JNK Inhibitor IX

製品コードS7508 バッチS750801

印刷

化学情報

Chemical Structure Synonyms TCS JNK 5a Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20 H16 N2 O S
分子量 332.42 CAS No. 312917-14-9
Solubility (25°C)* 体外 DMSO 20 mg/mL (60.16 mM)
Water Insoluble
Ethanol Insoluble
* <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.

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生物活性

製品説明 JNK inhibitor IX (TCS JNK 5a) is a selective and potent JNK inhibitor with pIC50 of 6.5 and 6.7 for JNK2 and JNK3, respectively.
in vitro JNK inhibitor IX significantly reduces caspase-3 activity by the inhibition of JNK activity in human dermal fibroblasts. [2] JNK inhibition by JNK inhibitor IX significantly increases apoptotic death in response to imatinib mesylate (IM) by preventing c-ABL complete de-phosphorylation at Ser residues. [3]

プロトコル(参考用のみ)

キナーゼアッセイ JNK3 kinase inhibitory activity
JNK3 kinase inhibitory activity is determined using a fluorescence anisotropy kinase binding assay. The kinase, a fluorescently labelled inhibitor and a variable concentration of test compound are incubated together to reach thermodynamic equilibrium under conditions such that in the absence of test compound the fluorescent inhibitor is significantly (>50%) enzyme bound and in the presence of a sufficient concentration of a potent inhibitor the anisotropy of the unbound fluorescent ligand is measurably different from the bound value. Truncated human JNK3 is expressed in baculovirus as a N-terminal His (6)-tagged fusion protein. This enzyme (JNK3) is activated in 50 mM Tris/HCl, pH 7.5, 0.1 mM EGTA, 0.1% β-mercaptoethanol, 0.1 mM sodium vanadate, 10 mM magnesium acetate, 0.1 mM ATP with 100 nM active MKK4 and MKK7β at 30°C for 30 min. Following activation, the JNK3 is purified by Ni-NTA agarose chromatography. The JNK3 is then dialyzed into storage buffer (50 mM Tris/HCl, pH 7.5, 270 mM Sucrose, 150 mM NaCl, 0.1 mM EGTA, 0.1% β-mercaptoethanol, 0.03% Brij-35, 1 mM benzamidine and 0.2 mM PMSF), snap frozen in liquid nitrogen and stored at −70°C. Inhibitor binding to JNK3 is assessed by a fluorescence anisotropy competitive binding assay. All components are dissolved in buffer of composition 50 mM Hepes, pH 7.5, 1 mM CHAPS, 1 mM DTT, 10 mM MgCl2 with final concentrations of 10 nM JNK3 and 2 nM of a fluorescently labelled inhibitor. This reaction mixture is added to wells containing various concentrations of test compound (0.28 nM-16.6 μM final) or DMSO vehicle (<3% final) in black 384-well microtitre plates and equilibrated for 30-300 min at room temperature to reach equilibrium. Fluorescence anisotropy is read in Molecular Devices Acquest (excitation 530 nm/emission 580 nm).

カスタマーフィードバック

Data from [Data independently produced by , , Tumor Biol, 2016, 37:3135–3144.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

A subpopulation of CD146+ macrophages enhances antitumor immunity by activating the NLRP3 inflammasome [ Cell Mol Immunol, 2023, 20(8):908-923] PubMed: 37308559
Transcriptional control of pancreatic cancer immunosuppression by metabolic enzyme CD73 in a tumor-autonomous and -autocrine manner [ Nat Commun, 2023, 14(1):3364] PubMed: 37291128
Enhanced JunD/RSK3 signalling due to loss of BRD4/FOXD3/miR-548d-3p axis determines BET inhibition resistance. [ Nat Commun, 2020, 11(1):258] PubMed: 31937753
Targeting JNK pathway promotes human hematopoietic stem cell expansion. [ Cell Discov, 2019, 5:2] PubMed: 30622738
Size uniformity of animal cells is actively maintained by a p38 MAPK-dependent regulation of G1-length. [ Elife, 2018, 7] PubMed: 29595474
Lab-Attenuated Rabies Virus Causes Abortive Infection and Induces Cytokine Expression in Astrocytes by Activating Mitochondrial Antiviral-Signaling Protein Signaling Pathway [ Front Immunol, 2017, 8:2011] PubMed: 29403485
Icaritin activates JNK-dependent mPTP necrosis pathway in colorectal cancer cells. [Zhou C, et al. Tumour Biol, 2016, 37(3):3135-44] PubMed: 26427664
Functional differences between GDNF-dependent and FGF2-dependent mouse spermatogonial stem cell self-renewal. [ Stem Cell Reports, 2015, 4(3):489-502] PubMed: 25684228
ROS-Induced JNK and p38 Signaling Is Required for Unpaired Cytokine Activation during Drosophila Regeneration [ PLoS Genet, 2015, 11(10):e1005595] PubMed: 26496642

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。

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