WH-4-023

製品コードS7565 バッチS756501

印刷

化学情報

Chemical Structure Synonyms KIN001-112, KIN112, Dual LCK/SRC inhibitor Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C32H36N6O4
分子量 568.67 CAS No. 837422-57-8
Solubility (25°C)* 体外 DMSO 12 mg/mL warmed with 50ºC water bath (21.1 mM)
Ethanol 6 mg/mL warmed with 50ºC water bath (10.55 mM)
Water 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 WH-4-023 (KIN001-112, KIN112, Dual LCK/SRC inhibitor) is a potent and orally active Lck/Src inhibitor with IC50s of 2 nM and 6 nM in cell-free assays, respectively. Exhibits >300-fold selectivity against p38α and KDR. Also potently inhibits SIK (IC50 values are 10, 22 and 60 nM for SIK 1, 2 and 3 respectively) and displays selectivity over a range of closely related kinases.
in vitro

WH-4-023 shows little activity on p38 and KDR. [1]

プロトコル(参考用のみ)

キナーゼアッセイ Lck Kinase Assay
The Lck HTRF kinase assay involves ATP-dependent phosphorylation of a biotinylated substrate peptide of gastrin in the presence or absence of inhibitor compound. The final concentration of gastrin is 1.2 μM. The final concentration of ATP is 0.5 μM (Km app = 0.6 ± 0.1 μM), and the final concentration of Lck (a GST-kinase domain fusion (AA 225−509)) is 250 pM. Buffer conditions are as follows:  50 mM HEPES pH = 7.5, 50 mM NaCl, 20 mM MgCl2, 5 mM MnCl, 2 mM DTT, 0.05% BSA. The assay is quenched and stopped with 160 μL of detection reagent. Detection reagents are as follows:  Buffer made of 50 mM Tris, pH = 7.5, 100 mM NaCl, 3 mM EDTA, 0.05% BSA, 0.1% Tween20. Prior to reading, Streptavidin allophycocyanin (SA-APC) is added at a final concentration in the assay of 0.0004 mg/mL, along with europilated anti-phosphotyrosine Ab (Eu-anti-PY) at a final conc of 0.025 nM. The assay plate is read in a Discovery fluorescence plate reader with excitation at 320 nm and emission at 615 and 655 nm. Assays for other kinases are done in a similar way as described above, varying the concentrations of enzyme, peptide substrate, and ATP added to the reaction, depending on the specific activity of the kinase and measured Kms for the substrates.
細胞アッセイ 細胞株 pgEpiSCs
濃度 1 μM
反応時間
実験の流れ

Cells were treated with indicated concentrations of drug.
動物実験 動物モデル C57BL/6 mice
投薬量 100 mg/kg
投与方法 i.v.

カスタマーフィードバック

Data from [Data independently produced by , , Blood, 2017, 130(25):2750-2761]

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：

Self-renewing human naïve pluripotent stem cells dedifferentiate in 3D culture and form blastoids spontaneously [ Nat Commun, 2024, 15(1):668] PubMed: 38253551
Generation of a humanized mesonephros in pigs from induced pluripotent stem cells via embryo complementation [ Cell Stem Cell, 2023, 30(9):1235-1245.e6] PubMed: 37683604
Modeling human pregastrulation development by 3D culture of blastoids generated from primed-to-naïve transitioning intermediates [ Protein Cell, 2023, 14(5):337-349] PubMed: 37155315
Short C-terminal Musashi-1 proteins regulate pluripotency states in embryonic stem cells [ Cell Rep, 2023, 42(10):113308] PubMed: 37858462
Discordance between chromatin accessibility and transcriptional activity during the human primed-to-naïve pluripotency transition process [ Cell Regen, 2023, 10.1186/s13619-023-00179-2] PubMed: 37938437
Generation and characterization of stable pig pregastrulation epiblast stem cell lines [ Cell Res, 2022, 32(4):383-400] PubMed: 34848870
Cell fate roadmap of human primed-to-naive transition reveals preimplantation cell lineage signatures [ Nat Commun, 2022, 13(1):3147] PubMed: 35672317
Recapitulating early human development with 8C-like cells [ Cell Rep, 2022, 39(12):110994] PubMed: 35732112
Oncogenic deubiquitination controls tyrosine kinase signaling and therapy response in acute lymphoblastic leukemia [ Sci Adv, 2022, 8(49):eabq8437] PubMed: 36490346
Generation and characterization of stable pig pregastrulation epiblast stem cell lines [ Cell Res, 2021, 10.1038/s41422-021-00592-9] PubMed: 34848870

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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