DYRK Inhibitor

ZJCK-6-46 (32) is a potential and orally activeDYRK1A inhibitor (IC₅₀ = 0.68 nM) with high BBB permeability (CNS+). ZJCK-6-46 (32) reduces tau phosphorylation. ZJCK-6-46 (32) ameliorates cognitive dysfunction by obviously reducing the expression of phosphorylated tau and neuronal loss _{in vivo}.

KH-CB20, an E/Z mixture, is a potent and selective inhibitor of CLK1 and the closely related isoform CLK4, with an IC₅₀ of 16.5 nM for CLK1. KH-CB20 can also inhibit DYRK1A (IC₅₀=57.8 nM) and CLK3 (IC₅₀=488 nM).

Tambiciclib (GFH009, JSH-009) dimaleate is an orally active, highly potent and selective CDK9 inhibitor (IC₅₀ = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over DYRK1A/B, and excellent selectivity over 468 kinases/mutants. Tambiciclib dimaleate demonstrates potent in vitro and in vivo antileukemic efficacy in acute myeloid leukemia (AML) mouse models by inhibiting RNA Pol II phosphorylation, downregulating MCL1 and MYC, and inducing apoptosis. Tambiciclib dimaleate can be used for AML research.

RD0392 (Compound 5) is a competitive tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitor (IC₅₀=1.3 nM). RD0392 is promising for research of neurodegenerative diseases like Alzheimer’s.

Harmine (Standard) is the analytical standard of Harmine. This product is intended for research and analytical applications. 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-HT2A serotonin receptor, with an Ki of 397 nM.

Harmine (GMP) (Telepathine (GMP)) is Harmine (HY-N0737A) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. 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.

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

DS12881479 is a selective non-ATP-competitive MNK1 inhibitor with an IC₅₀ value of 387 nM. DS12881479 stabilizes MNK1 in its autoinhibited DFD-out conformation, blocks eIF4E phosphorylation, suppresses tumor cell proliferation and induces weak apoptosis. DS12881479 also inhibits FLT3 and DYRK1a kinase activity at high concentrations. DS12881479 can be used for the research of cancer, such as leukemia.

Protein kinase inhibitor 1 is a novel inhibitor of HIPK2 with an IC₅₀ of 74 nM and K_d of 9.5 nM.

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.

ML 315 is a selective dual inhibitor of CDK and DYRK with IC₅₀s of 68 nM and 282 nM, respectively. ML 315 is used in cancer and neurological disease research.

ML 315 is a selective dual inhibitor of CDK and DYRK with IC₅₀s of 68 nM and 282 nM, respectively. ML 315 is used in cancer and neurological disease research.

Dyrk1A-IN-13 (Compound 1) is a DYRK1A inhibitor (IC₅₀: 41 nM). Dyrk1A-IN-13 reduces LPS-induced NO production and has antioxidant and anti-inflammatory activities. Dyrk1A-IN-13 can be used in the research of Alzheimer's disease, cancer and diabetes.

DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC₅₀s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 has antitumor activity.

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.

HTH-01-091 TFA is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC₅₀ of 10.5 nM. HTH-01-091 TFA also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 TFA can be uesd for breast cancer research.

(R)-(+)-O-Demethylbuchenavianine is an inhibitor for Cyclin-dependent kinases (CDK). (R)-(+)-O-Demethylbuchenavianine inhibits CDK1, CDK5, glycogen synthase kinase-3 (GSK3), cdc2-like kinase (CLK1) and dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A), with IC₅₀s of 1.1, 0.95, >10, >10 and >10 μM, respectively.

MBM-55S is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC₅₀ of 1 nM. MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC₅₀=5.4 nM) and DYRK1a (IC₅₀=6.5 nM). MBM-55S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice.

Dyrk1A/B-IN-1 (compound 3n) is a potent, selective and cell-permeable DYRK1A and DYRK1B inhibitor with K_is of 67.8 nM and 237.9 nM, and IC₅₀s of 1.1 μM and 0.8 μM, respectively. Dyrk1A/B-IN-1 is not toxic to human cells. Dyrk1A/B-IN-1 can be used for researching DYRK1A and DYRK1B cellular functions and their role in pathologies.

CSH-4044 can be isolated from fermented wheat germ extract. CSH-4044 is a unique benzothiazole compound. CSH-4044 can inhibit PIM3-driven BAD phosphorylation in pancreatic cancer cell lines as well as reducing DYRK1A-induced Tau phosphorylation in neuronal cells.