TNP

TNP is a competitive, reversible inhibitor of IP6K1 and IP3K, with IC50s of 0.55 μM and 10.2 μM for IP6K1 and IP3K, respectively. TNP competitively binds to the ATP binding site of IP6K, inhibits the generation of 5-IP7, and thus relieves the inhibition of 5-IP7 on the AKT signaling pathway. TNP can enhance insulin sensitivity and promote thermogenesis in adipose tissue. TNP cannot effectively pass through the blood-brain barrier and is mainly used in the study of obesity, type 2 diabetes, and metabolic syndrome. However, TNP also inhibits CYP3A4 and may need further optimization[1][2][3].

Product Specifications

CAS Number

[519178-28-0]

UNSPSC

12352005

Hazard Statement

H300, H319

Target

IPK Superfamily

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease; PI3K/Akt/mTOR

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/IP3K_Inhibitor.html

Purity

99.29

Solubility

DMSO : 37.5 mg/mL (ultrasonic)

Smiles

FC(C1=CC(CNC2=NC(NCC3=CC=C([N+]([O-])=O)C=C3)=C4N=CNC4=N2)=CC=C1)(F)F

Molecular Formula

C20H16F3N7O2

Molecular Weight

443.38

Precautions

H300, H319

References & Citations

[1]Chang YT, et al. Purine-based inhibitors of inositol-1,4,5-trisphosphate-3-kinase. Chembiochem. 2002 Sep 2;3 (9) :897-901.|[2]Ghoshal S, et al. TNP [N2- (m-Trifluorobenzyl), N6- (p-nitrobenzyl) purine] ameliorates diet induced obesity and insulin resistance via inhibition of the IP6K1 pathway. Mol Metab. 2016 Aug 21;5 (10) :903-917.|[3]Lee S, et al. TNP and its analogs: Modulation of IP6K and CYP3A4 inhibition. J Enzyme Inhib Med Chem. 2022 Dec;37 (1) :269-279.