Leucettinib-21 is a highly selective and potent dual inhibitor targeting both DYRK and CLK kinase families. It demonstrates nanomolar-level inhibitory activity, with IC50 values of 2.4 nM (DYRK1A), 6.7 nM (DYRK1B), 12 nM (CLK1), 33 nM (CLK2), and 5 nM (CLK4), respectively. This compound exhibits remarkable kinase selectivity, making it a valuable pharmacological tool for studying these kinase-mediated pathways.

GSK-626616 is a dual-specificity tyrosine-regulated kinase (DYRK3) inhibitor with an IC50 of 0.7 nM which is a potential therapy for the treatment of anemia.

DYRK2 inhibitor C17 is a potent, selective DYRK2 inhibitor with IC50 of 9 nM, weakly inhibits DYRK3 (IC50=68 nM), and does not inhibit DYRK1A/1B (IC50>2000 nM).C17 showed outstanding selectivity for the human kinome containing 467 other human kinases.C17 showed synergistic 4E-BP1 phosphorylation suppression combined with AKT and MEK inhibitors.C17 impeded the store-operated calcium entry process (ORAI1 channel).

YK-2-69 is a potent, hilghly selective inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 2 (DYRK2) with IC50 value of 9 nM, shows weak inhibition against DYRK1B (IC50=542 nM) and no activity against DYRK1A/3/4 (IC50>1,000 nM).

Y020-3945 is a selective dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitor with IC50 of 0.53 uM.

FC162 is a potent inhibitor of DYRK1A with IC50 of 11, 18, and 68 nM, against DYRK1A, CLK1, and GSK3, respectively.

INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC50s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a Ki value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells.

BT173 is a small molecule allosteric inhibitor of HIPK2-Smad3 interaction, specifically inhibits the TGF-β1/Smad3 pathway.BT173 disrupts HIPK2-Smad3 protein-protein interaction (PPI) without significant inhibition of HIPK2 kinase activity or inhibition of p53 activation.BT173 inhibits Smad3 phosphorylation in human kidney cells in vitro.BT173 significantly attenuated renal fibrosis development in the UUO mice, significantly decreased Smad3 phosphorylation and α-SMA expression in the UUO kidneys.Treatment of BT173 ameliorated kidney fibrosis in Tg26 mice.

GNF2133 is a selective DYRK1A inhibitor with an IC50 value of 6 nM.

JH-XVII-10 is a potent, selective and orally active DYRK1A and DYRK1B inhibitor with IC50s of 3 nM and 5 nM for DYRK1A and DYRK1B, respectively. JH-XVII-10 shows antitumor efficacy in neck squamous cell carcinoma (HNSCC) cell lines.

JH-XIV-68-3 is a selective macrocyclic inhibitor of DYRK1A/B. JH-XIV-68-3 displays selectivity for DYRK1A and close family member DYRK1B in biochemical and cellular assays. JH-XIV-68-3 demonstrates antitumor efficacy in head and neck squamous cell carcinoma (HNSCC) cell lines.

MU1787 is a potent, highly selective HIPK inhibitor with IC50 of 285/123/283 nM for HIPK1/2/3, repectively.MU1787 is highly selective across the kinome in a broad panel of 373 human kinases, does not inhibits HIPK4 at 10 uM.

LDN192960 (LDN 192960) is a highly potent and selective DYRK2 inhibitor with IC50 of 13 nM toward DYRK2 at 50 uM ATP.LDN192960 suppresses Thr25 RPT3 phosphorylation in a dose-dependent manner in HEK293T cells transiently overexpressing DYRK2-FLAG, with maximal effects at 1-10 uM.LDN192960 does not inhibit any of the 130+ kinases including other CMGC kinase family members that are closely related to the DYRKs.LDN192960 binds to the ATP-binding pocket of DYRK2, also potently inhibits DYRK1A, DYRK3 and Pim with IC50 of <3, 122 and 10 nM, respectively.LDN192960 perturbs proteasome activity, induces cell death, and impedes proliferation and invasion on MDA-MB-468 cells.LDN192960 impedes MM progression and delays myeloma-mediated bone degeneration.LDN192960 induces cytotoxicity in bortezomib-resistant MM, both in cells and in vivo. significantly alleviates tumor burden in standard and PDX TNBC models.

JWD-065 is a potent small molecule HIPK2 kinase inhibitor, blocks HIPK2 phosphorylation on S359/T360 and JNK activation in HEK293 cells and attenuates ER stress-induced cell death with EC50 of 641 nM.

AZ191 is a potent and selective DYRK1B inhibitor with IC50 of 17 nM, about 5- and 110-fold selectivity over DYRK1A and DYRK2, respectively.

Dyrk1A-IN-1 is a triple inhibitor of Dyrk1A kinase activity (IC50 = 119 nM) and the aggregation of tau and α-syn oligomers.

DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe.

DYRKs-IN-1 hydrochloride is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 hydrochloride has antitumor activity.

tBID is a selective inhibitor of homeodomain–interacting protein kinase 2 (HIPK2) with an IC50 of  0.33 µM.