LZK-IN-1
LZK-IN-1 is an orally active and selective LZK inhibitor with a Kd of 2.7 nM. LZK-IN-1 disrupts the LZK-AKT protein-protein interaction, blocks AKT autophosphorylation, and reduces the activation of the downstream JNK pathway. LZK-IN-1 inhibits the proliferation of cancer cells with MAP3K13 amplification and reduces in vivo tumor growth in xenograft mouse models. LZK-IN-1 can be used for the study of esophageal squamous cell carcinoma and head and neck squamous cell carcinoma with MAP3K13 amplification.
For research use only. We do not sell to patients.
- CAS No.: 2912371-82-3
- Formula: C23H30F2N6
- Molecular Weight:428.52
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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
- Purity & Documentation
- References
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Help & FAQs
All MAP3K Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
MAP3K13/LZK 2.7 nM (Kd) |
In Vitro
LZK-IN-1 (Compound #1) exhibits potent in vitro binding affinity for the LZK kinase protein, with a measured Kd of 2.7 nM[1].
LZK-IN-1 (100 nM) exhibits high selectivity for LZK in a panel of over 450 tested kinases[1].
LZK-IN-1 (100 nM-1 μM) effectively inhibits LZK-mediated activation of the JNK pathway in MAP3K13-amplified KYSE70 esophageal squamous cell carcinoma cells in a dose-dependent manner[1].
LZK-IN-1 (0 nM-10000 nM; 72 h) significantly reduces the viability of MAP3K13-amplified OVCAR5 cells in a 72-hour MTS assay[1].
LZK-IN-1 (0 nM-500 nM; 14 days) significantly inhibits the long-term clonogenic survival of MAP3K13-amplified OVCAR5 esophageal squamous cell carcinoma (ESCC) cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MAP3K13-amplified OVCAR5 cells
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Concentration:0 nM-10000 nM (12-point dose range)
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Incubation Time:72 h
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Result:Produces suppression of OVCAR5 cell viability to a comparable extent to the reference LZK inhibitor GNE-3511.
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 nude mice (6- to 8-week-old female)[1]
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Dosage:50 mg/kg
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Administration:oral gavage; twice daily; 4 to 8 weeks
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Result:Achieved significant tumor growth suppression in both MAP3K13-amplified ESCC PDX models.
Showed reduced Ki-67 proliferation marker staining in ES3862 tumor tissues.
Recorded no adverse body weight loss in exposed mice.
Chemical Information
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CAS No. 2912371-82-3
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Molecular Weight 428.52
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Formula C23H30F2N6
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SMILES
CC1=NC=C(NC2=CC(C3CCN(CC4CC4)CC3)=CC(N5CCC(F)(F)C5)=N2)N=C1
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LZK-IN-1 Related Classifications
HY-189202 Related Classifications
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