DYRK Inhibitor

DYRK2 Human Pre-designed siRNA Set A contains three designed siRNAs for DYRK2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Aristolactam A IIIa (Sch 546909) is an aristolactam-type alkaloid that can be isolated from Glycosmis chlorosperma. Aristolactam A IIIa is a DYRK1A Inhibitor. Aristolactam A IIIa inhibits platelet aggregation induced by arachidonic acid (AA), collagen and platelet-activating factor (PAF). Aristolactam A IIIa has strong cytotoxic effect on HeLa cells.

DYRKs-IN-2 (Example 132) is a potent DYRKs inhibitor with IC₅₀s of 30.6 nM and 12.8 nM for DYRK1B and DYRK1A, respectively. DYRKs-IN-2 has antitumor activity.

AnnH31 is a Dyrk1A inhibitor (IC₅₀: 81 nM). AnnH31 also inhibits MAO-A with an IC₅₀ of 3.2 μM. AnnH31 inhibits cell viability of HeLa, PC12 and SH-SY5Y cells.

Dyrk2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Dyrk2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

Dyrk1A-IN-10 (compound B4) is a DYRK1A inhibitor with antidiabetic activity. Dyrk1A-IN-10 can promote pancreatic β-cell proliferation, increase insulin secretion, and lower blood sugar.

Dyrk3 Rat Pre-designed siRNA Set A contains three designed siRNAs for Dyrk3 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

DYRK1A Human Pre-designed siRNA Set A contains three designed siRNAs for DYRK1A gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Dyrk3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Dyrk3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

FINDY is a folding intermediate-selective inhibitor of DYRK1A. FINDY can inhibit Ser97 autophosphorylation with an IC₅₀ value of 35 μM. FINDY can be used for the research of neurological disorder. FINDY is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

tBID (Standard) is the analytical standard of tBID (HY-100464). This product is intended for research and analytical applications. tBID is a selective inhibitor of homeodomain-interacting protein kinase 2 (HIPK2) with an IC50 of 0.33 μM.

LDN-209929 dihydrochloride (Standard) is the analytical standard of LDN-209929 (dihydrochloride) (HY-110320). This product is intended for research and analytical applications. LDN-209929 dihydrochloride is a potent and selective haspin K_inase inhibitor (IC₅₀=55 nM) with180-fold selectivity verses DYRK2 (IC₅₀=9.9 μM). LDN-209929 is a optimized analogue of LDN-192960 (HY-13455).

INDY (Standard) is the analytical standard of INDY (HY-108476). This product is intended for research and analytical applications. 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.

GSK-626616 (Standard) is the analytical standard of GSK-626616 (HY-105309). This product is intended for research and analytical applications. 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.

Aristolactam BIII is a potent DYRK1A inhibitor and inhibits the kinase activity of DYRK1A in vitro (IC₅₀= 9.67 nM. Aristolactam BIII rescues the proliferative defects of DYRK1A transgenic (TG) mouse-derived fibroblasts and neurological and phenotypic defects of DS-like Drosophila models.

Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.

DYRKi is an inhibitor of DYRK1 and DYRK1B with IC₅₀ values of 3.7 µM and 90 nM, respectively, which is used as a potent antagonist of Hh/Gli signaling. DYRKi impairs SMO-dependent and SMO-independent oncogenic GLI activity in human medulloblastoma cells. DYRKi is promising for research of HH/GLI-associated cancers.

Dyrk1A-IN-9 (Compound L9) is a moderately active DYRK1A inhibitor (IC₅₀: 1.67 μM). L9 shows neuroprotective activity by regulating the expression of Aβ and phosphorylation of Tau protein. Dyrk1A-IN-9 can be used for research of Alzheimer's disease.

ProINDY, a prodrug of INDY (HY-108476), is a DYRK1A and DYRK1B inhibitor. ProINDY effectively recovers Xenopus embryos from head malformation induced by Dyrk1A overexpression.

Dyrk1A-IN-6 (compound 7cc) is an EGCG-like non-competitive inhibitor of DYRK1A. Dyrk1A-IN-6 can be used to alleviate cognitive defects in Down syndrome models.