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| Targets |
The primary target of OAC2 is Oct4 (octamer-binding transcription factor 4). It acts as an activator of Oct4, promoting expression through the Oct4 gene promoter. Oct4 is a key regulator of embryonic stem cell pluripotency and is essential for the self-renewal of undifferentiated embryonic stem cells. By activating Oct4, OAC2 enhances iPSC reprogramming efficiency.
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| ln Vitro |
Octamer-binding transcription factor 4 (Oct4) is an essential player in the early phases of differentiation and a master regulator of the induction and maintenance of cellular pluripotency. It is the sole inducer of pluripotency that is irreplaceable by other proteins in the same family [1]. Oct4 is essential to the reprogramming process and has been demonstrated to be a significant regulator of embryonic stem cell (ESC) pluripotency. The structural analogue of OAC1 is OAC2. Similar to OAC1, OAC2 also activates the Oct4 and Nanog reporter genes. OAC1, its two structural analogs, OAC2 and OAC3, as well as Oct4, Sox2, Klf4, and c-Myc, four reprogramming factors[2].
In vitro, OAC2 activates expression through the Oct4 gene promoter. It enhances the efficiency of iPSC reprogramming and accelerates the reprogramming process. It is typically used in cell-based assays to study Oct4-mediated transcriptional regulation and reprogramming. Its activity is measured using reporter assays, such as Oct4-luc or Nanog-luc cells, treated with OAC2 at 1 µM or indicated concentrations. |
| ln Vivo |
In vivo, OAC2 is used to enhance reprogramming efficiency and accelerate the reprogramming process. Specific in vivo study protocols are not extensively detailed in the available literature, but its ability to activate Oct4 suggests potential applications in regenerative medicine and stem cell research.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for OAC2 are not typically performed, as it activates Oct4 expression through the gene promoter rather than binding directly to a receptor. Its activity is assessed in cell-based reporter assays using Oct4-luc or Nanog-luc cells. Cells are treated with OAC2, and luciferase activity is measured to quantify Oct4 promoter activation.
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| Cell Assay |
In vitro cellular assays for OAC2 are conducted in cell lines such as Oct4-luc or Nanog-luc reporter cells. Cells are treated with OAC2 at 1 µM or indicated concentrations, and luciferase activity is measured to assess Oct4 promoter activation. Its ability to enhance iPSC reprogramming efficiency is assessed in somatic cell reprogramming assays, where the number of iPSC colonies is counted following treatment with OAC2.
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| Animal Protocol |
In vivo animal studies for OAC2 are not extensively documented. As a research tool for stem cell biology, it may be used in animal models to study the role of Oct4 in development and regeneration. Its effects on Oct4 expression and cellular reprogramming in vivo could be assessed by measuring Oct4 levels in tissues or by evaluating the efficiency of in vivo reprogramming.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of OAC2 indicate it has a molecular weight of 236.27 and a molecular formula of C15H12N2O. It is soluble in DMSO at ≥ 2.4 mg/mL. The compound is typically stored as a powder at -20°C for up to 3 years. Its bioavailability and other PK parameters would be determined in preclinical studies for its use as a research tool.
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| Toxicity/Toxicokinetics |
Toxicological information for OAC2 is limited to its use as a research chemical. As an Oct4 activator, it may have effects on stem cell differentiation and pluripotency. Comprehensive toxicology studies would be required for its use in vivo, including assessments of its effects on development and cellular reprogramming.
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| References |
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| Additional Infomation |
OAC2 is a research compound used as an Oct4 activator to enhance iPSC reprogramming efficiency. It is also known as Oct4-activating compound 2. It activates expression through the Oct4 gene promoter. It is available from research chemical suppliers for stem cell research applications. It is not approved for clinical use.
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| Molecular Formula |
C15H12N2O
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| Molecular Weight |
236.274
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| Exact Mass |
236.094
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| Elemental Analysis |
C, 76.25; H, 5.12; N, 11.86; O, 6.77
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| CAS # |
6019-39-2
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| PubChem CID |
2814138
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| Appearance |
White to gray solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
364.3±15.0 °C at 760 mmHg
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| Flash Point |
174.1±20.4 °C
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| Vapour Pressure |
0.0±0.8 mmHg at 25°C
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| Index of Refraction |
1.743
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| LogP |
2.54
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
18
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| Complexity |
299
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C([H])=C([H])C([H])=C([H])C=1[H])N([H])C1C([H])=C([H])C2=C(C([H])=C([H])N2[H])C=1[H]
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| InChi Key |
JCAFGYWSIWYMOX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H12N2O/c18-15(11-4-2-1-3-5-11)17-13-6-7-14-12(10-13)8-9-16-14/h1-10,16H,(H,17,18)
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| Chemical Name |
N-(1H-indol-5-yl)benzamide
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| Synonyms |
OAC 2 OAC-2 Synonym
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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 : ≥ 100 mg/mL (~423.24 mM)
Ethanol : ~25 mg/mL (~105.81 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.58 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 25.0 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: 2.5 mg/mL (10.58 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), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (10.58 mM) (saturation unknown) in 10% EtOH + 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 25.0 mg/mL clear EtOH stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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 5: 2.5 mg/mL (10.58 mM) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH 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. Solubility in Formulation 6: ≥ 2.5 mg/mL (10.58 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (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 25.0 mg/mL clear EtOH stock solution to 900 μL of corn oil and mix evenly. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2324 mL | 21.1622 mL | 42.3245 mL | |
| 5 mM | 0.8465 mL | 4.2324 mL | 8.4649 mL | |
| 10 mM | 0.4232 mL | 2.1162 mL | 4.2324 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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