, highly selective over other bromodomain-containing proteins.
ターゲット
BET proteins [1]
(Cell-free assay)
35 nM
体外試験

I-BET-762 is an inhibitor for BET (bromodomain and extra terminal domain) proteins, BRD2, BRD3 and BRD4, binds to the tandem bromodomains of BET with Kd of 50.5–61.3 nM, displaces a tetra-acetylated H4 peptide prebound to tandem bromodomains of BET with IC50 of 32.5–42.5 nM in FRET analysis. I-BET-762 occupies the acetyl-lysine binding pocket of BET proteins and inhibits binding of BET proteins to acetylated histones, thus disrupts the formation of the chromatin complexes essential for expression of inflammatory genes. [1] I-BET-762 treatment during the first 2 d of differentiation alters CD4+ T-cell cytokine production, up-regulated expression of several antiinflammatory gene products and down-regulated expression of several proinflammatory cytokines. [2]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2 MoPlSpVv[3Srb36gZZN{[Xl? MmTYNVghcHK| MVXJcoR2[3Srb36gc4YhcHWvYX6gRZBwSTFiZ3Xu[UBmgHC{ZYPzbY9vKGmwIIP0ZYJtgSC2cnHud4Zm[3SnZDDoeY1idiCKZYDHNkBk\WyuczDjc4V5eHKnc4PpcochdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIFnfGW{IEG4JIhzeyCkeTDseY1qdmW|Y3XuZ4Uh[XO|YYmsJGVEPTBiPTCwMlch|ryPLh?= M331e|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNU[4N|IzLz5{MUW2PFMzOjxxYU6=
HepG2 NX35e5JCTnWwY4Tpc44h[XO|YYm= NWXlRmRuPiCqcoO= MonuTY5lfWO2aX;uJI9nKGi3bXHuJGFxd0FzIIDyc5RmcW5ic4nueIhme2m|IHnuJIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KG6nb4P5cpRp\XOrc3XkJJJi\GmxbHHi[Yxm\CCycn;0[YlvKHOnY4LleIlwdiCjZoTldkA3KGi{czDifUBUTFNiUFHHSUBidmGueYPpd{BqdiCycnXz[Y5k\SCxZjDbN|VUZW2ndHjpc45qdmV? M2XOWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNU[4N|IzLz5{MUW2PFMzOjxxYU6=
HepG2 NHrlW2VHfW6ldHnvckBie3OjeR?= MXGxPEBpenN? MYDVdJJm\3WuYYTpc44hd2ZiQYDvRVEh\XiycnXzd4lwdiCrbjDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{Bkd26lZX70doF1cW:wIILldZVqemWmIITvJIlv[3KnYYPlJFcxLSCxZjDseYNq\mW{YYPlJIFkfGm4aYT5JIFnfGW{IEG4JIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEWFMUewJF0hOC5{IN88UU4> NYPSW5czRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzPFY2OjlpPkKyN|g3PTJ7PD;hQi=>
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アッセイ
Methods Test Index PMID
Growth inhibition assay Cell viability 26840085
体内試験 I-BET-762 confers protection against lipopolysaccharide-induced endotoxic shock and bacteria induced sepsisa. Single dose of I-BET applied at 1.5 h after LPS injection cures the mice. Twice-daily injections of I-BET for 2 days protects mice against death caused by sepsis. [1] Limited treatment with I-BET-762 exclusively during early priming inhibited the ability of Th1-differentiated 2D2 T cells to induce neuroinflammation in a mouse model of experimental autoimmune encephalomyelitis (EAE). [2]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
  • Fluorescence resonance energy transfer (FRET) titrations:

    Fluorescence resonance energy transfer (FRET) titrations. I-BET is titrated against BRD2 (200 nM), BRD3 (100 nM) and BRD4 (50 nM) in 50 mM HEPES pH7.5, 50 mM NaCl, 0.5 mM CHAPS in the presence of tetra-acetylated Histone H4 peptide (200 nM). After equilibrating for 1 hour, the bromodomain protein : peptide interaction is detected using FRET following the addition of 2nM Europium cryptate labelled streptavidin and 10 nM XL-665-labelled anti-6His antibody in assay buffer containing 0.05% (v/v) BSA and 400 mM KF. Plates are read using an Envision Plate reader (excitation 320 nm, emission 615 nm and 665 nm).

細胞試験:[2]
  • 細胞株:CD4+ T cells
  • 濃度: ~500 nM
  • 反応時間:60–72 h
  • 実験の流れ:CD4+ T cells are isolated from lymph nodes and spleens of 10- to 12-wk old mice and activated with plate bound anti-CD3 and anti-CD28 antibodies in the presence of indicated cytokines. I-BET-762 compounds is included during the 60–72 h of initial activation. Over the course of 5 d of T-cell culture and expansion, the compounds is diluted 12-fold relative to the starting concentrations.
動物試験:[1]
  • 動物モデル:Mouse
  • 投薬量:30 mg/kg
  • 投与方法:i.v.

溶解度 (25°C)

体外

化学情報

分子量 423.9
化学式

C22H22ClN5O2

CAS No. 1260907-17-2
Storage 3年 -20°C
2年 -80°C in solvent
Smiles CCNC(=O)CC1C2=NN=C(N2C3=C(C=C(C=C3)OC)C(=N1)C4=CC=C(C=C4)Cl)C

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

便利ツール

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03266159 Withdrawn Drug: GSK525762 Besylate tablets|Drug: Trametinib tablets Solid Tumours GlaxoSmithKline November 27 2017 Phase 2
NCT02964507 Completed Drug: GSK525762|Drug: Placebo|Drug: Fulvestrant Neoplasms GlaxoSmithKline February 2 2017 Phase 1
NCT01943851 Completed Drug: GSK525762 Neoplasms GlaxoSmithKline May 14 2014 Phase 2
NCT01587703 Completed Drug: GSK525762 Carcinoma Midline GlaxoSmithKline March 28 2012 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

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Tags: Molibresib (I-BET-762)を買う | Molibresib (I-BET-762) ic50 | Molibresib (I-BET-762)供給者 | Molibresib (I-BET-762)を購入する | Molibresib (I-BET-762)費用 | Molibresib (I-BET-762)生産者 | オーダーMolibresib (I-BET-762) | Molibresib (I-BET-762)化学構造 | Molibresib (I-BET-762)分子量 | Molibresib (I-BET-762)代理店