Product Details
| Product Name:
GSK215 |
CAS No.:
2743427-26-9 |
| Purity:
99.30% |
Supply Ability:
10g |
| Release date:
2025/11/09 |
Product Introduction
Bioactivity
| Name | GSK215 |
| Description | GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader (pDC50= 8.4), designed using the FAK inhibitor VS-4718 and a binder for the VHL E3 ligase, capable of inducing rapid and prolonged FAK degradation. |
| In vitro | GSK215 induced degradation is proteasome and ubiquitin dependent. GSK215 (0.1-1000 nM; 2 h) effectively increases the FAK degradation by >90% and determines a DC50 of 1.3 nM in A549 cells[1]. GSK215 (100 nM, 48 h) inhibits migration, invasion and collagen deposition in A549 cells. GSK215 (above 100 nM, 6h) reduces primarily kinases CDK7, RPS6KA3, MET and GAK[1]. |
| In vivo | GSK215 (8 mg/kg; i.h.; once) degrades FAK, and exhibits the Cmax and tmax values of 526 ng/mL and 0.33 hours, respectively[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 225.0 mg/mL (228.4 mM ), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (5.08 mM), Sonication is recommended.
|
| Keywords | GSK-215 | GSK215 | GSK 215 | FAK |
| Inhibitors Related | Chloropyramine hydrochloride | ARV-471 | dBET6 | Roslin 2 bromide | Ifebemtinib FA | OXA-11 | Y15 | AU-15330 | Defactinib | PND-1186 | Masitinib | C004019 |
| Related Compound Libraries | Bioactive Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Angiogenesis related Compound Library | Bioactive Compounds Library Max | Cytoskeletal Signaling Pathway Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$0.00/10mg |
|
Hubei Chuchang Biotech Co., Ltd.
|
2024-04-17 |
United States