DGKα-IN-10
DGKα-IN-10 is an orally active and potent DGKα inhibitor with an IC50 of 0.27 nM. DGKα-IN-10 can induce IL-2 release and T cells proliferation. DGKα-IN-10 can be used for the research of cancer, such as colon cancer.
For research use only. We do not sell to patients.
- CAS No.: 2980579-79-9
- Formula: C25H25N5O4
- Molecular Weight:459.50
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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
Biological Activity
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DKGα 0.27 nM (IC50) |
IL-2 |
DGKα-IN-10 (Compound 16) induces IL-2 release in human peripheral blood mononuclear cells (PBMCs) with an EC50 of 0.29 μM[1].
DGKα-IN-10 (12-1000 nM, 4 h) promotes proliferation of CD4+ and CD8+ T cells in human PBMCs[1].
DGKα-IN-10 (59.85-163.3 nM) enhances pERK activation in human T cells[1].
DGKα-IN-10 (1 μM) exhibits ≥100-fold selectivity for DGKα over most DGK isoforms[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human peripheral blood mononuclear cells (PBMCs)
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Concentration:12, 37, 111, 333 and 1000 nM
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Incubation Time:4 h
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Result:Increased CD4+ and CD8+ T cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MC38/CT26 xenograft C57BL/6J mice models[1]
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Dosage:0.5, 3 and 10 mg/kg, combined with anti-PD-1 antibody (3-5 mg/kg)
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Administration:Orally administration, twice a day
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Result:Reduced tumor volume.
Showed tumor growth inhibition (TGI) rate of 51.2%-90.3%.
Had no significant body weight loss.
Chemical Information
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CAS No. 2980579-79-9
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Molecular Weight 459.50
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Formula C25H25N5O4
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SMILES
N#CC1=NC2=C(N(C)C(C=C2N3CCC(C4=NC5=CC(C)=CC=C5O4)CC3)=O)C=C1OCCO
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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)
DGKα-IN-10 Related Classifications
HY-178062 Related Classifications
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