Compound name
MU1210
Protein family
Protein Kinase
Target name
DYRK2
Affinity biochemical (nM)
1309
Affinity on-target cellular (nM)
1700
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000008b
SMILES
CN1C=C(C2=NC3=C(OC=C3C4=CC(C5=CC=NC=C5)=CC=C4)C=C2)C=N1
InChIKey
HEAGNKNMQVIVMM-UHFFFAOYSA-N
NCBI gene ID
9149
UniProt ID
Q9Y463
Synonyms
MIRK
Mode of action
Inhibitor
Negative control
MU140
Affinity biochemical definition
IC50
Affinity biochemical assay type
Eurofins radiometric assay
Affinity Biochemical Source Knowledge
https://onlinelibrary.wiley.com/doi/10.1002/anie.201810312
Affinity biochemical relation
=
Affinity on-target cellular definition
Ki
Affinity on-target cellular assay type
NanoBRET assay (in HEK293T cells)
Affinity on-target cellular source knowledge
https://www.thesgc.org/chemical-probes/MU1210
Affinity on-target cellular relation
=
Selectivity platform
Eurofins kinase panel
Selectivity platform number of targets
210
Selectivity remarks
Screened at 1 µM, closest targets as % of activity: HIPK2 (99%), HIPK3 (94%), GSK3A (90%); Eurofins binding assay: IC50(HIPK1) = 187 nM, IC50(HIPK2) = 23 nM, IC50(CLK3) >3 µM; In-cellular potency (NanoBRET assay in HEK293T cells): Ki(HIPK2) >10 µM, Ki(HIPK4) = 5.41 µM
Selectivity Source Knowledge
https://onlinelibrary.wiley.com/doi/10.1002/anie.201810312