- Shanghai Nianxing Industrial Co., Ltd
- China
- Product Name: FAK inhibitor 5
- Price:
- Purity: 98.0%
- Stocking Period: 10 Day
- Contact: Huang
1426683-30-8
1426683-30-8 structure
- Name: FAK inhibitor 5
- Chemical Name: FAK inhibitor 5
- CAS Number: 1426683-30-8
- Molecular Formula: C20H21N3O2S
- Molecular Weight: 367.46
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK FAK
- Create Date: 2020-06-01 18:14:13
- Modify Date: 2024-01-12 07:14:37
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FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range[1].
| Name | FAK inhibitor 5 |
|---|
| Description | FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range[1]. |
|---|---|
| Related Catalog | |
| Target |
1.6 μM (pre-incubation 5 min ATP 0.5 μM), 1.3 μM (pre-incubation 60 min ATP 0.5 μM), 3.0 μM (pre-incubation 5 min ATP 1000 μM), 1.0 μM (pre-incubation 60 min ATP 1000 μM). |
| In Vitro | The binding interactions between FAK inhibitor 5 (compound 2) in the FAK allosteric site is mostly hydrophobic in nature. Exposure of the allosteric pocket by the dramatic movement of Ile547 is accompanied by an equally significant movement of Arg550 in toward the allosteric binding site, where it packs along the tricyclic core of compounds 2. Notably, the terminal ethylphenyl group of compounds 2 occupies the DFG-in pocket, thereby dislodging Phe565 and enabling the structural rearrangement of the activation loop and observed occlusion of the FAK active site[1]. |
| References |
| Molecular Formula | C20H21N3O2S |
|---|---|
| Molecular Weight | 367.46 |