DYRK
Dual specificity tyrosine phosphorylation regulated kinase; Dual specificity tyrosine regulated kinase
DYRKs (dual-specificity tyrosine-regulated kinases; dual-specificity tyrosine phosphorylation-regulated kinases) comprise a family of protein kinases within the CMGC group of the eukaryotic kinome. DYRKs contain five members in humans that are clustered into two classes based on their phylogenetic relationships: class I DYRKs, DYRK1A and DYRK1B and class II DYRKs, DYRK2, DYRK3, and DYRK4.
DYRK kinases are “dual specificity” kinases, as they can phosphorylate both tyrosine (Y) and serine/threonine (S/T) residues, although Y-phosphorylation is limited to their autophosphorylation activity. DYRK kinases phosphorylate a broad set of substrates that are involved in a wide range of cellular processes, and they are thought to fulfill essential biological functions both during development and in maintaining homeostasis during the adult life. Consequently, the aberrant regulation or expression of DYRK kinases has been associated with several human pathologies, including cancer.
DYRK Isoform Specific Products
All Product Categories
-
DYRK Related Products (123)
Related Products (123)
-
Antibodies (1)
-
DYRK Isoform Comparison
-
DYRKs-IN-1 hydrochloride
0 ImagesDYRKs-IN-1 hydrochloride 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 hydrochloride has antitumor activity.
-
LDN-209929 dihydrochloride
0 ImagesLDN-209929 dihydrochloride is a potent and selective haspin kinase inhibitor (IC50=55 nM) with180-fold selectivity verses DYRK2 (IC50=9.9 μM). LDN-209929 is a optimized analogue of LDN-192960 (HY-13455).
-
ZJCK-6-46
0 ImagesZJCK-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
0 ImagesKH-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 dimaleate
0 ImagesSynonyms: GFH009 dimaleate; JSH-009 dimaleate; SLS009 dimaleateTambiciclib (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
0 ImagesRD0392 (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)
0 ImagesSynonyms: Telepathine (Standard)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)
0 ImagesCat. No.: HY-N0737AGCAS No.: 442-51-3Synonyms: Telepathine (GMP)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-HT2A serotonin receptor, with an Ki of 397 nM.
-
Dyrk1a Mouse Pre-designed siRNA Set A
0 ImagesCat. No.: HY-RS04095Dyrk1a 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
0 ImagesDS12881479 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
0 ImagesCat. No.: HY-U00439CAS No.: 1365986-44-2Protein kinase inhibitor 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
-
DYRK2-IN-2
0 ImagesCat. No.: HY-402805CAS No.: 2416195-65-6DYRK2-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
0 ImagesCat. No.: HY-117608CAS No.: 1440251-53-5ML 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 hydrochloride
0 ImagesML 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.
-
DYRKs-IN-1
0 ImagesCat. No.: HY-128758CAS No.: 1387090-01-8DYRKs-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.
-
PROTAC DYRK2 degrader 1
0 ImagesCat. No.: HY-161597CAS No.: 3061366-76-2PROTAC DYRK2 degrader 1 is a DYRK2 PROTAC degrader with DC50 values of 1.607 μM (MDA-MB-231 cells) and 3.265 μM (HeLa cells), respectively. PROTAC DYRK2 degrader 1 induces DYRK2 degradation via the ubiquitin-proteasome system. It is applicable to the research of triple-negative breast cancer and cervical cancer.
-
AO-365/43472821
0 ImagesAO-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.
-
(R)-(+)-O-Demethylbuchenavianine
0 Images(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.
