化合物SH-4-54 T6669

Product Introduction
Bioactivity


英文名: SH-4-54

描述: SH-4-54 是有效小分子非磷酸化 STAT3 抑制剂，与 STAT3 和 STAT5 结合的 KD 值分别为 300 和 464 nM。

细胞实验: BTSC spheres are dissociated to single cells with the enzyme Accumax, seeded at 1500 cells/ 96-well and treated with drug or vehicle (DMSO) one day after plating. Cytotoxicity studies are repeated independently using BTSC lines 25M, 67EF, 73EF, 84EF and 127EF. BTSC spheres are dissociated to single cells as above and plated in 96 well plates in triplicate at 3000 cells/ 96-well. In both sets of experiments drugs are used as serial dilutions within the range of 5 μM to 100 nM in the first set and 25 μM to 10 nM. Cell viability following drug treatment is assessed three days later using the alamarBlue assay according to the manufacturer's instructions. All culture experiments are performed in triplicate with a minimum of three wells per condition.(Only for Reference)

激酶实验: Surface Plasmon Resonance (SPR) studies: The binding experiments are carried out on a ProteOn XPR36 biosensor at 25°C using the HTE sensor chip. The flow cells of the sensor chip are loaded with a nickel solution at 30 μL/min for 120 s to saturate the Tris–NTA surface with Ni(II) ions. Purified His-tagged STAT3 and STAT5 in PBST buffer (PBS with 0.005% (v/v) Tween-20 and 0.001% DMSO pH 7.4) is injected in the first and second channels of the chip respectively in the vertical direction at a flow rate of 25 μg/μL for 300 s, which attained, on average, ~8000 resonance unit (RU). After a wash with PBST buffer, inhibitors binding to the immobilized proteins is monitored by injecting a range of concentrations along with a blank at a flow rate of 100 μL/min for 200 s for each of these small molecules. When the injection of the small molecule inhibitor is completed, running buffer is allowed to flow over the immobilized substrates for the non-specifically bound inhibitors to dissociate for 600 s. Following dissociation of the inhibitors, the chip surface is regenerated with an injection of 1 M NaCl at a flow rate of 100 μL/ml for 18 s. Interspot channel reference is used for non-specific binding corrections and the blank channel used with each analyte injection served as a double reference to correct for possible baseline drift. Data are analyzed using ProteOn Manager Software version 3.1. The Langmuir 1:1 binding model was used to determine the KD values.

体外活性: SH-4-54有效抑制STAT3的磷酸化和其下游转录靶点。此外,SH-4-54对人恶性胶质瘤脑肿瘤肝细胞表现出空前的细胞毒性,而对人类胚胎星形胶质细胞没有毒性。

体内活性: 给BT73原位异种移植的小鼠腹腔注射10 mg/kgSH-4-54,有效抑制神经胶质肿瘤生长,并抑制pSTAT3.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 93 mg/mL (152.3 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 47 mg/mL (77 mM)


关键字: SH 4 54 | Inhibitor | SH-4-54 | SH454 | inhibit | STAT

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相关库: JAK-STAT Compound Library | Anti-Prostate Cancer Compound Library | Anti-Liver Cancer Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Diabetic Compound Library | Stem Cell Differentiation Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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