dyrk3

EHT 1610 (EHT 5372) is a potent inhibitor of DYRK, with an IC50 of 0.36 nM and 0.59 nM for DYRK1A and DYRK1B, respectively. EHT 1610 has an inhibitory effect on leukemia, regulating cell cycle and inducing cell apoptosis.

GSK-626616 is a potent and orally bioavailable DYRK3 inhibitor (IC50: 0.7 nM). It inhibits other members of the DYRK family with similar potency. GSK-626616 is a potential therapy for the treatment of anemia.

HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor (IC50: 10.5 nM) that also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK, and CLK2. It can be used to study breast cancer.

TBB (NSC-231634)(NSC-231634) is a highly selective, ATP/GTP-competitive inhibitor of casein kinase-2 (CK2).

EHT 5372 is a potent and selective inhibitor of DYRK's family kinases. EHT 5372 shows IC 50 s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, 221 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, GSK-3β.

HTH-01-091 TFA, a potent and selective inhibitor of maternal embryonic leucine zipper kinase (MELK), exhibits an IC50 of 10.5 nM. Besides its primary target, it also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK, and CLK2, positioning it as a promising agent for breast cancer research [1].

Leucettinib-92 (compound 92) is a kinase inhibitor selective for the DYRK CLK families, with IC50 values of 147 nM for CLK1, 39 nM for CLK2, 5.2 nM for CLK4, 0.8 μM for CLK3, 124 nM for DYRK1A, 204 nM for DYRK1B, 0.16 μM for DYRK2, 1.0 μM for DYRK3, 0.52 μM for DYRK4, and 2.78 μM for GSK3 [1].

ZJCK-6-46 (32) is a potential orally active DYRK1A inhibitor (IC50= 0.68 nM) with favorable CNC permeability. It downregulates tau phosphorylation and improves cognitive impairments by significantly reducing the expression of phosphorylated tau proteins and neuronal loss.