DYRK

Harmine (Telepathine) is an alkaloid isolated from seeds of Peganum harmala.

ML 315 is a selective Clk and DYRK inhibitor with potential anticancer activity for the study of neurological disorders.

YK-2-69 is a highly selective DYRK2 inhibitor with anti-prostate cancer effects.

ProINDY (Pro-indy) is a potent DYRK inhibitor that activates NFAT for the study of Down syndrome.

AnnH31 is a potent Dyrk1A inhibitor with an IC50 value of 81 nM.AnnH31 inhibits MAO-A with an IC50 of 3.2 μみゅーM.AnnH31 can be used as a probe to confirm the involvement of DYRK1A in cellular phosphorylation.

ARN25068 is a potent inhibitor of GSK-3βべーた, FYN, and DYRK1A protein kinases, exerting its activity in the sub-micromolar range. This compound effectively addresses tau hyperphosphorylation [1].

CK2/ERK8-IN-1 (TMCB) is a dual inhibitor of casein kinase 2 (CK2) (Ki: 0.25 µM) and ERK8 (IC50s: 0.50 μみゅーM) with pro-apoptotic efficacy. CK2/ERK8-IN-1 also binds to PIM1, DYRK1A, and HIPK2 (Kis: 8.65 µM, 11.9 µM, and 15.25 µM).

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.

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.

Clk1-in-3 is a + selective and highly potent sexual Clk1 inhibitor with an IC50 of 5 nM and 300 pairs higher affinity than Dyrk1A. CLK1-IN-3 also showed highly effective inhibition of Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 is effective in inducing autophagy in vitro and can be used for prevention and human treatment of acute liver injury (ALI).

GNF4877 is a potent inhibitor of DYRK1A and GSK3βべーた (IC50s: 6 nM and 16 nM, respectively), resulting in the blockade of nuclear export of nuclear factor of activated T-cells (NFATc) and increased βべーた-cell proliferation.

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.

LDN-192960 is a potent inhibitor of Haspin and DYRK2 (IC50s: 10 nM and 48 nM).

GNF2133 is an effective and selective inhibitor of DYRK1A with IC50s of 6.2 nM. GNF2133 can be used in studies about type 1 diabetes.

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

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

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.

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.

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.

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.

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.

ID-8, a DYRK inhibitor, sustains embryonic stem cell self-renewal in long-term culture.

Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.

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

7-bromoindirubin-3'-oxime (7BIO) is a caspase independent nonapoptotic cell death inducer. 7BIO is an inhibitor of FLT3, DYRK1A, DYRK2, Aurora B and Aurora C kinases.