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DYRK

DYRK

DYRKs (dual-specificity tyrosine-regulated kinases; dual-specificity tyrosine phosphorylation-regulated kinases) comprise a family of protein kinases within the CMGC group of the eukaryotic kinome.Based on their phylogenetic relationships, DYRKs in humans have five members that are grouped into two classes: class I DYRKs, which include DYRK1A and DYRK1B, and class II DYRKs, which include DYRK2, DYRK3, and DYRK4.

Tyrosine (Y) and serine/threonine (S/T) residues can both be phosphorylated by DYRK kinases, though Y-phosphorylation is only possible through their autophosphorylation activity. DYRK kinases are believed to play crucial roles in maintaining homeostasis throughout adulthood and during development because they phosphorylate a wide variety of substrates involved in a wide range of cellular processes. As a result, several human pathologies, including cancer, have been linked to the aberrant regulation or expression of DYRK kinases.

DYRK related products

Structure Cat No. Product Name CAS No. Product Description
4-(Trifluoromethyl)aniline-d4 (4-Aminobenzotrifluoride-d4) V69711 4-(Trifluoromethyl)aniline-d4 (4-Aminobenzotrifluoride-d4) 1219795-48-8 4-(Trifluoromethyl)aniline-d4 is the deuterated form of 4-(Trifluoromethyl)aniline.
Aristolactam A IIIa (Aristolactam A IIIa; Sch 546909) V69712 Aristolactam A IIIa (Aristolactam A IIIa; Sch 546909) 97399-91-2 Aristolactam A IIIa (Sch 546909) is an aristolactam-type alkaloid extracted from Glycosmis chlorosperma.
Aristolactam BIII V69716 Aristolactam BIII 53948-10-0 Aristolactam BIII is a potent DYRK1A inhibitor that can suppress the kinase activity of DYRK1A in vitro (IC50=9.67 nM).
AZ191 V1954 AZ191 1594092-37-1 AZ191 is a potent and selective DYRK1B (Dual-specificity tyrosine phosphorylation-regulated kinase) inhibitor with IC50 of 17 nM in a cell-free assay, about 5- and 110-fold selectivity over DYRK1A and DYRK2, respectively.
BT173 V69717 BT173 2232180-74-2 BT173 is a potent homeodomain-interacting protein kinase 2 (HIPK2) inhibitor.
DYRK1-IN-1 V69705 DYRK1-IN-1 2814486-79-6 DYRK1-IN-1 is a selective and ligand-efficient DYRK1A inhibitor.
Dyrk1A-IN-1 V69715 Dyrk1A-IN-1 2858696-72-5 Dyrk1A-IN-1 is a tripartite inhibitor of Dyrk1Kinase activity (IC50 = 119 nM), aggregation of tau and α-syn oligomers.
Dyrk1A-IN-6 V84259 Dyrk1A-IN-6
Dyrk1A-IN-7 V88015 Dyrk1A-IN-7 Dyrk1A-IN-7 (Compound 29) is a selective DYRK1A kinase inhibitor with good kinase selectivity over CLK1 kinase, with an IC50 of 28 nM for DYRK1A and a Kd of 17.5 nM for CLK2.
Dyrk1A-IN-8 V88016 Dyrk1A-IN-8 101578-13-6 Dyrk1A-IN-8 (compound 4C) is a potent inhibitor of Dyrk1A with IC50 of 209 nM.
Dyrk1A-IN-9 V88018 Dyrk1A-IN-9 Dyrk1A-IN-9 (Compound L9) is a moderately active DYRK1A inhibitor (IC50: 1.67 μM).
Dyrk1A/α-synuclein-IN-1 V69719 Dyrk1A/α-synuclein-IN-1 2789711-47-1 Dyrk1A/α-synuclein-IN-1 (Compound b1) is a dual (bifunctional) inhibitor of Dyrk1A and α-synuclein aggregation with IC50s of 177 nM and 10.5 µM, respectively.
Dyrk1A/α-synuclein-IN-2 V69707 Dyrk1A/α-synuclein-IN-2 2789711-66-4 Dyrk1A/α-synuclein-IN-2 (Compound b20) is a dual (bifunctional) inhibitor of Dyrk1A and α-synuclein aggregation with IC50 of 7.8 µM for α-synuclein.
DYRK2-IN-1 V85608 DYRK2-IN-1
DYRKs-IN-1 hydrochloride V69710 DYRKs-IN-1 hydrochloride 1386980-55-7 DYRKs-IN-1 HCl is a potent inhibitor of DYRKs (dual-specificity tyrosine phosphorylation-regulated kinases) with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively.
EHT-1610 V20428 EHT-1610 1425945-60-3 EHT-1610 is a novel, potent and selective DYRK kinase inhibitor with IC50s of 0.22, 0.28 nM for DYRK1A and DYRK1B, respectively.
FINDY V69713 FINDY 1507367-37-4 FINDY is an intermediate-fold selective inhibitor of DYRK1A.
GNF2133 V69703 GNF2133 2561414-56-8 GNF2133 is a specific, orally bioactive DYRK1A inhibitor (antagonist) with IC50 of 0.0062 and >50 µM for DYRK1A and GSK3β, respectively.
GSK-626616 V21894 GSK-626616 1025821-33-3 GSK 626616 is a novel, potent, and orally bioavailable YAK3/DYRK3 kinase inhibitor with IC50of 0.7 nM for DYRK3.
ID-8 V1953 ID-8 147591-46-6 ID-8 is a novel and potent small molecule DYRK (Dual-specificity tyrosine phosphorylation-regulated kinase) inhibitor that sustains embryonic stem cell self-renewal in long-term culture.
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