化合物BIBF0775 T5197

Product Introduction
Bioactivity


英文名: BIBF0775

描述: BIBF0775 是一种选择性的TGFβI 型受体抑制剂(IC50:34 nM)。

细胞实验: The high-content cytotoxicity assay (kit I) was performed according to the manufacturer's instructions. HaCaT cells were cultured overnight in black 96-well plates, incubated for 24 h with each compound at different concentrations, and stained with cytotoxicity cocktail. Cells were fixed, washed, and scanned on the Cellomics ArrayScan II platform. Images were analyzed with the Cell Health image analysis algorithm. Cytotoxicity indices were calculated for each of the four parameters (cellular membrane integrity, nuclear fragmentation and density, and lysosomal mass) to indicate the percentage of cells outside of the normal range which was defined using a vehicle-treated reference cell population.

激酶实验: The inhibition of the kinase activity of TGFβRI was determined using the Promega Kinase-Glo kit according to the manufacturer's protocol in the presence of 600 nM ATP. N-terminally his-tagged human TGFβRI (aa 162-end) expressed in baculovirus and purified using nickel affinity chromatography was used at a final concentration of 0.03 μg/mL. The inhibition of the kinase activity of PDGFRR was determined using the Z0-LYTE assay technology according to the manufacturer's protocol. Full-length human PDGFRR (5.6 nM per assay) and the Tyr4 peptide (2 μM per assay) were obtained from Invitrogen, too. IC50 values were determined by the use of the Graph PadPrism software.

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

溶解度: DMSO : 60 mg/mL


关键字: BIBF-0775 | BIBF0775 | inhibit | Transforming growth factor beta receptors | TGF-β Receptor | BIBF 0775 | Inhibitor

相关产品: KRCA-0008 | Alectinib | A 83-01 | Ceritinib dihydrochloride | SB 525334 | Entrectinib | SB-505124 | ALK2-IN-2 | (-)-Cevimeline hydrochloride hemihydrate | GSK1838705A

相关库: Anti-Liver Cancer Compound Library | Immuno-Oncology Compound Library | Membrane Protein-targeted Compound Library | Anti-Ovarian Cancer Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Colorectal Cancer Compound Library | Tyrosine Kinase Inhibitor Library | TGF-beta/Smad Compound Library | Anti-Cardiovascular Disease Compound Library

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