JNK Inhibitor IX

製品コードS7508 バッチS7508

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
* <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
A subpopulation of CD146+ macrophages enhances antitumor immunity by activating the NLRP3 inflammasome [ Cellular & Molecular Immunology, 2023, 908-923]	PubMed: 37308559.0
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
JNK inhibitor IX restrains pancreatic cancer through p53 and p21 [ Frontiers in Oncology, 2022, 1006131]	PubMed: 36568248.0
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 Discovery, 2019, 2]	PubMed: 30622738.0
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

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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