5.30959

TAZ Activity Modulator, TM-25659

• Synonym(s): TAZ Activity Modulator, TM-25659, TM25659, TM 25659
• Empirical Formula (Hill Notation): C₃₀H₂₈N₈
• CAS Number: 260553-97-7
• Molecular Weight: 500.60
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• 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

Description

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable