TNP-470 (Synonyms: AGM-1470)

TNP-470 is a methionine aminopeptidase-2 inhibitor and also an angiogenesis inhibitor.

methionine aminopeptidase-2^[1], angiogenesis^[2]

No significant difference of apoptotic cell numbers is observed between cells treated with TNP-470 and the controls. The IC₅₀s of TNP-470 are 16.86±0.9 µg/mL, 3.16±0.6 µg/mL and 1.78±0.8 µg/mL for KKU-M213 cells at 24, 48 and 72 h, respectively. The results show that TNP-470 significantly reduces the number of migrated cells and invaded cells as compare with the vehicle treated group. TNP-470 decreases the migrated cells of KKU-M213 to 26% and of KKU-M214 to 11% (P<0.01). Similarly, TNP-470 also significantly affects cell invasion, the number of invaded cells is reduced to 25% in KKU-M213 (P<0.01) and to 15% in KKU-M214 (P<0.01). The relative expressions of MMP2, MMP9 and c-MYC in TNP-470 treated cells are significantly suppressed compare to the vehicle treated cells^[1].

Treatment with TNP-470 attenuates (P<0.05) liver lipid accumulation compare to high fat fed (HFF) mice. By day 5, TNP-470 treated mice consume significantly less grams of high fat food than vehicle treated HFF mice. By day 15 of treatment, TNP-470 mice are consuming an equivalent number of calories to that of chow fed mice, despite the provision of high fat diet. Treatment with TNP-470 increases (P<0.05) expression of adipose tissue LPL mRNA, compare to chow-fed and high-fat fed controls. TNP-470 decreases energy intake and increases energy expenditure^[2].

401.88

C₁₉H₂₈ClNO₆

129298-91-5

C[[email protected]]1([[email protected]@H](C/C=C(C)/C)O1)[[email protected]]([[email protected]@H]2OC)([H])[[email protected]]3(CC[[email protected]]2OC(NC(CCl)=O)=O)CO3

Room temperature in continental US; may vary elsewhere.

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

• [1]. Kidoikhammouan S, et al. TNP-470, a methionine aminopeptidase-2 inhibitor, inhibits cell proliferation, migration and invasion of human cholangiocarcinoma cells in vitro. Asian Pac J Cancer Prev. 2012;13 Suppl:155-60.

  [2]. White HM, et al. The angiogenic inhibitor TNP-470 decreases caloric intake and weight gain in high-fat fed mice. Obesity (Silver Spring). 2012 Oct;20(10):2003-9.