| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
TAZ[1]
TAZ (Transcriptional coactivator with PDZ-binding motif), a downstream effector of the Hippo signaling pathway. TAZ is a transcriptional coactivator that shuttles between the cytoplasm and nucleus. When dephosphorylated, it translocates to the nucleus and binds to TEAD transcription factors, driving the expression of genes involved in cell proliferation, survival, and stemness. IBS008738 stabilizes TAZ by increasing the level of its active, unphosphorylated form. |
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| 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].
In C2C12 cells, treatment with IBS008738 enhances the expression of TAZ, with a peak effect observed at 24 hours. At a concentration of 10 microM, it enhances the mRNAs of myogenic markers (e.g., MyoD, myogenin) but does not affect myofusion markers. It upregulates MyoD-dependent gene transcription and promotes myogenesis. It also enhances mRNAs of IL-10 in C2C12 cells, indicating an anti-inflammatory effect. It competes with myostatin, a negative regulator of muscle growth. |
| 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].
In a muscle injury model, IBS008738 facilitates muscle repair. Specifically, it has been shown to promote muscle repair and inhibit muscle injury in a mouse model of sport-induced injury. In addition, it can prevent dexamethasone-induced muscle atrophy in mice, demonstrating its ability to counteract muscle-wasting conditions. These effects are mediated by the stabilization and activation of TAZ, which in turn drives the expression of myogenic genes. |
| Enzyme Assay |
The activity of IBS008738 as a TAZ activator can be confirmed in a cell-free binding assay using a fluorescence polarization (FP) or surface plasmon resonance (SPR) method. However, since TAZ is a coactivator that functions by protein-protein interaction, a direct binding assay is complex. Instead, a common approach is to assess its ability to disrupt the TAZ-TEAD interaction using a TR-FRET (Time-Resolved Fluorescence Resonance Energy Transfer) assay with purified proteins.
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| 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. A functional cellular assay for TAZ activation is a luciferase reporter gene assay. C2C12 cells are co-transfected with a TEAD-responsive luciferase reporter and a Renilla control plasmid. After 24 hours, cells are treated with IBS008738 at various concentrations (e.g., 0, 10, 20 microM). After an additional 24-48 hours, luciferase activity is measured. An increase in the reporter signal indicates that the compound is promoting the nuclear translocation and transcriptional activity of TAZ. |
| 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. The in vivo efficacy of IBS008738 is assessed in a cardiotoxin-induced muscle injury mouse model. Mice are given an intramuscular injection of cardiotoxin to cause localized muscle damage. IBS008738 (e.g., 30 microM, 100 microL) or vehicle is then administered locally, often via intramuscular injection, for several days. Muscle regeneration is evaluated by histology, muscle fiber size measurement, and the expression of myogenic markers. Another model is systemic administration to prevent dexamethasone-induced muscle atrophy. |
| ADME/Pharmacokinetics |
For in vivo studies, IBS008738 is typically dissolved in DMSO and then diluted in a suitable vehicle (e.g., PBS). In a reported mouse model, it was administered at a concentration of 30 microM and a volume of 100 microL, presumably via intramuscular injection. The compound has sufficient solubility in DMSO (45 mg/mL) to formulate for in vivo administration. More detailed ADME (absorption, distribution, metabolism, excretion) properties are not publicly available as it is a research tool.
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| Toxicity/Toxicokinetics |
Specific toxicity data for IBS008738 is not reported in the standard research product literature. However, in the described muscle injury and atrophy models, treatment did not result in any reported adverse effects or mortality at the administered doses, suggesting it is well-tolerated in the short term. It is not a drug, and comprehensive toxicological profiling would be required to assess its safety for potential therapeutic applications.
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| 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. |
| Additional Infomation |
IBS008738 is a research chemical that has been identified as a potent activator of TAZ. It stabilizes the TAZ protein, prevents its degradation, and promotes its active, unphosphorylated form, thereby enhancing its transcriptional activity. It has no known clinical status and is not approved for any therapeutic indication. It is used as a tool to investigate the role of TAZ in myogenesis, muscle repair, and as a potential treatment for muscle-wasting diseases like cachexia and sarcopenia.
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| Molecular Formula |
C22H22N4O2
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|---|---|
| Molecular Weight |
374.435684680939
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| Exact Mass |
374.174
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| CAS # |
385425-03-6
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| PubChem CID |
6160351
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.3
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
535
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC=C(C=C1)N2C=NC(=C2C(=O)C3=CC=CC=C3)/N=C/N4CCOCC4
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| InChi Key |
UCDKLMTYEDPEMY-HZHRSRAPSA-N
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| 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+
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| Chemical Name |
[3-(4-methylphenyl)-5-[(E)-morpholin-4-ylmethylideneamino]imidazol-4-yl]-phenylmethanone
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: 50 mg/mL (133.53 mM)
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| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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