AHL-7160
AHL-7160 is a molecular glue degrader targeting DGKα, with an IC50 value of 12 nM against the human protein. AHL-7160 rapidly recruits DGKα to the plasma membrane, blocks DGKα-mediated phosphatidic acid production, and induces proteasome-dependent degradation of DGKα with full proteome selectivity. AHL-7160 enhances primary T cell-mediated glioblastoma cell killing. AHL-7160 can be used in related research on glioblastoma.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C28H30N8O3S
- Molecular Weight:558.65
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
IL-2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293-A | EC50 |
39 nM
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Recruitment of endogenous DGKα to the plasma membrane of CRISPR-edited HEK293A cells stably expressing NG-tagged endogenous DGKα, measured via TIRF microscopy over up to 600 seconds post-treatment.
Recruitment of endogenous DGKα to the plasma membrane of CRISPR-edited HEK293A cells stably expressing NG-tagged endogenous DGKα, measured via TIRF microscopy over up to 600 seconds post-treatment.
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PMC12713590 |
| HEK293-A | IC50 |
340 nM
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Inhibition of DGKα-mediated phosphatidic acid production at mitochondrial and plasma membrane subcellular regions in HEK293A cells with a chemically inducible mitochondrial DGKα activation system, monitored via the PILS-Nir1 biosensor over up to 10 minutes post-stimulation with rapamycin.
Inhibition of DGKα-mediated phosphatidic acid production at mitochondrial and plasma membrane subcellular regions in HEK293A cells with a chemically inducible mitochondrial DGKα activation system, monitored via the PILS-Nir1 biosensor over up to 10 minutes post-stimulation with rapamycin.
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PMC12713590 |
In Vitro
AHL-7160 potently and covalently inhibits recombinant human DGKα-HEK293T proteome activity with an IC50 of 12 nM[1].
AHL-7160 (5 µM; 2 hours) stereoselectively engages endogenous DGKα at residues Y669 and K411 in Jurkat T cells without altering DGKα protein abundance[1].
AHL-7160 (1-1000 nM; up to 10 minutes post-stimulation) stereoselectively blocks DGKα-mediated PA production at mitochondrial and plasma membrane subcellular regions in HEK293A cells with an IC50 of 340 nM[1].
AHL-7160 (0.01-10 µM; 24 hours primary T cell cytokine assays) stereoselectively potentiates MAPK signaling and IL-2 production in anti-CD3/CD28-activated Jurkat T cells, and elicits a broad, multi-effector cytokine response in activated primary human CD4+ and CD8+ T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 558.65
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Formel C28H30N8O3S
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SMILES
CN(C1=CC=C(C#N)N=C1C(N2C[C@@H](C)N(CC3=CC=C(S(N4C=NC(C5CC5)=N4)(=O)=O)C=C3)C[C@@H]2C)=C6)C6=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
AHL-7160 Related Classifications
HY-180898 Related Classifications
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