SML3355
GSK626616
≥98% (HPLC)
别名:
(5Z)-2-(2,6-Dichloroanilino)-5-(quinoxalin-6-ylmethylidene)-1,3-thiazolone, (5Z)-2-[(2,6-Dichlorophenyl)amino]-5-(6-quinoxalinylmethylene)-4(5H)-thiazolone, (5Z)-5-(6-Quinoxalinylmethylidene)-2-[(2,6-dichlorophenyl)amino]-1,3-thiazol-4(5H)-one, (Z)-2-(2,6-Dichlorophenylamino)-5-(quinoxalin-6-ylmethylene)thiazol-4(5H)-one, GSK 626616, GSK-626616
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关于此项目
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
SMILES string
ClC(C=CC=C1Cl)=C1NC2=NC(/C(S2)=C/C3=CC4=C(N=CC=N4)C=C3)=O
InChI
1S/C18H10Cl2N4OS/c19-11-2-1-3-12(20)16(11)23-18-24-17(25)15(26-18)9-10-4-5-13-14(8-10)22-7-6-21-13/h1-9H,(H,23,24,25)/b15-9-
InChI key
RJPNRXFBYZVRIB-DHDCSXOGSA-N
Biochem/physiol Actions
GSK626616 is an orally available, ATP-competitive, potent and selective dual-specificity tyrosine phosphorylation-regulated kinase DYRK inhibitor (DYRK3 IC50 = 0.7 nM; similar potency against DYRK1A and DYRK2) with 20-fold selectivity over the closed related casein kinase 2. GSK626616 enhances Epo-stimulated increase of human marrow erythroid colony formation units (CFU-E), without affecting megakaryocyte colony growth or CFU-GM formation. GSK626616 enhances the percentage and number of Ter119+/CD71+ erythroid progenitors derived from kit+ mouse marrow in the presence of SCF and Epo in cultures, and exhibits therapeutic efficacy in a murine anemia model in vivo (0.03 mg/kg/d i.p.)
Orally available, ATP-competitive, potent and selective dual-specificity tyrosine phosphorylation-regulated kinase DYRK1A/DYRK2/DYRK3 inhibitor in vitro and in vivo.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Kuglae Kim et al.
Journal of molecular biology, 430(10), 1521-1530 (2018-04-11)
Dual-specificity tyrosine-regulated kinases (DYRKs) auto-phosphorylate a critical tyrosine residue in their activation loop and phosphorylate their substrate on serine and threonine residues. The auto-phosphorylation occurs intramolecularly and is a one-off event. DYRK3 is selectively expressed at a high level in
Frank Wippich et al.
Cell, 152(4), 791-805 (2013-02-19)
Cytosolic compartmentalization through liquid-liquid unmixing, such as the formation of RNA granules, is involved in many cellular processes and might be used to regulate signal transduction. However, specific molecular mechanisms by which liquid-liquid unmixing and signal transduction are coupled remain
Zhentao Zhang et al.
Nature communications, 8, 14740-14740 (2017-03-28)
δ-secretase, also known as asparagine endopeptidase (AEP) or legumain, is a lysosomal cysteine protease that cleaves both amyloid precursor protein (APP) and tau, mediating the amyloid-β and tau pathology in Alzheimer's disease (AD). Here we report the therapeutic effect of
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| SML3355-5MG | 04065268342350 |
| SML3355-25MG | 04065268342343 |