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.
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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]|
DKGα 0.27 nM (IC50) |
IL-2 |
In Vitro
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. Further protocols information, click here.
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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.
Parmacokinetics
In Vivo
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.
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.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
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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