JNK Inhibitor IX

製品コードS7508 バッチS750801

印刷

化学情報

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

体内（毎回新しく調製した物を用意してください）

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 この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.500mg/ml (4.51mM)	Taking the 1 mL working solution as an example, add 50 μL of 30 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.

* <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	JNK Inhibitor IX (TCS JNK 5a) は、JNK2 および JNK3 に対する pIC50 がそれぞれ 6.5 および 6.7 の、選択的かつ強力な JNK 阻害剤です。
in vitro	JNK inhibitor IX significantly reduces caspase-3 activity by the inhibition of JNK activity in human dermal fibroblasts. 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.

プロトコル(参考用のみ)

キナーゼアッセイ	JNK3 kinase inhibitory activity
キナーゼアッセイ	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).

参考

https://pubmed.ncbi.nlm.nih.gov/17194588/
https://pubmed.ncbi.nlm.nih.gov/19406221/
https://pubmed.ncbi.nlm.nih.gov/19220809/

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：

JNK mediates serine phosphorylation of STAT3 in response to fatty acids released by lipolysis [ Res Sq, 2025, rs.3.rs-6150649]	PubMed: 40092442
SRC kinase drives multidrug resistance induced by KRAS-G12C inhibition [ Sci Adv, 2024, 10(50):eadq4274]	PubMed: 39661665
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

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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