CPS-021
CPS-021 is a selective PAK4 PROTAC degrader with a DC50 of 50 nM. CPS-021 degrades PAK4 via the ubiquitin-proteasome system. CPS-021 inhibits the migration and invasion of tumor cells, suppresses TGFβ-induced epithelial-mesenchymal transition (EMT) in tumor cells, and can be used in studies related to lung cancer metastasis.
(Pink: PAK4 ligand (HY-174822); Blue: Cereblon ligand (HY-10984); Black: linker).
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- 화학식: C52H63N11O7
- 분자량:954.13
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
All PROTACs Isoforms
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Biological Activity
제품 설명
IC50 & Target
[1]|
PAK4 50 nM (DC50) |
LIMK1 |
In Vitro
CPS-021 (0.05-15.0 μM; 2-24 h) induces concentration-dependent and time-dependent degradation of PAK4 protein in A549 and MDA-MB-231 cells, without altering the phosphorylation level of PAK5[1].
CPS-021 inhibits PAK4 kinase activity in a cell-free system, with an IC50 value of 382.7 nM[1].
CPS-021 (0.6-10 µM) significantly reduces the protein and phosphorylation levels of PAK4 and its downstream target LIMK1 in H1299 cells[1].
CPS-021 (0.32-20 µM; 72 h) exhibits minimal cytotoxicity and weak antiproliferative activity in A549, MDA-MB-231 and H1299 cells[1].
CPS-021 (1-10 µM; 24-48 h) inhibits cell wound healing, migration and invasion in a concentration-dependent manner in A549, MDA-MB-231 and H1299 cells[1].
CPS-021 (0.01-0.64 μM) combined with TGF-β1 (HY-P78213) (5 ng/mL) blocks TGF-β-induced epithelial-mesenchymal transition (EMT) and alters the expression of related markers in A549 cells[1].
CPS-021 (5 μM; 14 h) exerts significant effects on altering the global proteome profile and regulating signaling pathways such as NOD-like receptors in A549 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 and MDA-MB-231
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Concentration:0.05, 0.15, 0.50, 1.50, 5.00, 15.0 µM
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Incubation Time:2, 4, 8, 12, 14, 24 h
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Result:Degraded PAK4 protein in a concentration-dependent manner.
Reduced PAK4 protein levels in a time-dependent manner, reaching maximum degradation at 24 hours.
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Cell Line:A549, MDA-MB-231, and H1299
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Concentration:0.32, 0.63, 1.25, 2.50, 5.00, 10.00, 20.00 µM
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Incubation Time:72 h
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Result:Exhibited low cytotoxicity at the tested concentrations and showed weak antiproliferative effects.
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Cell Line:A549, MDA-MB-231, and H1299
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Concentration:1.0, 5.0, 10.0 µM
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Incubation Time:24 h, 48 h
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Result:Effectively inhibited the wound healing and migration processes of the cells.
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Cell Line:A549, MDA-MB-231, and H1299
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Concentration:1.0, 5.0, 10.0 µM
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Incubation Time:48 h
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Result:Inhibited the migration and invasion capabilities of the cells in a concentration-dependent manner.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c-nu nude mice (lung cancer metastasis model via A549-luc luciferase-expressing lung cancer cell challenge)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:once daily; 14 days
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Result:Inhibited the in vivo migration of lung cancer cells.
Was well tolerated.
Inhibited tumor cell metastasis in vivo in a dose-dependent manner.
Chemical Information
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분자량 954.13
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화학식 C52H63N11O7
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SMILES
O=C(N1CCN(CC1)CCCCCCCC(N2CCN(CC2)CCNC3=CC=CC4=C3C(N(C4=O)C5CCC(NC5=O)=O)=O)=O)C(C6=CC=C(C#CC7(O)CCCCC7)C=C86)=CN8C9=NC(N)=NC=C9
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CPS-021 Related Classifications
HY-174247 Related Classifications
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