GSK143

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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.

For research use only. We do not sell to patients.

GSK143 Chemical Structure

CAS No. : 1240390-27-5

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Other Forms of GSK143:

GSK143 dihydrochloride Get quote

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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].

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.

Cell Viability Assay^[2]

Cell Line:	Chronic lymphocytic leukaemia (CLL) cells
Concentration:	10, 100, 1000, 10000 nM
Incubation Time:	Every 24 h for 3 days
Result:	Had an IC₅₀ of 323 nM.

In Vivo

GSK143 (0.1-10 mg/kg; orally; 1.5 hours) reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis of 1 mg/kg^[3].
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 T_1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a V_ss of 4.1 L/kg in rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Wild type C57NL/BL6 mice, 10-12 weeks old^[3]
Dosage:	0.1, 1, 3, 10 mg/kg
Administration:	Orally; 1.5 hours before intestinal manipulation (IM)
Result:	Reduced inflammation and prevented recruitment of immune cells in the intestinal muscularis.

Animal Model:	Male CD rats (175-200 g)^[1]
Dosage:	1 mg/kg of iv; 3 mg/kg of po (Pharmacokinetic Analysis)
Administration:	IV or PO
Result:	Had a T_1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a V_ss of 4.1 L/kg.

Molecular Weight

342.40

Formula

C₁₇H₂₂N₆O₂

CAS No.

1240390-27-5

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

GSK143 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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