DYRK Inhibitor

HIPK2-IN-2 is an orally active and selective HIPK2 inhibitor with an IC₅₀ of 0.36 μM against HIPK2. HIPK2-IN-2 reduces HIPK2 protein expression levels. HIPK2-IN-2 inhibits the proliferation and migration of renal interstitial fibroblasts, alleviates renal tubular injury and collagen deposition, and suppresses TGF-β/Smad3-mediated profibrotic signaling pathways as well as TNF-α/NF-κB-mediated inflammatory signaling pathways in renal cells. HIPK2-IN-2 is used for the study of chronic kidney disease-associated renal fibrosis.

Dyrk1A/α-synuclein-IN-2 (Compound b20) is a dual Dyrk1A and α-synuclein aggregation inhibitor with an IC₅₀ of 7.8 µM for α-synuclein. Dyrk1A/α-synuclein-IN-2 has high predictive CNS penetration and neuroprotective effect.

hAChE-IN-8 (Compound S-12) is a orally effective and selective inhibitor of hAChE (IC₅₀=0.486 μM). hAChE-IN-8 also inhibits BACE-1 (IC₅₀=0.542 μM), and does not inhibit Dyrk1A (IC₅₀>10 μM). hAChE-IN-8 can reduce Aβ aggregation, has good blood-brain barrier penetration. hAChE-IN-8 is mainly used in Alzheimer's disease research.

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.

HIPK2-IN-1 is an orally active and selective HIPK2 inhibitor with an IC₅₀ of 0.56 μM. HIPK2-IN-1 exerts antifibrotic and anti-inflammatory activities. HIPK2-IN-1 binds to HIPK2, inhibits the downstream TGF‑β/Smad3, p53, and TNF‑α/NF‑κB signaling pathways, reduces the expression of fibrotic markers, suppresses cell proliferation and migration, and alleviates renal tubular injury and collagen deposition. HIPK2-IN-1 is used for the study of renal fibrosis associated with chronic kidney disease.

MU1787 is a highly selective homeodomain-interacting protein kinase (HIPK) inhibitor with a furopyridine core, and shows improved selectivity against CLKs, with inactivity against DYRK1B, DYRK2, and MLK2/3 in in vitro cellular assays. MU1787 can be used for the research of malignancies.

JH-XIV-68-3 is a selective macrocyclic inhibitor of DYRK1A/B. JH-XIV-68-3 displays selectivity for DYRK1A and close family member DYRK1B in biochemical and cellular assays. JH-XIV-68-3 demonstrates antitumor efficacy in head and neck squamous cell carcinoma (HNSCC) cell lines.

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.

BI-5521 is an orally active GSK-3 inhibitor with an IC₅₀ of 1.1 nM against GSK-3β. BI-5521 targets the two GSK-3 isoforms with similar potency and exhibits potent inhibitory activity against DYRK1A. By modulating GSK-3 activity, BI-5521 inhibits tumor proliferation and cancer cell growth, exerts cytotoxic effects, and reduces cancer cell viability. It shows consistent chemosensitivity across all subtypes of rhabdomyosarcoma, produces synergistic growth inhibitory effects when combined with SOS1 inhibitors, reduces oral glucose levels, regulates the myofibroblast differentiation pathway, decreases the nuclear localization of YAP/SMAD2/3, and lowers the positive rate of α-SMA in fibroblasts without affecting the apoptosis of CD4⁺ T cells. BI-5521 can be used in the research of non-small cell lung cancer, pleomorphic rhabdomyosarcoma, type 2 diabetes, pancreatic ductal adenocarcinoma, Alzheimer's disease, bipolar disorder, and metabolic dysfunction-associated steatotic liver disease.

KTD-092 is a hit for DYRK1A inhibition, with an IC₅₀ of 22 nM for human DYRK1A. KTD-092 can be used in the research for Down syndrome (DS), Alzheimer's disease (AD), autism spectrum disorder (ASD), diabetes and other neurodegenerative diseases.

Dyrk1A-IN-8 (compound 4C) is a potent inhibitor of Dyrk1A , with the IC₅₀ of 209 nM. Dyrk1A-IN-8 plays an important role in neurodegenerative diseases.

Haspin-IN-1 (compound 2a) is a haspin inhibitor with an IC₅₀ of 119 nM. Haspin-IN-1 also inbibits CLK1 and DYRK1A with IC₅₀s of 221 nM and 916.3 nM, respectively.

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.

GNF7156 is a DYRK1A/GSK3B inhibitor, IC₅₀ values of 100 nM for DYRK1A and 40 nM for GSK3B. GNF7156 inhibits DYRK1A and GSK3B kinase activity and induces NFAT nuclear retention. GNF7156 stimulates beta-cell cycle entry and division and maintains insulin secretory capacity. GNF7156 can be used for the research of type 1 diabetes, and type 2 diabetes.