2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs FAK
  4. PROTAC FAK degrader 3

PROTAC FAK degrader 3 is a selective FAK PROTAC degrader (DC50 = 1.08 nM). PROTAC FAK degrader 3-induced FAK degradation is dependent on the ubiquitin-proteasome system and its binding to FAK and CRBN. PROTAC FAK degrader 3 upregulates MHC-I gene transcription and tumor cell surface expression by inhibiting the non-catalytic activity of FAK, leading to increased antigen presentation and activation of cytotoxic CD8 T cells. PROTAC FAK degrader 3 enhances in vivo anti-tumor activity by promoting MHC-I expression and enhancing T cell activation. PROTAC FAK degrader 3 can be used in cancer research targeting FAK degradation in ovarian cancer, hepatocellular carcinoma, and other cancers. (Pink: FAK-IN-3:HY-143407, Blue: Thalidomide-4-OH:HY-103596, Blue + Black: FAK ligand-3: HY-W939883, Black: Linker).

For research use only. We do not sell to patients.

PROTAC FAK degrader 3

PROTAC FAK degrader 3 Chemical Structure

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PROTAC FAK degrader 3 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

PROTAC FAK degrader 3 is a selective FAK PROTAC degrader (DC50 = 1.08 nM). PROTAC FAK degrader 3-induced FAK degradation is dependent on the ubiquitin-proteasome system and its binding to FAK and CRBN. PROTAC FAK degrader 3 upregulates MHC-I gene transcription and tumor cell surface expression by inhibiting the non-catalytic activity of FAK, leading to increased antigen presentation and activation of cytotoxic CD8 T cells. PROTAC FAK degrader 3 enhances in vivo anti-tumor activity by promoting MHC-I expression and enhancing T cell activation. PROTAC FAK degrader 3 can be used in cancer research targeting FAK degradation in ovarian cancer, hepatocellular carcinoma, and other cancers. (Pink: FAK-IN-3:HY-143407, Blue: Thalidomide-4-OH:HY-103596, Blue + Black: FAK ligand-3: HY-W939883, Black: Linker)[1].

IC50 & Target[1]

Cereblon

 

In Vitro

PROTAC FAK degrader 3 (Compound D4) (0-1000 nM, 24 h) induces FAK degradation in PA-1, ID8, 4T1, H22, HEY, MDA-MB-231, and PLC/PRF5 cells, induces 89% degradation of FAK at 50 nM and 92% degradation of FAK at 500 nM in PA-1 cells [1].
PROTAC FAK degrader 3 (1 μM) inhibits FAK (99%) (IC50 = 0.44 nM), STK33 (92%), CLK4 (87%), and Fes (86%) kinase activity[1].
PROTAC FAK degrader 3 (0.01-100 μM, 72 h) exhibits antiproliferative activity against PA-1, HEY, and Huh-7 cells[1].
PROTAC FAK degrader 3 (0-3 μM, 1-7 days) reduces colony formation, migration, and invasion in PA-1 cells[1].
PROTAC FAK degrader 3 (3 μM, 24 h) upregulates genes related to tumor immunogenicity, antigen presentation-related genes (HLA-B, HLA-F, and B2M), and immunoproteasome-related genes (PSMB8 and PSMB9) in PA-1 cells[1].
PROTAC FAK degrader 3 (3 μM, 24 h) promotes antigen presentation and MHC-I expression on the surface of tumor cells in ID8, PA-1, H22, PLC/PRF5 cells[1].
PROTAC FAK degrader 3 (3 μM, 72 h) promotes the activation and proliferation of antigen-specific CD8 T cells in ID8 cells cocultured with activated murine CD8 T cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PROTAC FAK degrader 3 Related Antibodies

Western Blot Analysis[1]

Cell Line: PA-1 cells
Concentration: 0 nM, 0.14 nM, 0.41 nM, 1.23 nM, 3.7 nM, 11.1 nM, 33.3 nM, 100 nM
Incubation Time: 0 h, 1 h, 2 h, 4 h, 6 h, 12 h, 24 h
Result: Induced FAK degradation, with almost complete degradation at 11.1 nM and achieved almost complete degradation at 24 h.

Western Blot Analysis[1]

Cell Line: ID8, 4T1, H22, HEY, MDA-MB-231, and PLC/PRF5 cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Induced FAK degradation.

Western Blot Analysis[1]

Cell Line: PA-1, H22 cells
Concentration: 3, 10, 30 nM
Incubation Time: 24 h
Result: Induced FAK degradation, showed comparable degradation activity to GSK215 (HY-132296) and was more effective than BI-3663 (HY-111546).

RT-PCR[1]

Cell Line: PA-1 cells
Concentration: 3 μM
Incubation Time: 24 h
Result: Had little effect on FAK mRNA levels.

Cell Migration Assay [1]

Cell Line: PA-1 cells
Concentration: 0.5 μM
Incubation Time: 24 h
Result: Reduced migration and invasion ability.

Western Blot Analysis[1]

Cell Line: ID8, PA-1, H22, PLC/PRF5 cells
Concentration: 3 μM
Incubation Time: 72 h
Result: Induced FAK degradation.
In Vivo

PROTAC FAK degrader 3 (Compound D4) (15 mg/kg, i.p., once a day, 8 days) improves antitumor activity by promoting MHC-I expression and reinforcing T cell activation in H22 tumor mice model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: H22 (1 × 106) tumor-bearing syngeneic mice (6 week-old BALB/cJ) model[1]
Dosage: 15 mg/kg
Administration: i.p., once a day, 8 days
Result: Inhibited tumor growth without affecting the body weight, enhanced expression of H2-Kd/H2-Dd on CD45- tumor cells (3.19-fold versus vehicle), without affecting Pd-l1 expression, expressed a higher level of CD107a (2.82-fold versus vehicle), indicating enhanced cell cytotoxicity.
Molecular Weight

882.96

Formula

C48H50N8O9
SMILES

O=C1CCC2=C1C(OC3=NC(NC4=CC=C(C=C4OC)C(NC5CCN(CC5)CCCCCCCOC6=C7C(C(N(C7=O)C8C(NC(CC8)=O)=O)=O)=CC=C6)=O)=NC9=C3C=CN9)=CC=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC FAK degrader 3 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC FAK degrader 3PROTAC FAK degrader3PROTAC FAK degrader-3PROTACsFAKPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinasePROTACdegraderovarian cancerhepatocellular carcinomaPA-1 cellsH22 cellsInhibitorinhibitorinhibit

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