Mammalian DYRKs are a subfamily of mitogen-activated protein kinase-related protein kinases and are originally discovered on the basis of homology to the Saccharomyces cerevisiae Yak1 and Drosophila mini-brain kinases. DYRKs possess Ser/Thr phosphorylation activity as well as autophosphorylation activity on Tyr residue(s). Two isoforms of DYRK, DYRK1A and DYRK1B, co-immunoprecipitate with HAN11 when coexpressed in COS cells indicating that the proteins interact in mammalian cells. Co-expression of DYRK1A, DYRK1B, or DYRK2 with a series of glycogen synthase mutants with Ser/Ala substitutions at the phosphorylation sites in COS cells revealed that protein kinases cause phosphorylation of site 3a in glycogen synthase. Control of glycogen synthase by DYRK represents a novel mechanism, and a potentially novel pathway, for the regulation of glycogen synthesis.


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BT173

BT173 is a small molecule allosteric inhibitor of HIPK2-Smad3 interaction, specifically inhibits the TGF-β1/Smad3 pathway.BT173 disrupts HIPK2-Smad3 protein-protein interaction (PPI) without significant inhibition of HIPK2 kinase activity or inhibition of p53 activation.BT173 inhibits Smad3 phosphorylation in human kidney cells in vitro.BT173 significantly attenuated renal fibrosis development in the UUO mice, significantly decreased Smad3 phosphorylation and α-SMA expression in the UUO kidneys.Treatment of BT173 ameliorated kidney fibrosis in Tg26 mice.

  • CAS Number: 2232180-74-2
  • MF: C18H12BrN3O2
  • MW: 382.217
  • Catalog: DYRK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LDN-192960 hydrochloride

LDN-192960 hydrochloride is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively[1].

  • CAS Number: 2309172-48-1
  • MF: C18H22Cl2N2O2S
  • MW: 401.35
  • Catalog: Haspin Kinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DYRKs-IN-1

DYRKs-IN-1 (Example 183) is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 9 nM and 5 nM for DYRK1B and DYRK1A, respectively. DYRKs-IN-1 has antitumor activity[1][2].

  • CAS Number: 1387090-01-8
  • MF: C30H30ClN7O4
  • MW: 588.06
  • Catalog: DYRK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

JH-XIV-68-3

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[1].

  • CAS Number: 2426628-52-4
  • MF: C21H17F3N8O
  • MW: 454.41
  • Catalog: DYRK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TC-S 7004

Mirk-IN-1 is a potent inhibitor of Dyrk1B(Mirk kianse) and Dyrk1A with IC50 of 68±48 nM and 22±8 nM respectively.IC50 value: 68±48/22±8 nM (Dyrk1B/Dyrk1A) [1]Target: Dyrk inhibitorMirk-IN-1 had an EC50 of 1.9 ±0.2 mmol/L on SW620 cells. At a much higher concentration of 10 mmol/L in a kinase assay, Mirk-IN-1 inhibited the activities of DYRK1A, ABL, FLT3, and MARK1 by88%, 64%, 56%, and 73%, respectively [1]. Mirk-IN-1 was able to block tumor cells from undergoing reversible arrest in a quiescent G0 state and enable some cells to exit quiescence [2].

  • CAS Number: 1386979-55-0
  • MF: C23H17Cl2N5O4
  • MW: 498.318
  • Catalog: DYRK
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

INDY

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 Ki 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[1][2].

  • CAS Number: 1169755-45-6
  • MF: C12H13NO2S
  • MW: 235.30200
  • Catalog: DYRK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Woodtide

Woodtide is a substrate for the DYRK (DYRK) family of kinases whose sequence is based on that around the DYRK phosphorylation site in FKHR[1][2].

  • CAS Number: 634592-23-7
  • MF: C68H122N20O21S
  • MW: 1587.88
  • Catalog: DYRK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

FINDY

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[1].

  • CAS Number: 1507367-37-4
  • MF: C16H17NO2S2Si
  • MW: 347.53
  • Catalog: DYRK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A