dyrk2

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

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

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.

Abemaciclib methanesulfonate (LY2835219) is a specific and effective inhibitor of CDK4(IC50=2 nM) and CDK6(IC50=10 nM).

Abemaciclib (LY2835219) is a dual inhibitor of CDK4 6 (IC50=2 10 nM) with selectivity and specificity. Abemaciclib has antitumor activity and is used to treat advanced or metastatic breast cancer.

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.

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

LDN-192960 hydrochloride is an inhibitor of Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) and Haspin, with IC50 values of 48 nM and 10 nM, respectively.

Dyrk1A-IN-4 (compound 48) is a potent and orally active dual inhibitor of DYRK1A (IC50 = 2 nM) and DYRK2 (IC50 = 6 nM) with anticancer effects [1].

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

DMAT (Casein kinase II Inhibitor) is a potent and specific inhibitor of CK2(IC50 value of 130 nM).

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.

SGC-CK2-1 is a highly specific inhibitor of CK2, a inducer of insulin production and secretion in pancreatic β-cells, and can be used in the study of neurodegenerative diseases.

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.

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].

Leucettine L41 (LeucettineL41) is a selective DYRK1A inhibitor that inhibits DYRK2, CLK1, and CLK3, inducing autophagy linked to CLK inhibition. It is used to study Alzheimer's disease and memory deficits.

LDN-209929 dihydrochloride is a potent and selective inhibitor of haspin kinase (IC50= 55 nM), demonstrating 180-fold selectivity versus DYRK2 (IC50= 9.9 μM).

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.

MU1210 (compound 12f) acts as an inhibitor of CDC-like kinases Clk1, Clk2, and Clk4 with IC50 values of 8, 20, and 12 nM, respectively, and exhibits IC50 values of 187 and 1309 nM for HIPK1 and DYRK2. Additionally, MU1210 demonstrates favorable pharmacokinetic properties in mice (10 mg kg, intraperitoneal injection: Cmax=1.24 μM, T1 2=58 minutes; no acute toxicity observed).

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.

AZD2858 is a selective GSK-3 inhibitor, inhibiting tau phosphorylation at the S396 site and activating Wnt signaling pathway.