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

GSK143 dihydrochloride 

Cat. No.: HY-12736A
Handling Instructions

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). GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.

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GSK143 dihydrochloride Chemical Structure

GSK143 dihydrochloride Chemical Structure

CAS No. : 2341796-81-2

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Description

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].

IC50 & Target

pIC50: 7.5 (SYK) and 7.1 (pErk)[1]

In Vitro

GSK143 dihydrochloride (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 dihydrochloride (10-10000 nM; every 24 hours for 3 days) has an IC50 of 323 nM in CLL cells. GSK 143 dihydrochloride (1 μM; 30 mins) abrogates early signalling events including SYK phosphorylation and calcium flux[2].
GSK143 dihydrochloride (0.1-10 μM; for 30 min) reduces cytokine expression in bone marrow derived macrophages in a concentration-dependent manner[3].

Cell Viability Assay[2]

Cell Line: Chronic lymphocytic leukaemia (CLL) cells
Concentration: 10, 100, 1000, 10000 nM
Incubation Time: Every 24 hours 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].

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

415.32

Formula

C₁₇H₂₄Cl₂N₆O₂

CAS No.

2341796-81-2

SMILES

[H]Cl.[H]Cl.O=C(C1=CN=C(N[[email protected]]2[[email protected]@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.

References
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Keywords:

GSK143GSK 143GSK-143SykPERKSpleen tyrosine kinaseProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseorallyspleentyrosinekinasephosphorylatedinflammationZAP-70LCKLYNJAK1JAK2JAK3AuroraBhWBhERGCLLInhibitorinhibitorinhibit

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GSK143 dihydrochloride
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HY-12736A
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