IBS008738 is a potent TAZ activator. IBS008738 stabilizes TAZ in C2C12 cells, increases unphosphorylated TAZ levels, enhances the binding of MyoD to the myogenin promoter, upregulates MyoD-dependent gene transcription, and competes with myostatin. IBS008738 enhances myogenesis in C2C12 cells and promotes muscle repair in a muscle injury model.

Physicochemical Properties

Molecular Formula	C22H22N4O2
Molecular Weight	374.435684680939
Exact Mass	374.174
CAS #	385425-03-6
PubChem CID	6160351
Appearance	Light yellow to yellow solid powder
LogP	3.3
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	5
Heavy Atom Count	28
Complexity	535
Defined Atom Stereocenter Count	0
SMILES	CC1=CC=C(C=C1)N2C=NC(=C2C(=O)C3=CC=CC=C3)/N=C/N4CCOCC4
InChi Key	UCDKLMTYEDPEMY-HZHRSRAPSA-N
InChi Code	InChI=1S/C22H22N4O2/c1-17-7-9-19(10-8-17)26-16-24-22(23-15-25-11-13-28-14-12-25)20(26)21(27)18-5-3-2-4-6-18/h2-10,15-16H,11-14H2,1H3/b23-15+
Chemical Name	[3-(4-methylphenyl)-5-[(E)-morpholin-4-ylmethylideneamino]imidazol-4-yl]-phenylmethanone
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	TAZ[1]
ln Vitro	TAZ expression is increased by IBS008738 (0, 24, 48, and 72 hours), peaking at 24 hours[1]. mRNAs in C2C12 cells are enhanced by IBS008738 (10 μM; 0, 24, 72 h) in terms of IL-10 mRNAs [2].
ln Vivo	When muscles are injected with cardiotoxin, IBS008738 (3 nmol) facilitates muscle regeneration[1]. Muscle atrophy brought on by dexamethasone is prevented by IBS008738 (30 μM, 100 μL)[1]. After traumatic brain injury (TBI), IBS008738 (30 μM in 100 μL volume; intramuscular injection; immediately and day 2 after TBI) decreases TNF alpha and IL-6 expression but enhances IL-10 mRNA expression in muscles[2].
Cell Assay	Western Blot Analysis[1] Cell Types: C2C12 cells Tested Concentrations: Incubation Duration:Treated for 0, 24, 48, 72 h under differentiation conditions after 24 h under growth conditions. Experimental Results: Enhanced TAZ expression, with a peak at 24 h. RT-PCR[1] Cell Types: C2C12 cells Tested Concentrations: 10 μM Incubation Duration: 0, 24, 72 h under differentiation Experimental Results: Enhanced mRNAs of myogenic markers but not of myofusion markers.
Animal Protocol	Animal/Disease Models: Sixweeks old female BALB/cByJ mice[1] Doses: 3 nmol (0.3 μL of 10 mM IBS008738 was diluted in 100 μL of PBS) Route of Administration: Injected into the tibialis anterior (TA) muscle of mice under anesthesia. Experimental Results: Facilitated muscle repair in Cardiotoxin-injected muscles. Animal/Disease Models: Sixweeks old female BALB/cByJ mice[1] Doses: 30 μM (100 μL) Route of Administration: Injected into the tibialis anterior (TA) and gastrocnemius (GM ) muscles on days 9, 11, and 13. Experimental Results: 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.

Solubility Data

Solubility (In Vitro)

DMSO: 50 mg/mL (133.53 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 1.25 mg/mL (3.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (3.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.6707 mL	13.3533 mL	26.7065 mL
	5 mM	0.5341 mL	2.6707 mL	5.3413 mL
	10 mM	0.2671 mL	1.3353 mL	2.6707 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.