Dyrk1A-IN-16
Dyrk1A-IN-16 is a selective, brain-penetrant and ATP-competitive Dyrk1A inhibitor with a IC50 of 53 nM. Dyrk1A-IN-16 displays high selectivity across a broad kinase panel (specific for DYRK kinases) with nanomolar potency. Dyrk1A-IN-16 impairs neurosphere self-renewal, cell invasion, and EGFR stability in vitro. Dyrk1A-IN-16 inhibits tumor growth and prolongs survival in vivo. Dyrk1A-IN-16 has potential for glioblastoma (GBM) research.
For research use only. We do not sell to patients.
- CAS No.: 2805339-74-4
- Formula: C14H9NO5S
- Molecular Weight:303.29
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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
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Biological Activity
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DYRK1A 50 nM (IC50) |
Dyrk1A-IN-16 (compound FC-3) (0-100 nM) is a reversible and ATP-competitive inhibitor, could be overcome at higher concentrations of ATP[1].
Dyrk1A-IN-16 (5-20 µM, 72 h) primarily targets at DYRK1A in the GBM cell line U87MG[1].
Dyrk1A-IN-16 (5-10 µM, 24 h) exerts inhibitory effects on invasion through an on-target effect on DYRK1A in the GBM cell line U87MG[1].
Dyrk1A-IN-16 (1-10 µM, 20 h) accelerates EGFR destabilization, causing the lysosomal degradation in EGFR dependent glioblastoma in the GBM cell line U87MG [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:GBM cell line U87MG
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Concentration:5, 10, 20 µM
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Incubation Time:72 h
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Result:Was resistant to the mutant but the mutant retained its kinase activity, when DYRK1A-knockout clones were Rescued with the DYRK1A wild-type and the F238L-M240R double mutant[1].
Dyrk1a-in-16 reduced neurosphere size and number only in the populations rescued with wild-type DYRK1A, but not in those expressing the F238L-M240R mutant[1].
Not decreased neurosphere proliferation, unlike the DYRK1A knockout clones in DYRK2 and DYRK3-knockout clones[1].
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Cell Line:GBM cell line U87MG
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Concentration:5 or 10 µM
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Incubation Time:24 h
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Result:Reduced invasion of U87MG cells in a dose-dependent manner[1].
Did not observe any significant reduction of invasion in cells rescued with the DYRK1A F238L-M240R mutant as opposed to rescue with DYRK1A wild type[1].
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Cell Line:GBM cell line U87MG
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Concentration:1 or 10 µM
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Incubation Time:20 h
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Result:Observed a reduction in total EGFR and ERK phosphorylation levels in U87MG DYRK1A-knockout cell lines.
Induced the accumulation of EGFR when lysosomal degradation was inhibited by BaFA1.
Increased EGFR degradation, a phenotype also observed in DYRK1A-knockout cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:U87MG or U87MG-DYRK1A KO cells (1 x 106) induced- NuJ nude mice[1]
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Dosage:2 mg/kg
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Administration:i.p., daily for 30 days
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Result:Observed the tumors substantially smaller.
Failed to develop any tumors in the the DYRK1A-knockout line cohort.
Had markedly lower EGFR levels.
Chemical Information
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CAS No. 2805339-74-4
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Molecular Weight 303.29
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Formula C14H9NO5S
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SMILES
OC1=C(O)C=C(SC(C(C2=CC=C(O)C(O)=C2)=O)=N3)C3=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)
Dyrk1A-IN-16 Related Classifications
HY-179600 Related Classifications
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