Cart
sales@molnova.com
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)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 606 | Get Quote |
|
| 500MG | Get Quote | Get Quote |
|
| 1G | Get Quote | Get Quote |
|
Biological Information
-
Product NameGNF362
-
NoteResearch use only, not for human use.
-
Brief DescriptionGNF362 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.
-
DescriptionGNF362 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 VitroGNF362 (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 VivoGNF362 (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——
-
PathwayMetabolic Enzyme/Protease
-
TargetPhosphatase
-
RecptorPhosphatase
-
Research Area——
-
Indication——
Chemical Information
-
CAS Number1003019-41-7
-
Formula Weight426.44
-
Molecular FormulaC22H21F3N6
-
Purity>98% (HPLC)
-
SolubilityIn Vitro:?DMSO : 100 mg/mL (234.50 mM; Ultrasonic )Ethanol : ≥ 50 mg/mL (117.25 mM)
-
SMILESC[C@@H]1CN(Cc2cn[nH]c2-c2ccc(cc2)C#N)CCN1c1ccc(cn1)C(F)(F)F
-
Chemical Name——
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith 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.?
molnova catalog
related products
-
Talabostat mesylate
Talabostat mesylate is an orally active, selective inhibitor of dipeptidyl peptidases IV (DPP4, IC50: 0.18 nM), including tumor-associated fibroblast activation protein.
-
EWP 815
EWP 815 is a disulfiram analogue that functions as a powerful inhibitor of Ins(1,4) P 2 phosphatase, Ins(1,4,5) P 3 5-phosphatase, and dopamine β-hydroxylase activity .
-
JMS-053
JMS-053 is a potent and selective inhibitor of the phosphatase DUSP3, inhibits PTP4A3, PTP4A1, PTP4A2 and CDC25B, inhibits cancer cell migration and sphere growth, and avoids disruption of the microvascular endothelial barrier by vascular endothelial growth factor or lipopolysaccharide.
