1. Metabolic Enzyme/Protease
  2. Phosphatase
  3. GNF362

GNF362 

Cat. No.: HY-126750
Handling Instructions

GNF362 is a selective, potent, and orally bioavailable inhibitor of inositol trisphosphate 3’ kinase B (Itpkb) with an IC50 of 9 nM. GNF362 also inhibits Itpka and Itpkc with IC50 values of 20 nM and 19 nM, respectively. Inositol trisphosphate 3’ kinase B (Itpkb) is a Ca2+-dependent kinase, which phosphorylates the 3’ position of Ins (1,4,5) P3 to generate inositol 1,3,4,5-tetrakisphosphate [Ins (1,3,4,5) P4].

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

GNF362 Chemical Structure

GNF362 Chemical Structure

CAS No. : 1003019-41-7

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Description

GNF362 is a selective, potent, and orally bioavailable inhibitor of inositol trisphosphate 3’ kinase B (Itpkb) with an IC50 of 9 nM. GNF362 also inhibits Itpka and Itpkc with IC50 values of 20 nM and 19 nM, respectively. Inositol trisphosphate 3’ kinase B (Itpkb) is a Ca2+-dependent kinase, which phosphorylates the 3’ position of Ins (1,4,5) P3 to generate inositol 1,3,4,5-tetrakisphosphate [Ins (1,3,4,5) P4][1].

In Vitro

GNF362 (0-10 mM) blocks Ins (1,3,4,5) P4 production, enhances antigen receptor-driven Ca2+ responses and lead to apoptosis of activated T cells in an Itpkb-dependent manner in lymphocytes[1].
GNF362 augments SOC responses following antigen receptor cross-linking, with an EC50 of 12 nM in primary B or T lymphocytes[1].

In Vivo

GNF362 (orally administration; 6 or 20 mg/kg; twice daily; 21 days) shows minimal block in antibody production but shows significant inhibition of joint swelling at 6 mg/kg, reduces inflammatory cell infiltrate, joint damage, and proteoglycan loss at 20 mg/kg[1].

Animal Model: A Lewis rat antigen-induced arthritis (rAIA) model[1]
Dosage: 6 or 20 mg/kg
Administration: Orally administration; 6 or 20 mg/kg; twice daily; 21 days
Result: Reduced knee swelling in both the 20mg/kg and 6mg/kg treatment groups of GNF362 by 47% and 34%, respectively.
Molecular Weight

426.44

Formula

C₂₂H₂₁F₃N₆

CAS No.

1003019-41-7

SMILES

N#CC1=CC=C(C=C1)C2=C(C=NN2)CN3C[[email protected]](N(CC3)C4=NC=C(C=C4)C(F)(F)F)C

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Storage

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

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Keywords:

GNF362GNF 362GNF-362PhosphataseInhibitorinhibitorinhibit

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