DYRK Inhibitor

DYRK3 Human Pre-designed siRNA Set A contains three designed siRNAs for DYRK3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Haspin-IN-2 (compound 4) is a potent and selective haspin inhibitor with an IC₅₀ of 50 nM. Haspin-IN-1 also inbibits CLK1 and DYRK1A with IC₅₀s of 445 nM and 917 nM, respectively.

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.

TSL2109 is an orally active and selective DYRK2 and CDK4/6 inhibitor with an IC₅₀ value of 22 nM for DYRK2. TSL2109 exhibits high kinase selectivity over 93%. TSL2109 arrests cell cycle and induces apoptosis in virto. TSL2109 effectively overcomes Enzalutamide (HY-70002) resistance by suppressing tumor growth in vivo and virto. TSL2109 also shows CDK4/6 inhibitor resistance.TSL2109 demonstrates safety profile. TSL2109 can be used for prostate cancer research and breast cancer^[1][2].

VS-II-173 is a pan-Pim kinase inhibitor with IC₅₀ values ​​of 0.07 μM and 0.02 μM for Pim1 and Pim3, respectively, and a residual activity of 46% for Pim2 at 1 μM. VS-II-173 also inhibits kinases such as HIPK2, PRK2, RSK1, DYRK1a and AMPK_α1, selectively inhibiting acute myeloid leukemia (AML) cells with significantly lower toxicity to non-malignant cells (EC₅₀ > 30 μM). VS-II-173 weakens the phosphorylation of substrates such as Stat5 (Y694), MDM2 (S166), Bad (S112), and 4E-BP1 (T37/46) by inhibiting Pim kinase-mediated signaling pathways, blocking pro-survival signals in AML cells and inducing apoptosis. VS-II-173 synergistically enhances anti-AML activity when combined with Daunorubicin (HY-13062A). VS-II-173 can be used in AML research, especially for AML with FLT3-ITD mutations and NPM1 mutations .

Dyrk1a Rat Pre-designed siRNA Set A contains three designed siRNAs for Dyrk1a gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

JH-XVII-10 is a potent, selective and orally active DYRK1A and DYRK1B inhibitor with IC₅₀s of 3 nM and 5 nM for DYRK1A and DYRK1B, respectively. JH-XVII-10 shows antitumor efficacy in neck squamous cell carcinoma (HNSCC) cell lines.

GSK3-IN-10 (Compound 4) is a multi-target inhibitor, that mainly targets GSK3α and GSK3β with IC₅₀ of 1.0 nM and 2.0 nM. GSK3-IN-10 inhibits the activation of β-catenin, promotes the neuronal survival, and exhibits a protective effect against endoplasmic reticulum stress.

Dyrk1A-IN-15 is a selective, brain-penetrant and ATP-competitive Dyrk1A inhibitor with a IC₅₀ of 19 nM. Dyrk1A-IN-15 displays high selectivity across a broad kinase panel (specific for DYRK kinases) with nanomolar potency. Dyrk1A-IN-15 impairs neurosphere self-renewal, cell invasion, and EGFR stability in vitro. Dyrk1A-IN-15 inhibits tumor growth and prolongs survival in vivo. Dyrk1A-IN-15 has potential for glioblastoma (GBM) research.

Dyrk1A/α-synuclein-IN-1 (Compound b1) is a dual Dyrk1A and α-synuclein aggregation inhibitor with IC₅₀ values of 177 nM and 10.5 µM, respectively. Dyrk1A/α-synuclein-IN-1 has high predictive CNS penetration and neuroprotective effect.

KuWal151 is a CLK1, CLK2 and CLK4 inhibitor with a high selectivity margin towards DYRK kinases. KuWal151 has potent antiproliferative activity in an array of cultured cancer cell lines.

Dyrk1a-in-7 (Compound 29) is a selective DYRK1A kinase inhibitor, and has good kinase selectivity for CLK1 kinase. The IC₅₀ value of DYRK1A is 28 nM. For CLK2, K_d is 17.5 nM. Dyrk1a-in-7 can be used in the research of cancer, type Ⅱ diabetes and neurological diseases.

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

Dyrk1A-IN-16 is a selective, brain-penetrant and ATP-competitive Dyrk1A inhibitor with a IC₅₀ of 53 nM. Dyrk1A-IN-16 displays high selectivity across a broad kinase panel (specific for DYRK kinases) with nanomolar potency. Dyrk1A-IN-16 impairs neurosphere self-renewal, cell invasion, and EGFR stability in vitro. Dyrk1A-IN-16 inhibits tumor growth and prolongs survival in vivo. Dyrk1A-IN-16 has potential for glioblastoma (GBM) research.

Dyrk1A-IN-1 is a triple inhibitor of Dyrk1A kinase activity (IC₅₀ = 119 nM) and the aggregation of tau and α-syn oligomers.

DYRK2-IN-1 (Compd 54) is an orally bioavailable DYRK2 inhibitor, with an IC₅₀ of 14 nM. DYRK2-IN-1 (Compd 54) can be used in the study of prostate cancer.

XRF-1021 is an orally active HIPK2 inhibitor (IC₅₀ = 0.18 μM). XRF-1021 reduces the expression of fibrotic markers in TGF-β1 stimulated NRK-49F and HK-2 cells, including Fibronectin, Collagen I and α-SMA. XRF-1021 blocks TGF-β, NF-κB, p53, Wnt/β-catenin, and Notch signaling. XRF-1021 reduces renal injury and fibrosis in vivo. XRF-1021 can be used for the research of chronic kidney disease.

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.

UNC9750 is an inositol phosphate multikinase (IPMK) inhibitor with IC₅₀ values ​​of 31.6 and 374 nM for IPMK and IP6K2, respectively.. UNC9750 inhibits cellular accumulation of InsP₅, the direct product of IPMK kinase activity, while having no effect on either InsP6 or InsP₇ levels. UNC9750 has ≥ 75% inhibition of four kinases (DAPK1, DYRK1B, PDGFR, and KDR). UNC9750 can be used for the study of glioblastoma.

DYRK2 ligand 2 is a curcumin analog and an inhibitor targeting DYRK2, which serves as a ligand for target protein for PROTAC against DYRK2. DYRK2 ligand 2 is applicable to studies related to PROTAC synthesis, such as for PROTAC DYRK2 degrader-2 (HY-186287).