2. Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage
  3. Syk PERK
  4. GSK143

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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GSK143 Chemical Structure

GSK143 Chemical Structure

CAS No. : 1240390-27-5

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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.

GSK143 Related Antibodies

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 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.

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 T1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a Vss of 4.1 L/kg.
Molecular Weight

342.40

Formula

C17H22N6O2
CAS No.
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
References
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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.

Keywords:

GSK1431240390-27-5GSK 143GSK-143SykPERKSpleen tyrosine kinaseProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseorallyspleentyrosinekinasephosphorylatedinflammationZAP-70LCKLYNJAK1JAK2JAK3AuroraBhWBhERGCLLInhibitorinhibitorinhibit

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