| Name | BIBF0775 |
| Description | BIBF0775 is a selective TGFβ type I receptor (Alk5) inhibitor (IC50: 34 nM). |
| Cell Research | 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. |
| Kinase Assay | 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.04 mM), Sonication is recommended.
DMSO : 11 mg/mL (22.24 mM), Sonication is recommended.
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| Keywords | Transforming growth factor beta receptors | TGFβR1(ALK5) | TGF-β/Smad | TGF-β Receptor | TGFβ | TGFbeta/Smad | TGF-beta | TGFbeta | TGF-b/Smad | TGFb | Smad | Inhibitor | inhibit | BIBF-0775 | BIBF0775 | BIBF 0775 | Alk5 |
| Inhibitors Related | Alectinib | Trimethylamine N-oxide | Melamine | SB-431542 | Hydrochlorothiazide | Crizotinib | Brigatinib | Pirfenidone | A 83-01 | Cetrimonium bromide | Galunisertib | Alantolactone |
| Related Compound Libraries | Anti-Lung Cancer Compound Library | Reprogramming Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Fibrosis Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | TGF-beta/Smad Compound Library |
United States
