T0070907 is a potent, selective, covalent PPARγ antagonist with binding IC50 of 1 nM, >800-fold preference for PPARγ over PPARα and PPARδ.
T0070907 specifically blocks PPARγ function in both cell-based reporter gene and adipocyte differentiation assays, with no effect on FXR, LXR, PR.
T0070907 modulates the interaction of PPARγ with cofactor proteins by affecting the conformation of helix 12 of the PPARγ ligand-binding domain (LBD).
T0070907 significantly more efficient at causing cancer cell death than the activators troglitazone and rosiglitazone.
Physicochemical Properties
M.Wt
277.6632
Formula
C12H8ClN3O3
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
Benzamide, 2-chloro-5-nitro-N-4-pyridinyl-
References
1. Lee G, et al. J Biol Chem. 2002 May 31;277(22):19649-57.
2. Schaefer KL, et al. Cancer Res. 2005 Mar 15;65(6):2251-9.
3. Masuda T, et al. Clin Cancer Res. 2005 Jun 1;11(11):4012-21.
4. Zaytseva YY et al. Anticancer Res. 2011, 31(3), 813-823.
