GSK215

SKU: orb1685568

Description

GSK215 is a potent and selective PROTAC degrader of focal adhesion kinase (FAK), achieving degradation with a pDC50 of 8.4. It is built from the FAK inhibitor VS-4718 and a VHL E3 ligase ligand, enabling rapid and sustained FAK loss, a valuable tool for studying FAK biology in cancer and metastasis research both in vitro and in vivo.

Research Area

Cardiovascular Research, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 2743427-26-9
• MW: 985.13
• Purity: 99.97% (May vary between batches)
• Formula: C₅₀H₅₉F₃N₁₀O₆S
• SMILES: CNC(=O)c1ccccc1Nc1cc(Nc2ccc(cc2OC)N2CCN(CC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)N[C@@H](C)c3ccc(cc3)-c3scnc3C)C(C)(C)C)CC2)ncc1C(F)(F)F
• Target: PROTACs,FAK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (5.08 mM);DMSO:225 mg/mL (228.4 mM)

Bioactivity

• 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.
• 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. 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GSK 215, GSK215, GSK-215, FAK

Compound Identifiers

PubChem CID

156600270