DGKα&ζ-IN-2
DGKα/ζ-IN-2 is a potent, orally active and selective dual DGKα/ζ inhibitor with IC50 values of 23 nM (DGKα) and 1.2 nM (DGKζ). DGKα/ζ-IN-2 exhibits selectivity over other DGK isoforms, such as DGKβ and DGKγ. DGKα/ζ-IN-2 shows robust and dose-dependent immune activation in the presence of antigen presentation in an OT-1 murine model. DGKα/ζ-IN-2 can be used for antitumor immunity.
For research use only. We do not sell to patients.
- CAS No.: 3039488-61-1
- Formula: C35H34F4N6O2
- Molecular Weight:646.68
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
DGKα/ζ-IN-2 (compound 17) demonstrates an excellent selectivity across a broad panel of kinases (HPK1, EPHA2, FLT3, KDR, KIT, PDGFRβ and TRKA), with IC50 values > 10 μM[1].
DGKα/ζ-IN-2 demonstrates potent functional activity by promoting IL-2 production in both Jurkat cells (EC50 = 64 nM) and human whole blood (EC50 = 447 nM)[1].
DGKα/ζ-IN-2 exhibits a balanced in vitro ADME profile, with low human microsomal clearance (0.6 L/h/kg), high Caco-2 permeability (1.2 × 10⁻⁶ cm/s), and high solubility in both fasted-state simulated intestinal fluid (> 1000 μg/mL) and simulated gastric fluid (659 μg/mL)[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:Female OT-I mice[1]
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Dosage:5, 25, and 50 mg/kg
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Administration:p.o., single dose
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Result:Resulted in a dose-dependent increase in CD69+ CD8+ T cells when combined with low dose (0.225 μg) SIINFEKL (HY-P5411), with the highest activation observed at 50 mg/kg.
Partial coverage of the whole blood EC₅₀ was sufficient to achieve full T cell activation.
Did not elicit significant T cell activation alone.
Showed no unexpected deaths or significant adverse effects.
Chemical Information
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CAS No. 3039488-61-1
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Molecular Weight 646.68
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Formula C35H34F4N6O2
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SMILES
F/C(C1=NC(C2=CC=NN=C2)=CN=C1)=C\C3=CC=C(C(C(F)(F)F)=C3N4CCOC5(C4)CCN(CC5)CC6CC6)OC7=CC=CC=C7
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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&ζ-IN-2 Related Classifications
HY-178327 Related Classifications
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