DYRK1

DYRK1 Related Products (60):

By Type:	Pan (23) Selective (10)

Cat. No.	Product Name	Effect	Purity

HY-N0737A

Harmine	Inhibitor	99.97%
Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT_2A serotonin receptor, with an K_i of 397 nM.

HY-12277

AZ191	Inhibitor	99.98%
AZ191 is a potent inhibitor that selectively inhibits DYRK1B with IC₅₀ of 17 nM.

HY-142295

GNF2133	Inhibitor	99.67%
GNF2133 is a potent, selective and orally active DYRK1A inhibitor with IC₅₀s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively. GNF2133 shows good proliferation potency and efficacy on rat and human primary β-cell. GNF2133 significantly improves glucose disposal capacity and increases insulin secretion. GNF2133 has the potential for the research of type 1 diabetes.

HY-N0737

Harmine hydrochloride	Inhibitor	99.98%
Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT_2A serotonin receptor, with an K_i of 397 nM.

HY-129492

GNF4877	Inhibitor	99.82%
GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC₅₀s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC₅₀ of 0.66 μM for mouse β (R7T1) cells).

HY-402805

DYRK2-IN-2	Inhibitor
DYRK2-IN-2 (Compound C17) is a selective inhibitor of DYRK2, with its IC₅₀ value being 40.3 nM. The inhibitory activity of DYRK2-IN-2 on DYRK1A (IC₅₀ = 1842 nM), DYRK1B (IC₅₀ = 1335 nM), DYRK4 (IC₅₀ = 1931 nM), DYRK3 (IC₅₀ = 112 nM), and CLKs (IC₅₀ = 540-6496 NM) is relatively low. DYRK2-IN-2 inhibits the phosphorylation of Tau protein at Thr212 and shows moderate cytotoxicity in HT22 cells. DYRK2-IN-2 can be used in cancer research.

HY-179177

AO-365/43472821	Inhibitor
AO-365/43472821 is a selective, brain-penetrant Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitor (IC₅₀ = 0.29 μM) and shows a significant inhibitory effect on (CDC-like kinase 1) CLK1 (IC₅₀ = 0.08 μM). AO-365/43472821 could protect the human neuroblastoma cell line SH-SY5Y from Okadaic acid (HY-N6785) (OA)-induced injury. AO-365/43472821 decreased tau (pSer396)/tau and Aβ1-42 protein expression. AO-365/43472821 can be used for the study of Alzheimer's disease.

HY-N17356

Atalaphyllidine	Inhibitor
Atalaphyllidine is a natural product. Atalaphyllidine can be isolated from the stem bark of Glycosmis chlorosperma. Atalaphyllidine inhibits DYRK1A kinase activity with an IC₅₀ of 2.2 μM. Atalaphyllidine can be used in the research of neurodegenerative diseases.

HY-105309

GSK-626616	Inhibitor	99.88%
GSK-626616 is a potent, orally bioavailable inhibitor of DYRK3 (IC₅₀=0.7 nM). GSK-626616 inhibits other members of the DYRK family (e.g., DYRK1A and DYRK2) with similar potency, which is a potential therapy for the treatment of anemia.

HY-108476

INDY	Inhibitor	99.32%
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 K_i 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.

HY-112296

T025	Inhibitor	99.64%
T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with K_d values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC₅₀ values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research.

HY-15951

ML167	Inhibitor	98.62%
ML167 is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor with IC₅₀ of 136 nM, >10-fold selectivity for closely related kinases Clk1, Clk2, Clk3 and Dyrk1A/1B.

HY-U00439A

Protein kinase inhibitor 1 hydrochloride	Inhibitor	98.0%
Protein kinase inhibitor 1 hydrochloride is a potent HIPK2 inhibitor, with IC₅₀s of 136 and 74 nM for HIPK1 and HIPK2, and a K_d of 9.5 nM for HIPK2.

HY-117049

Leucettine L41	Inhibitor	98.98%
Leucettine L41 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs) and CDC-like kinases (CLKs). Leucettine L41 can also inhibit GSK-3 singnaling. Leucettine L41 can inhibit cell apoptosis and ROS production. Leucettine L41 can promote β-cell cell cycle progression, cell proliferation and increase insulin secretion. Leucettine L41 can be used for the researches of neurological disease and metabolic disease, such as Alzheimer’s disease (AD) and diabetes.

HY-132308

DYRK1-IN-1	Inhibitor	99.71%
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.

HY-12838

RO5454948	Inhibitor	99.53%
RO5454948 (Compound 9) is the inhibitor for Dyrk1B and Dyrk1A with IC₅₀ of 68 nM and 22 nM. RO5454948 exhibits cytotoxicity in cancer cell SW620 with EC₅₀ of 1.9 μM.

HY-146221

Dyrk1A-IN-5	Inhibitor	98.06%
Dyrk1A-IN-5 (Compound 5j) is a potent and selective DYRK1A inhibitor, with an IC₅₀ of 6 nM. yrk1A-IN-5 exhibits significant selectivity for DYRK1B (IC₅₀ = 600 nM) and CLK1 (IC₅₀ = 500 nM), but shows almost no inhibition of DYRK2 (IC₅₀ > 10 μM). Dyrk1A-IN-5 can be used for Down syndrome research.

HY-117391

AZ-Dyrk1B-33	Inhibitor	99.78%
AZ-Dyrk1B-33 is a potent and selective Dyrk1B kinase inhibitor, with an IC₅₀ of 7 nM.

HY-34222

7-Deazaguanine	Inhibitor	99.73%
7-Deazaguanine (Compound 1) is a highly selective, well-tolerated, brain-penetrant DYRK1A inhibitor. 7-Deazaguanine is promising for research of cancers and Down’s syndrome.

HY-147066

Dyrk1A-IN-4	Inhibitor	99.30%
Dyrk1A-IN-4 is a potent and orally active Dyrk1A inhibitor. Dyrk1A-IN-4 exhibits IC₅₀s against DYRK1A and DYRK2 of 2 nM and 6 nM. Dyrk1A-IN-4 exhibits the inhibition of the DYRK1A pSer520 autophosphorylation in U2OS cells with an IC₅₀ of 28 nM. Dyrk1A-IN-4 can be used for the studies of ovarian adenocarcinoma, neuroblastoma and cervical squamous cell carcinoma.

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