GSK143 (dihydrochloride)

GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC50=7.1) [1]. GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice[2][3].

Product Specifications

CAS Number

[2341796-81-2]

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-dihydrochloride.html

Concentration

10mM

Purity

99.37

Solubility

DMSO : ≥ 50 mg/mL|H2O : 100 mg/mL (ultrasonic)

Smiles

[H]Cl.[H]Cl.O=C(C1=CN=C(N[C@H]2[C@@H](N)COCC2)N=C1NC3=CC=C(C)C=C3)N

Molecular Formula

C17H24Cl2N6O2

Molecular Weight

415.32

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.