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Referencia número: HY-174247

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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).

Para uso exclusivo en investigación. No vendemos a pacientes.

Fòrmula: C₅₂H₆₃N₁₁O₇
Peso molecular:954.13

Almacenamiento:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

CPS-021 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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^[1]. (Pink: PAK4 ligand (HY-174822); Blue: Cereblon ligand (HY-10984); Black: linker).

IC₅₀ & Target

^[1]

PAK4

50 nM (DC₅₀)

LIMK1

Ver todos los productos específicos de isoformas PROTACs :

Ver todos los productos específicos de isoformas PAK :

Ver todos los productos específicos de isoformas LIM Kinase (LIMK) :

LIMK1
LIMK2

Ver todos los productos específicos de isoformas TGF-β Receptor :

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.

Western Blot Analysis^[1]

Cell Line:

A549 and MDA-MB-231
Concentration:

0.05, 0.15, 0.50, 1.50, 5.00, 15.0 µM
Incubation Time:

2, 4, 8, 12, 14, 24 h
Result:

Degraded PAK4 protein in a concentration-dependent manner.
Reduced PAK4 protein levels in a time-dependent manner, reaching maximum degradation at 24 hours.

Cell Viability Assay^[1]

Cell Line:

A549, MDA-MB-231, and H1299
Concentration:

0.32, 0.63, 1.25, 2.50, 5.00, 10.00, 20.00 µM
Incubation Time:

72 h
Result:

Exhibited low cytotoxicity at the tested concentrations and showed weak antiproliferative effects.

Cell Migration Assay ^[1]

Cell Line:

A549, MDA-MB-231, and H1299
Concentration:

1.0, 5.0, 10.0 µM
Incubation Time:

24 h, 48 h
Result:

Effectively inhibited the wound healing and migration processes of the cells.

Cell Invasion Assay^[1]

Cell Line:

A549, MDA-MB-231, and H1299
Concentration:

1.0, 5.0, 10.0 µM
Incubation Time:

48 h
Result:

Inhibited the migration and invasion capabilities of the cells in a concentration-dependent manner.

Parmacokinetics

Species	Dose	Route	T_1/2	C₀	C_max	T_max	AUC_0-∞	AUC_0-t	CL	V_ss	F
Mice^[1]	1 mg/kg	i.v.	3.32 h	657.70 ng/mL	459.90 ng/mL	0.0833 h	332.62 ng·h/mL	312.84 ng·h/mL	52.12 mL/min/kg	8.59 L/kg	/
Mice^[1]	2 mg/kg	i.p.	1.36 h	/	343.11 ng/mL	2.00 h	1220.51 ng·h/mL	1191.40 ng·h/mL	/	/	183.47 %

In Vivo

CPS-021 (5-20 mg/kg; once daily; 14 days) exerts inhibitory effects on tumor metastasis and invasion in the BALB/c-nu nude mouse model of tumor lung metastasis^[1].

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

Animal Model:

Balb/c-nu nude mice (lung cancer metastasis model via A549-luc luciferase-expressing lung cancer cell challenge)^[1]
Dosage:

5 mg/kg; 10 mg/kg; 20 mg/kg
Administration:

once daily; 14 days
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

Peso molecular 954.13
Fòrmula C₅₂H₆₃N₁₁O₇
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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Wang H, et al. Design, Synthesis, and Biological Evaluation of Selective PAK4 Degrader for the Treatment of Lung Tumor Metastasis. Journal of medicinal chemistry. 2025 Jun 12;68(11):11231-11269. [Content Brief]

Calculators

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

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100 mg

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureza y Documentación
Referencias

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Cantidad:
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CPS-021

Ver todos los productos específicos de isoformas PROTACs

Ver todos los productos específicos de isoformas PAK

Ver todos los productos específicos de isoformas LIM Kinase (LIMK)

Ver todos los productos específicos de isoformas TGF-β Receptor