Product Details
Product Name:
GSK215 |
CAS No.:
2743427-26-9 |
Purity:
99.3% |
Supply Ability:
10g |
Release date:
2024/11/15 |
Product Introduction
Bioactivity
名稱 | GSK215 |
描述 | 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. |
體外活性 | 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]. |
體內(nèi)活性 | 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]. |
存儲(chǔ)條件 | Shipping with blue ice. |
溶解度 | DMSO : 225.0 mg/mL (228.4 mM ), Sonication is recommended.
|
關(guān)鍵字 | GSK215 | GSK 215 | GSK-215 |
相關(guān)產(chǎn)品 | Chloropyramine hydrochloride | ARV-471 | dBET6 | Roslin 2 bromide | Ifebemtinib FA | Ifebemtinib | Y15 | Defactinib | Masitinib | C004019 |
相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 酪氨酸激酶分子庫(kù) | 激酶抑制劑庫(kù) | 已知活性化合物庫(kù) | 細(xì)胞骨架化合物庫(kù) |
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 |
VIP1Y
|
Hubei Chuchang Biotech Co., Ltd.
|
2024-04-17 |