| Chemical Properties | Back Directory | [Boiling point ]
623.9±55.0 °C(Predicted) | [density ]
1.38±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 125 mg/mL (293.12 mM) | [form ]
Solid | [pka]
13.04±0.50(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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 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. |
| [storage]
Store at -20°C | [References]
[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. DOI:10.1371/journal.pone.0131071 |
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| Company Name: |
MedChemExpress
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| Tel: |
021-58955995 |
| Website: |
www.medchemexpress.com |
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