Pim-1 kinase-IN-17
Pim-1 kinase-IN-17 is a non-orthosteric inhibitor of PIM-1 onco-protein. Pim-1 kinase-IN-17 physically interacts with PIM-1 via a non-orthosteric binding site (Kd of 1.38 μM), does not inhibit PIM-1 kinase function, and decreases PIM-1 concentration under cellular conditions. Pim-1 kinase-IN-17 reduces tumor burden. Pim-1 kinase-IN-17 can be used for the research of triple-negative breast cancer.
For research use only. We do not sell to patients.
- Formula: C23H20N2O2S
- Molecular Weight:388.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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
Biological Activity
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PIM1 1.38 μM (Ki) |
Pim-1 kinase-IN-17 (compound 6d) (10 μM; 24 h) reduces PIM-1 protein concentration in MDA-MB-231 human TNBC cells, causing a 40.57% decrease in normalized luminescence[1].
Pim-1 kinase-IN-17 (10 μM; 24 h) reduces PIM-1 protein expression by 73% in MDA-MB-231 human TNBC cells[1].
Pim-1 kinase-IN-17 (0.1 μM-100 μM; 48 h) inhibits the viability of MDA-MB-231, 4T1, and EMT6 TNBC cells with IC50 values of 4.76 μM, 78.41 μM, and 8.59 μM, respectively[1].
Pim-1 kinase-IN-17 (10 μM; 7-9 days) strongly inhibits the clonogenic potential of MDA-MB-231 and EMT6 TNBC cells[1].
Pim-1 kinase-IN-17 (0.1 nM-10 μM) does not inhibit the catalytic activity of purified PIM-1 protein[1].
Pim-1 kinase-IN-17 (0.625 μM-10 μM) directly binds to purified His-tagged PIM-1 protein with an approximated Kd of 1.38 μM, as measured by BLI[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c (female, 8-9 weeks old, orthotopic xenograft model via implantation of 1×105 EMT6 mouse breast cancer cells mixed with Matrigel 1:1 into the mammary fat pad)[1]
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Dosage:30 mg/kg
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Administration:i.p.; 5 days per week; 21 days
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Result:Reduced tumor progression significantly compared to vehicle control.
Reduced final tumor weight significantly compared to vehicle control.
Reduced tumor volume with statistical significance relative to vehicle control.
Caused no significant changes in mouse body weight, indicating no treatment toxicity.
Chemical Information
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Molecular Weight 388.48
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Formula C23H20N2O2S
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SMILES
CC1=CC=C(C(NC2=CC=C(N(C)C(/C3=C/C4=CC=C(C)S4)=O)C3=C2)=O)C=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)
Pim-1 kinase-IN-17 Related Classifications
HY-184268 Related Classifications
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