Dyrk1A-IN-15
Dyrk1A-IN-15 is a selective, brain-penetrant and ATP-competitive Dyrk1A inhibitor with a IC50 of 19 nM. Dyrk1A-IN-15 displays high selectivity across a broad kinase panel (specific for DYRK kinases) with nanomolar potency. Dyrk1A-IN-15 impairs neurosphere self-renewal, cell invasion, and EGFR stability in vitro. Dyrk1A-IN-15 inhibits tumor growth and prolongs survival in vivo. Dyrk1A-IN-15 has potential for glioblastoma (GBM) research.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 1448757-02-5
- Formule: C14H9NO4S
- Masse moléculaire:287.29
-
Stockage:
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]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Voir tous les produits spécifiques à Isoform EGFR
More
Activité biologique
|
DYRK1A 19 nM (IC50) |
Dyrk1A-IN-15 (compound FC-2) (0-100 nM) is a reversible and ATP-competitive inhibitor, could be overcome at higher concentrations of ATP[1].
Dyrk1A-IN-15 (5-20 µM, 72 h) primarily targets at DYRK1A in the GBM cell line U87MG[1].
Dyrk1A-IN-15 (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-15 (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.
-
Cell Line:U87MG
-
Concentration:5, 10, 20 µM
-
Incubation Time:72 h
-
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].
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].
-
Cell Line:U87MG
-
Concentration:5 or 10 µM
-
Incubation Time:24 h
-
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].
-
Cell Line:U87MG
-
Concentration:1 or 10 µM
-
Incubation Time:20 h
-
Result:Observed a reduction in total EGFR and ERK phosphorylation levels in U87MG DYRK1A-knockout and U87MG 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.
-
Animal Model:U87MG or U87MG-DYRK1A KO cells (1 x 106) induced- NuJ nude mice[1]
-
Dosage:2 mg/kg
-
Administration:i.p., daily for 30 days
-
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
-
CAS No. 1448757-02-5
-
Masse moléculaire 287.29
-
Formule C14H9NO4S
-
SMILES
OC1=CC(C2=NC3=CC(OCO4)=C4C=C3S2)=CC=C1O
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Dyrk1A-IN-15 Related Classifications
HY-179599 Related Classifications
Powered by Bioz