Powder: -20°C for 3 years | In solvent: -80°C for 1 year
WH-4-023 (Dual LCK/SRC inhibitor) 是选择性Lck 和Src 抑制剂,它们的 IC50 分别为 2 nM、6 nM,对p38α 和 KDR 作用效果稍弱。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 389 | 现货 | ||
5 mg | ¥ 667 | 现货 | ||
10 mg | ¥ 995 | 现货 | ||
50 mg | ¥ 2,125 | 现货 | ||
100 mg | ¥ 3,798 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 829 | 现货 |
产品描述 | WH-4-023 (Dual LCK/SRC inhibitor) is a potent and orally active Lck/Src inhibitor. It also potently inhibits SIK. |
靶点活性 | Lck:2 nM, Src:6 nM |
体外活性 | WH-4-023 shows little activity on p38 and KDR. [1] |
激酶实验 | 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 MnCl2, 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[1]. |
细胞实验 | WH-4-023 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. The purpose of this assay is to test the potency of T cell receptor (TCR; CD3) and CD28 signaling pathway inhibitors in human T cells. T cells are purified from human peripheral blood lymphocytes (hPBL) and preincubated with or without compound prior to stimulation with a combination of an anti-CD3 and an anti-CD28 antibody in 96-well tissue culture plates (1×105 T cells/well). Cells are cultured for ~20 h at 37°C in 5% CO2 and then secreted IL-2 in the supernatants is quantified by cytokine ELISA. The cells remaining in the wells are then pulsed with 3H-thymidine overnight to assess the T cell proliferative response. Cells are harvested onto glass fiber filters and 3H-thymidine incorporation into DNA is analyzed by liquid scintillation counter. For comparison purposes, phorbol myristic acid (PMA) and calcium ionophore are used in combination to induce IL-2 secretion from purified T cells. Potential inhibitor compounds are tested for inhibition of this response as described above for anti-CD3 and -CD28 antibodies. Human whole-blood anti-CD3/CD28-induced IL-2 secretion assays are run in a similar fashion as described above using whole blood from normal volunteers diluted 50% in tissue culture medium prior to stimulation[1]. |
别名 | KIN112, KIN001-112, Dual LCK/SRC inhibitor |
分子量 | 568.67 |
分子式 | C32H36N6O4 |
CAS No. | 837422-57-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 10 mg/mL (17.6 mM)
Ethanol: 6 mg/mL (10.55 mM), Heating is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.7585 mL | 8.7924 mL | 17.5849 mL | 43.9622 mL |
5 mM | 0.3517 mL | 1.7585 mL | 3.517 mL | 8.7924 mL | |
10 mM | 0.1758 mL | 0.8792 mL | 1.7585 mL | 4.3962 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
WH-4-023 837422-57-8 Angiogenesis Tyrosine Kinase/Adaptors Src WH 4 023 KIN112 inhibit Inhibitor KIN 112 KIN-112 KIN001-112 WH4023 Dual LCK/SRC inhibitor inhibitor