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Home - Products - Metabolic Enzyme/Protease - Phosphatase - GNF362

GNF362

CAS No. 1003019-41-7

GNF362( —— )

Catalog No. M32944 CAS No. 1003019-41-7

GNF362 is an orally available, selective and potent inhibitor of inositol trisphosphate 3'kinase B (ITPKB), inhibits Itpka and Itpkc, overcomes TMZ chemoresistance, and selectively deletes donor allogeneic reactive T-cells.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    GNF362
  • Note
    Research use only, not for human use.
  • Brief Description
    GNF362 is an orally available, selective and potent inhibitor of inositol trisphosphate 3'kinase B (ITPKB), inhibits Itpka and Itpkc, overcomes TMZ chemoresistance, and selectively deletes donor allogeneic reactive T-cells.
  • 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].
  • 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.GNF362 augments SOC responses following antigen receptor cross-linking, with an EC50 of 12 nM in primary B or T lymphocytes.
  • 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.Animal Model:A Lewis rat antigen-induced arthritis (rAIA) model 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.
  • Synonyms
    ——
  • Pathway
    Metabolic Enzyme/Protease
  • Target
    Phosphatase
  • Recptor
    Phosphatase
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1003019-41-7
  • Formula Weight
    426.44
  • Molecular Formula
    C22H21F3N6
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (234.50 mM; Ultrasonic )Ethanol : ≥ 50 mg/mL (117.25 mM)
  • SMILES
    C[C@@H]1CN(Cc2cn[nH]c2-c2ccc(cc2)C#N)CCN1c1ccc(cn1)C(F)(F)F
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Miller AT, et al. Conversion of antigen-specific effector/memory T cells into Foxp3-expressing Treg cells by inhibition of CDK8/19. Sci Immunol. 2019 Oct 25;4(40). pii: eaaw2707.?
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