dyrk1b

ML167 (CID44968231) is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor.

Harmine hydrochloride (telepathine hydrochloride) is extracted from Peganum Harmala Genus.

CLK-IN-T3 is an inhibitor of CLK1, CLK2, and CLK3 with IC50s of 0.67, 15, and 110 nM. CLK-IN-T3 exhibits anti-cancer activity.

AZ-Dyrk1B-33 (3-(2-Methyl-4-pyrimidinyl)-1-(phenylmethyl)-1H-pyrrolo[2,3-c]pyridine) is a potent and selective Dyrk1B kinase inhibitor with an IC50 of 7 nM.

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.

AZ191(IC50 of 17 nM) is an effective and specific DYRK1B inhibitor. The specificity of AZ191 for DYRK1B is about 5- and 110-fold greater over DYRK1A and DYRK2, respectively.

DYRKs-IN-2 has antitumor activity. DYRKs-IN-2 is a potent DYRKs inhibitor with IC50s of 30.6 nM and 12.8 nM for DYRK1B and DYRK1A, respectively.

Dyrk1A B-IN-1 (compound 3n) is a potent, selective, and cell-permeable inhibitor of DYRK1A and DYRK1B, with Kis of 67.8 nM and 237.9 nM, and IC 50 s of 1.1 μM and 0.8 μM, respectively.

Leucettinib-21 (LCTB-21) (compound 4) serves as a selective and potent inhibitor of DYRK1A, exhibiting IC50 values of 2.4, 6.7, 12, 33, and 5 nM for DYRK1A, DYRK1B, CLK1, CLK2, and CLK4, respectively. This compound is applicable for the study of Down syndrome and Alzheimer's disease [1].

Mirk-IN-1 is an effective inhibitor of Dyrk1B(Mirk kianse) and Dyrk1A (IC50: 68±48 nM and 22±8 nM respectively).

JH-XVII-10 is a selective, orally active and potent inhibitor of DYRK1A (IC50: 3 nM) and DYRK1B (IC50: 5 nM).JH-XVII-10 exhibits antitumor effects in squamous cell carcinoma of the neck (HNSCC) cell lines.

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.

JH-XIV-68-3 is a selective inhibitor of the DYRK1A B macrocycle, acting specifically on DYRK1A and DYRK1B in biochemical and cellular assays, and exhibiting antitumor effects in head and neck squamous cell carcinoma (HNSCC) cell lines.

ON 108600 is a chemical inhibitor targeting CK2 (Casein Kinase 2), TNIK, and DYRK1, demonstrating IC50 values of 0.016 μM and 0.007 μM for DYRK1A and DYRK1B, 0.028 μM for DYRK2, 0.05 μM and 0.005 μM for CK2α1 and CK2α2, and 0.005 μM for TNIK, respectively. This compound exhibits antitumor activity [1].

DYRKs-IN-1 hydrochloride is a potent inhibitor of Dual-specificity tyrosine-phosphorylation-regulated kinases (DYRKs), with IC50 values of 5 nM for DYRK1A and 8 nM for DYRK1B, and exhibits antitumor activity.

INDY is an ATP-competitive inhibitor of Dyrk1A and Dyrk1B with IC50s of 0.24 μM and 0.23 μM and a Ki of 0.18 μM for Dyrk1A ATP pocket, respectively.

DYRKs-IN-1 has antitumor activity. DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 9 nM and 5 nM for DYRK1B and DYRK1A, respectively.

DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor that inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. It exhibits good permeability and cellular activity without P-glycoprotein liability, making it suitable for research on central nervous system penetrant DYRK1A chemical probes [1].

Dyrk1A-IN-5 (compound 5j) is a highly potent and selective DYRK1A inhibitor with an IC50 of 6 nM, reducing the phosphorylation of Thr434 in SF3B1 dose-dependently (IC50 = 0.5 μM) and inhibiting tau phosphorylation at Thr212 (IC50 = 2.1 μM), making it valuable for Down syndrome research [1].

T025 is a pan CLK inhibitor with Kds of 4.8, 0.096, 6.5, 0.61, and 0.074 nM for CLK1-4, respectively. T025 displays anti-proliferative activities with IC50s of 30-300 nM in hematological and solid cancer cell lines. T025 can be used in studies about MYC-driven diseases.

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].

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.