GSK143
Based on 1 publication(s) in Google Scholar
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). GSK143 reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.
At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (GSK143 dihydrochloride) usually boasts enhanced water solubility and stability.
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- CAS No.: 1240390-27-5
- Formule: C17H22N6O2
- Masse moléculaire:342.40
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Stockage:
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Other In-stock Forms of GSK143
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Activité biologique
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Chemical Information
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- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) GSK143
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Activité biologique
Description
IC50 & Target
pIC50: 7.5 (SYK) and 7.1 (pErk)[1]
In Vitro
GSK143 (compound 20) inhibits ZAP-70 (pIC50=4.7), LCK (pIC50=5.3), LYN (pIC50=5.4), JAK1/2/3 (pIC50=5.8/5.8/5.7), Aurora B (pIC50=4.8), hWB (pIC50=6.6), hERG (pIC50=4.7)[1].
GSK143 (10-10000 nM; every 24 h for 3 days) has an IC50 of 323 nM in CLL cells. GSK 143 (1 μM; 30 mins) abrogates early signalling events including SYK phosphorylation and calcium flux[2].
GSK143 (0.1-10 μM; for 30 min) reduces cytokine expression in bone marrow derived macrophages in a concentration-dependent manner[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Chronic lymphocytic leukaemia (CLL) cells
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Concentration:10, 100, 1000, 10000 nM
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Incubation Time:Every 24 h for 3 days
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Result:Had an IC50 of 323 nM.
In Vivo
GSK143 (3, 10, 30, 100 mg/kg; oral; 1 hour before ovalbumin challenge) reduces the cutaneous reverse passive Arthus reaction in a dose dependent manner by approximately 50% and 70% at 10 mg/kg and 30 mg/kg, respectively[2].
GSK143 (iv of 1 mg/kg; po of 3 mg/kg) has a T1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a Vss of 4.1 L/kg in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wild type C57NL/BL6 mice, 10-12 weeks old[3]
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Dosage:0.1, 1, 3, 10 mg/kg
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Administration:Orally; 1.5 hours before intestinal manipulation (IM)
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Result:Reduced inflammation and prevented recruitment of immune cells in the intestinal muscularis.
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Animal Model:Male CD rats (175-200 g)[1]
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Dosage:1 mg/kg of iv; 3 mg/kg of po (Pharmacokinetic Analysis)
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Administration:IV or PO
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Result:Had a T1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a Vss of 4.1 L/kg.
Chemical Information
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CAS No. 1240390-27-5
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Masse moléculaire 342.40
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Formule C17H22N6O2
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SMILES
O=C(C1=CN=C(N[C@H]2[C@@H](N)COCC2)N=C1NC3=CC=C(C)C=C3)N
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
Pureté et documentation
Références
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GSK143 Related Classifications
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