受注:045-509-1970 |
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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 |
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化学式 | C32H36N6O4 |
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分子量 | 568.67 | CAS No. | 837422-57-8 | ||||
Solubility (25°C)* | 体外 | DMSO (warmed with 50ºC water bath) | 100 mg/mL (175.84 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) |
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* <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. |
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. |
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in vitro | WH-4-023 shows little activity on p38 and KDR. [1] |
キナーゼアッセイ | Lck Kinase Assay | |
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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. |
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動物実験 | 動物モデル | C57BL/6 mice |
投薬量 | 100 mg/kg | |
投与方法 | i.v. |
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Data from [Data independently produced by , , Blood, 2017, 130(25):2750-2761]
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。