PAK1-IN-3
PAK1-IN-3 is a PAK1 inhibitor with an IC50 of 10 nM, an IC50 of 20 nM against PAK2, and an IC50 of 1079 nM against hERG potassium channels. PAK1-IN-3 forms a salt bridge with Asp106 in PAK1 via a properly positioned tertiary amine. PAK1-IN-3 inhibits PAK2 and hERG potassium channels.
For research use only. We do not sell to patients.
- Formula: C27H31ClN8O2
- Molecular Weight:535.04
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Storage:
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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PAK1 10 nM (IC50) |
PAK2 20 nM (IC50) |
In Vitro
PAK1-IN-3 (Compound 12) has a logD7.4 of 3.02, moderate solubility in PBS pH 7.4, high plasma protein binding, parent-like metabolic stability in human hepatocytes, and efflux ratios of 0.7 in MDCKII cells and 2.9 in Caco-2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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Molecular Weight 535.04
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Formula C27H31ClN8O2
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SMILES
O=C1C(C2=CC=C(C3=NC(C)=CN=C3)C=C2Cl)=CC4=CN=C(NCCN5OCCN(C)CC5)N=C4N1CC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PAK1-IN-3 Related Classifications
HY-182357 Related Classifications
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