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Merck
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주요 문서

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SML3355

Sigma-Aldrich

GSK626616

≥98% (HPLC)

동의어(들):

(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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모든 사진(1)

About This Item

실험식(Hill 표기법):
C18H10Cl2N4OS
CAS Number:
1025821-33-3
Molecular Weight:
401.27
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

100

분석

≥98% (HPLC)

양식

powder

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

−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-

생화학적/생리학적 작용

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.)

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

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시험 성적서(COA)

Lot/Batch Number
0000181254
0000181253
0000176214

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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
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