Sigma-Aldrich Taz Activity Modulator Tm

Assay

≥97% (HPLC)

Quality Level

100

Form

powder

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
protect from light

Color

yellow

Solubility

DMSO: 50 mg/mL

Storage Temp.

2-8°C

Smiles String

CC1=NC2=C(N=C(CCCC)N2CC3=CC=C(C4=CC=CC=C4C5=NN=NN5)C=C3)C=C1C6=CN=CC=C6

General Description

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 t_1/2= 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.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany