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ALK5 Inhibitor (RepSox) is a potent and selective inhibitor of the TGF-β RI kinase with IC50 values of 0.004 and 0.023 μM for ALK5 autophosphorylation and ALK5 binding, respectively. It enhances the efficiency of cellular reprogramming. ALK5 Inhibitor affects a range of related kinases selectively, including p38 MAPK, GSK3 and JNK1 (IC50 > 16 μM).
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Source | PLoS One (2013). Figure 3. ALK5 Inhibitor II |
| Method | HSA staining | |
| Cell Lines | HepG2 and HSC cells | |
| Concentrations | 10 μM | |
| Incubation Time | 48 h | |
| Results | The specificity of the conjugate was also determined by examining the effect of both free LY364947 and conjugate on HepG2 hepatocytes. The conjugate did not bind to these cells |
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Source | PLoS One (2013). Figure 2. ALK5 Inhibitor II |
| Method | ||
| Cell Lines | HepG2 and HSC cells | |
| Concentrations | 10 μM | |
| Incubation Time | 48 h | |
| Results | Both free LY-364947 and the conjugate significantly inhibited TGF-b1-induced Smad signaling, measured as luciferase activity, whereas the carrier itself did not have any effect. |
| Cell Experiment | |
|---|---|
| Cell lines | iPS cells |
| Preparation method | Cell Cyle Analysis Cells were treated with 25 μΜ RepSox in mES media without feeders for 72 hours and subjected to cell cycle analysis by propidium iodide staining and flow cytometry. Cells were harvested with .25% trypsin and fixed with 70% ethanol overnight. Following at least one hour of incubation with propidium iodide staining solution (50 μg/ml propidium iodide in PBS, .1% BSA, .1% Rnase A) in the dark, samples were analyzed on a BD LRSII Flow Cytometer (BD Biosciences). |
| Concentrations | 25µM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | chimeric embryos E13.5 |
| Formulation | not refered |
| Dosages | |
| Administration | |
| Molecular Weight | 287.32 |
| Formula | C17H13N5 |
| CAS Number | 446859-33-2 |
| Solubility (25°C) | DMSO ≥ 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related ALK Products |
|---|
| F-1
F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50 values of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively. |
| TL13-22
TL13-22 is a negative control for TL13-12 and a potent ALK inhibitor with an IC50 of 0.54 nM. |
| TL13-110
TL13-110 is a negative control for TL13-112 and a potent ALK inhibitor with an IC50 of 0.34 nM. |
| ALK inhibitor 2
ALK inhibitor 2 is a potent pyrimidin ALK inhibitor. |
| NVL-655 TFA
NVL-655 (ALK-IN-27) TFA is a novel, brain-permeable, selective ALK inhibitor with antitumor activity. For Ba/F3 CLIP1-LTK cells, NVL-655 (ALK-IN-27) TFA has an IC50 of 2.7 nM. It can be used in studies related to ALK-positive non-small cell lung cancer (NSCLC). |
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