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GSK J4 HCl

GSK J4 HCl is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family.

GSK J4 HCl化学構造

CAS No. 1797983-09-5

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 33000 国内在庫あり
JPY 25500 国内在庫あり
JPY 85500 国内在庫あり
JPY 145500 国内在庫あり
JPY 448500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
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GSK J4 HCl関連製品

シグナル伝達経路

Histone Demethylase Signaling Pathways

Histone Demethylaseシグナル伝達経路

Histone Demethylase阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
MCF7 Function assay 1 to 10 uM 30 hrs Inhibition of KDM5A in human MCF7 cells assessed as effect on H3K4me3 methylation levels at 1 to 10 uM after 30 hrs by Western blot analysis 30392349
MCF7 Function assay 1 to 10 uM 30 hrs Inhibition of KDM5A in human MCF7 cells assessed as effect on H3K27me3 methylation levels at 1 to 10 uM after 30 hrs by Western blot analysis 30392349
RAW264.7 0.82 uM 24 hrs Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells 0.82 uM after 24 hrs by ELISA 26776360
SF8628 Growth inhibitory assay 6 μM inhibits K28M glioma cell growth 25401693
SF7761 Growth inhibitory assay 6 μM inhibits K27M glioma cell growth 25401693
human astrocytes Kinase assay 6 μM increases K33 methylation 25401693
SF9427 Kinase assay 6 μM increases K32 methylation 25401693
SF9402 Kinase assay 6 μM increases K31 methylation 25401693
SF9012 Kinase assay 6 μM increases K30 methylation 25401693
H3.3 Kinase assay 6 μM increases K29 methylation 25401693
SF8628 Kinase assay 6 μM increases K28 methylation 25401693
SF7761 Kinase assay 6 μM increases K27 methylation 25401693
CUTLL1 Kinase assay 6 μM leads to increased H3K27me3 25132549
CUTLL1 Function assay 2 μM induces cell cycle arrest 25132549
CUTLL1 Apoptosis assay 2 μM induces apoptosis 25132549
CUTLL1 Growth inhibitory assay 2 μM affects cell growth 25132549
H3.3 Growth inhibitory assay 6 μM inhibits K29M glioma cell growth 25401693
SF9012 Growth inhibitory assay 6 μM inhibits K30M glioma cell growth 25401693
SF9402 Growth inhibitory assay 6 μM inhibits K31M glioma cell growth 25401693
SF9427 Growth inhibitory assay 6 μM inhibits K32M glioma cell growth 25401693
human astrocytes Growth inhibitory assay 6 μM inhibits K33M glioma cell growth 25401693
TG neurons Function assay 50 μM inhibits HSV-1 reactivation from sensory neurons 25552720
Th17 Function assay 80 nM inhibits cell differentiation 25840993
β-cells Function assay 20 μM blunts IFNγ, Il-1β, and TNFα-induced chemokine gene expression 26505193
β-cells Function assay 20 μM induces β-cell dysfunction 26505193
ESCs Function assay 1.8 µM induces DNA damage along with activation of the DNA damage response 26759175
Raw 264.7 Function assay 0.8192 µM inhibits TNF-α production 26776360
RAW264.7 24 hrs Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells after 24 hrs by ELISA 26776360
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生物活性

製品説明 GSK J4 HCl is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family.
Targets
JMJD3 [1]
(Cell-free assay)
60 nM
In Vitro
In vitro

GSK J4 HCl is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 with an IC50 value greater than 50 μM in vitro. GSK J4 HCl is used to probe the consequences of demethylation of H3K27me3. In human primary macrophages, GSK-J4 inhibits the lipopolysaccharide-induced production of cytokines, including pro-inflammatory tumour necrosis factor (TNF). In addition, GSK-J4 prevents the lipopolysaccharide-induced loss of H3K27me3 associated with the TNF transcription start sites and blocked the recruitment of RNA polymerase II. [1]
Kinase Assay Histone Demethylase AlphaScreen
Inhibition of histone demethylases is assessed using the histone demethylase AlphaScreen assay (Amplified Luminescence Proximity Homogenous Assay). This assay uses a biotinylated peptide substrate and relies on detection of the product methyl mark using a specific antibody coupled to protein-A acceptor beads and a Steptavidin donor bead to capture the peptide. In brief, recombinant demethylase enzymes are incubated in the presence of Fe2+ in the form of Ferrous Ammonium Sulphate (FAS), -ketoglutarate (KG) and biotinylated peptide substrate. L-Ascorbic Acid is included to provide a reducing environment and prevent oxidation of Fe2+. After incubation with peptide substrate the presence of the product is detected using AlphaScreen technology. The demethylase AlphaScreen assays are performed in 384-well plate format using white proxiplates. All steps are carried out in assay buffer (50 mM HEPES pH 7.5, 0.1% (w/v) BSA and 0.01 % (v/v) Tween-20). FAS is dissolved fresh each day in 20 mM HCl to a concentration of 400 mM and diluted to 1.0 mM in deionized water. All other components are dissolved fresh each day in deionized water. For IC50 determinations 5 μL of assay buffer containing demethylase enzyme is transferred to wells of a 384-well proxiplate. Titrations of compound (0.1 μL) are transferred to each well and the enzymes allowed to pre-incubate for 15 minutes with compound (final concentration of DMSO is 1%). The enzyme reaction is initiated by addition of 5 μL of a substrate mix consisting of α-KG, FAS, L-Ascorbic Acid and biotinylated peptide substrate and the reaction incubated for the indicated time at room temperature. The enzyme reaction is stopped after the indicated time by addinton of 5 μL of EDTA (7.5 mM final concentration in assay buffer). Streptavidin Donor beads (0.08 mg/ml) and Protein-A conjugated acceptor beads (0.08 mg/ml) are pre-incubated for 1 hour with an antibody to the product methyl mark and the presence of biotin-H3-product is detected by addition of 5 μL of the preincubated AlphaScreen beads (final concentrations of 0.02 mg/ml with respect to acceptor and donor beads). Detection is allowed to proceed for 1 hour at room temperature and the assay plates read in a BMG Labtech Pherastar FS plate reader. Data are normalized to the no enzyme control and the IC50 determined from the nonlinear regression curve fit using GraphPad Prism 5.
細胞実験 細胞株 Mouse podocytes
濃度 5 μM
反応時間 48 h
実験の流れ

Cells were serum starved for 4 hours, followed by treatment with EPZ-6438 (10 μM) or GSK-J4 (5 μM) for 48 hours.
In Vivo
In Vivo

GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A. It inhibits LPS-induced TNF-α production in human primary macrophages. GSK-J4 hydrochloride is a cell permeable prodrug of GSK-J1.
動物実験 動物モデル BALB/c mice
投与量 10 mg/kg
投与経路 i.p.

化学情報

分子量 453.96 化学式

C24H27N5O2.HCl
CAS No. 1797983-09-5 SDF Download GSK J4 HCl SDFをダウンロードする
Smiles CCOC(=O)CCNC1=CC(=NC(=N1)C2=CC=CC=N2)N3CCC4=CC=CC=C4CC3.Cl
保管

In vitro
Batch:

DMSO : 91 mg/mL ( (200.45 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 91 mg/mL

Water : 10 mg/mL

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

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 匹

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。

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