PAK1-IN-1

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PAK1-IN-1 is a potent and selective PAK1 inhibitor with an IC₅₀ of 9.8 nM. PAK1-IN-1 inhibits the migration and invasion of PAK1-related tumour cells in a dose-dependent manner.

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

PAK1-IN-1 Chemical Structure

CAS No. : 2485732-30-5

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PAK1 PAK2 PAK3 PAK4 PAK5 PAK6

Biological Activity
Purity & Documentation
References
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Description

PAK1-IN-1 is a potent and selective PAK1 inhibitor with an IC₅₀ of 9.8 nM. PAK1-IN-1 inhibits the migration and invasion of PAK1-related tumour cells in a dose-dependent manner^[1].

IC₅₀ & Target^[1]

PAK1

9.8 nM (IC₅₀)

PAK4

>10 μM (IC₅₀)

In Vitro

PAK1-IN-1 (compound 30l) (0-10 µM) shows selectivity with IC₅₀s of 0.01, >10 µM for PAK1 and PAK4, respectively^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	MDA-MB-231, HCT-116 cells
Concentration:	1 µM
Incubation Time:	72 h
Result:	Showed antiproliferative activity against MDA-MB-231and HCT-116 cells with inhibition of 6.31% and 8.73%, respectively.

Western Blot Analysis^[1]

Cell Line:	MDA-MB-231 cells
Concentration:	2.5, 5, 10, 20 µM
Incubation Time:	1, 24 h
Result:	Decreased the expression of activated PAK1 (PAKp-Ser144) and Snail in a dose-dependent manner.

Molecular Weight

469.92

Formula

C₂₆H₂₀ClN₅O₂

CAS No.

2485732-30-5

SMILES

CC1=CC=CN(C1=O)C2=CC=C(C(Cl)=C2)C3=CC=C4C(NN=C4C(NCC5=CC=NC=C5)=O)=C3

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

Handling Instructions (2659 KB)

References

[1]. Zhang M, et al. Design and synthesis of 1H-indazole-3-carboxamide derivatives as potent and selective PAK1 inhibitors with anti-tumour migration and invasion activities. Eur J Med Chem. 2020 Oct 1;203:112517. [Content Brief]

PAK1-IN-1 Related Classifications

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

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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:

PAK1-IN-12485732-30-5PAKp21 activated kinaseslow cytotoxicityanticancerSnailMDA-MB-231HCT-116 cellsanti-migrationinvasionInhibitorinhibitorinhibit

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