GSK143

CAT: 0804-HY-12736Size: 1 EachDry Ice: NoHazardous: No
CAT#:0804-HY-12736Size:1 Each
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Description
GSK143 is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 inhibits phosphorylated Erk (pErk: pIC50=7.1) [1]. GSK143 reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice[2][3].
CAS Number
[1240390-27-5]
UNSPSC
12352005
Target
ERK; Syk
Type
Reference compound
Related Pathways
MAPK/ERK Pathway; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt
Applications
COVID-19-anti-virus
Field of Research
Cancer; Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/gsk143.html
Solubility
10 mM in DMSO
Smiles
O=C(C1=CN=C(N[C@H]2[C@@H](N)COCC2)N=C1NC3=CC=C(C)C=C3)N
Molecular Formula
C17H22N6O2
Molecular Weight
342.40
References & Citations
[1]John Liddle, et al. Discovery of GSK143, a Highly Potent, Selective and Orally Efficacious Spleen Tyrosine Kinase Inhibitor. Bioorg Med Chem Lett. 2011 Oct 15;21 (20) :6188-94.|[2]Abraham M Varghese, et al. Highly Selective SYK Inhibitor, GSK143, Abrogates Survival Signals in Chronic Lymphocytic Leukaemia. Br J Haematol. 2018 Sep;182 (6) :927-930.|[3]Sjoerd H W van Bree, et al. Inhibition of Spleen Tyrosine Kinase as Treatment of Postoperative Ileus. Gut. 2013 Nov;62 (11) :1581-90.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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