An ITPK inhibitor
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GNF-362

Item No. 35866

Technical Information
Formal Name
4-[4-[[(3R)-3-methyl-4-[5-(trifluoromethyl)-2-pyridinyl]-1-piperazinyl]methyl]-1H-pyrazol-3-yl]-benzonitrile
CAS Number
1003019-41-7
Molecular Formula
C22H21F3N6
Formula Weight
Purity
≥98%
A solid
DMSO: SolubleEthanol: SolubleMethanol: Soluble
SMILES
N#CC(C=C1)=CC=C1C2=NNC=C2CN3C[C@H](N(C4=CC=C(C=N4)C(F)(F)F)CC3)C
InChi Code
InChI=1S/C22H21F3N6/c1-15-13-30(8-9-31(15)20-7-6-19(12-27-20)22(23,24)25)14-18-11-28-29-21(18)17-4-2-16(10-26)3-5-17/h2-7,11-12,15H,8-9,13-14H2,1H3,(H,28,29)/t15-/m1/s1
InChi Key
VNTCGXMLDSKOKN-OAHLLOKOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    GNF-362 is an inositol triphosphate 3 kinase (ITPK) inhibitor (IC50s = 20, 9, and 19 nM for ITPKA, ITPKB, and ITPKC, respectively).1 It induces calcium influx in isolated mouse splenocytes (EC50 = 12 nM). In vivo, GNF-362 (10 and 25 mg/kg) reduces the number of thymic CD4+ T cells in mice. It also reduces inflammatory cell infiltration, joint erosion, and proteoglycan loss, in a rat model of antigen-induced arthritis when administered at a dose of 20 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Miller, A.T., Dahlberg, C., Sandberg, M.L., et alInhibition of the inositol kinase Itpkb augments calcium signaling in lymphocytes and reveals a novel strategy to treat autoimmune disease. PLoS One 10(6), e0131071 (2015).