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IBS008738

Names

[ CAS No. ]:
385425-03-6

[ Name ]:
IBS008738

Biological Activity

[Description]:

IBS008738 is a potent TAZ activator. IBS008738 stabilizes TAZ, increases the unphosphorylated TAZ level, enhances the association of MyoD with the myogenin promoter, upregulates MyoD-dependent gene transcription, and competes with myostatin in C2C12 cells. IBS008738 enhances myogenesis in C2C12 cells and facilitates muscle repair in a muscle injury model[1][2].

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Inflammation/Immunology

[Target]

TAZ[1]


[In Vitro]

IBS008738 (0, 24, 48, 72 h) enhances TAZ expression, with a peak at 24 h[1]. IBS008738 (10 μM; 0, 24, 72 h) enhances mRNAs of myogenic markers but not of myofusion markers[1]. IBS008738 (10 μM; 24h) enhances mRNAs of IL-10 in C2C12 cells[2]. Western Blot Analysis[1] Cell Line: C2C12 cells Concentration: Incubation Time: Treated for 0, 24, 48, 72 h under differentiation conditions after 24 h under growth conditions. Result: Enhanced TAZ expression, with a peak at 24 h. RT-PCR[1] Cell Line: C2C12 cells Concentration: 10 μM Incubation Time: 0, 24, 72 h under differentiation Result: Enhanced mRNAs of myogenic markers but not of myofusion markers.

[In Vivo]

IBS008738 (3 nmol) facilitates muscle repair in Cardiotoxin-injected muscles[1]. IBS008738 (30 μM, 100 μL) prevents Dexamethasone-induced muscle atrophy[1]. IBS008738 (100-μL volume of 30 μM; intramuscular injection; immediately and on day 2 after TBI) diminishes the expression of TNF α and IL-6 but increases that of IL-10 mRNAs in muscles of traumatic brain injury (TBI)[2]. Animal Model: Six-week-old female BALB/cByJ mice[1] Dosage: 3 nmol (0.3 μL of 10 mM IBS008738 was diluted in 100 μL of PBS) Administration: Injected into the tibialis anterior (TA) muscle of mice under anesthesia. Result: Facilitated muscle repair in Cardiotoxin-injected muscles. Animal Model: Six-week-old female BALB/cByJ mice[1] Dosage: 30 μM (100 μL) Administration: Injected into the tibialis anterior (TA) and gastrocnemius (GM) muscles on days 9, 11, and 13. Result: Prevented Dexamethasone-induced muscle atrophy.

[References]

[1]. Yang Z, et al. Screening with a novel cell-based assay for TAZ activators identifies a compound that enhances myogenesis in C2C12 cells and facilitates muscle repair in a muscle injury model. Mol Cell Biol. 2014;34(9):1607-1621.

[2]. Zou R, et al. TAZ Activator Is Involved in IL-10-Mediated Muscle Responses in an Animal Model of Traumatic Brain Injury. Inflammation. 2017;40(1):100-105.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H22N4O2

[ Molecular Weight ]:
374.44


Related Compounds

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