A cell permeable, orally bioavailable imidazol-[4,5-b]pyridine derivative that enhances nuclear localization of transcriptional co-activator with PDZ-binding motif (TAZ) in a dose-dependent manner without affecting the total amount of TAZ in pluripotent C3H10T1/2 cells. Does not affect Ser89 phosphorylation in TAZ, but reduces tyrosine phosphorylation. Reduces PPARg levels in differentiated adipocytes and acts as a suppressor of PPARg-dependent adipocyte differentiation. Also shown to enhance RUNX2-induced osteoblast differentiation of C3H10T1/2 cells and mineralization in a dose-dependent manner. Reduces weight gain in ob/ob mice (50 mg/kg, i.p.) and attenuates bone loss in ovariectomized mice. Displays desirable pharmacokinetic properties with t1/2 = 9.85 h.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
A cell permeable, orally bioavailable imidazol-pyrimidine derivative that enhances nuclear localization of transcriptional co-activator with PDZ-binding motif (TAZ) in a dose-dependent manner without affecting the total amount of TAZ in pluripotent C3H10T1/2 cells. Does not affect Ser89 phosphorylation in TAZ, but reduces tyrosine phosphorylation. Reduces PPARg levels in differentiated adipocytes and acts as a suppressor of PPARg-dependent adipocyte differentiation. Also shown to enhance RUNX2-induced osteoblast differentiation of C3H10T1/2 cells and mineralization in a dose-dependent manner. Reduces weight gain in ob/ob mice (50 mg/kg, i.p.) and attenuates bone loss in ovariectomized mice. Displays desirable pharmacokinetic properties with t1/2 = 9.85 h.
A cell-permeable enhancer of nuclear localization of transcriptional co-activator with PDZ-binding motif (TAZ). Does not affect the total amount of TAZ in pluripotent C3H10T1/2 cells.
Biochem/physiol Actions
Cell permeable: yes
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Jang, E.J., et al. 2012. Br. J. Pharmacol.165, 1584.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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