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| Targets |
Oct4 inducer-1 targets the Oct4 promoter, activating the expression of Oct4, a critical transcription factor for maintaining pluripotency. Oct4 is a member of the POU family of transcription factors and is essential for the self-renewal and pluripotency of embryonic stem cells. The compound also activates the Nanog promoter, another key pluripotency factor. By enhancing Oct4 and Nanog expression, Oct4 inducer-1 promotes the reprogramming of somatic cells to induced pluripotent stem cells. The molecular target of Oct4 inducer-1 may involve direct or indirect activation of Oct4 gene transcription, though the exact binding site and mechanism remain to be fully elucidated.
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| ln Vitro |
Oct4 inducer-1 (compound OAC-3; 1 μM) activates Oct4-luc reporter and Nanog-luc reporter in embryonic stem cells (ESCs) to increase reprogramming efficiency. Oct4 inducer-1 promotes the production of induced pluripotent stem cells (iPSCs) and quickens the development of colonies that resembleiPSCs[1]. Infected mouse embryonic fibroblasts (MEF) with Oct4 inducer-1 (1 μM) have been shown to increase reprogramming efficiency in iSF1 media[1].
In vitro studies have demonstrated that Oct4 inducer-1 (OAC-3) is a potent activator of Oct4 and Nanog expression. In embryonic stem cell-based reporter assays, Oct4 inducer-1 at 1 μM significantly activates the Oct4-luciferase reporter and the Nanog-luciferase reporter. The compound enhances the efficiency of iPSC generation by increasing the rate of reprogramming and shortening the time required for somatic cell reprogramming. Oct4 inducer-1 does not affect cell viability at effective concentrations and shows specificity for pluripotency gene activation. The compound has been used in various cell lines to study the molecular mechanisms of pluripotency maintenance and somatic cell reprogramming. |
| ln Vivo |
In vivo activity data for Oct4 inducer-1 itself is limited in publicly available literature, as the compound is primarily used as a research tool for in vitro stem cell studies. The compound's ability to activate Oct4 and Nanog has been demonstrated in cell-based systems, but comprehensive in vivo studies in animal models are not extensively reported. As a small molecule for stem cell research, the compound may be used in ex vivo cell reprogramming applications prior to transplantation, but its direct in vivo effects on pluripotency have not been thoroughly characterized. Future studies may explore its potential for in vivo regenerative medicine applications.
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| Enzyme Assay |
Cell-free biochemical assays for Oct4 inducer-1 are limited due to the compound's mechanism of action involving transcriptional regulation rather than direct enzyme inhibition. Standard characterization involves assessing the compound's purity and identity using HPLC and NMR spectroscopy. The compound is typically dissolved in DMSO for stock solutions. Binding studies to potential molecular targets may employ surface plasmon resonance or isothermal titration calorimetry if a specific target is identified. However, the primary assay format for this compound is cell-based reporter assays, as the compound's activity is measured through transcriptional activation rather than direct target binding.
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| Cell Assay |
Cellular assays for Oct4 inducer-1 typically use embryonic stem cells or somatic cells undergoing reprogramming. A standard protocol involves culturing mouse or human ESCs or iPSCs in appropriate media. For Oct4-luciferase reporter assays, cells are seeded in 96-well plates and treated with Oct4 inducer-1 at concentrations ranging from 0.1-10 μM for 24-48 hours. Luciferase activity is measured using a luciferase substrate and quantified with a luminometer. For reprogramming efficiency assays, somatic cells are transduced with Yamanaka factors and treated with Oct4 inducer-1, and iPSC colonies are counted after 2-3 weeks. Cell viability is assessed by MTT or CellTiter-Glo assays.
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| Animal Protocol |
In vivo studies involving Oct4 inducer-1 are not extensively reported in the literature. If conducted, a typical protocol might involve administration of the compound to mice to evaluate its effects on stem cell populations or tissue regeneration. The compound could be administered by intraperitoneal injection at various doses, with endpoints including assessment of Oct4 expression in tissues, analysis of stem cell markers, and evaluation of regenerative outcomes. However, the primary application of Oct4 inducer-1 remains in vitro cell reprogramming and stem cell research, and in vivo studies are limited.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Oct4 inducer-1 is not extensively available in the published literature, as the compound is primarily used as a research tool in cell-based studies rather than as a drug candidate. The compound's molecular weight and physicochemical properties would be expected to allow reasonable cell permeability, given its activity in cell-based assays. For studies involving systemic administration, standard PK parameters including oral bioavailability, half-life, and clearance would need to be determined empirically. The compound is typically dissolved in DMSO for in vitro studies.
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| Toxicity/Toxicokinetics |
Toxicological data specific to Oct4 inducer-1 is limited, as the compound is a research chemical used primarily in in vitro settings. In cell-based assays, the compound does not show significant cytotoxicity at effective concentrations (around 1 μM). Higher concentrations may have toxic effects depending on the cell type and exposure duration. For any in vivo applications, comprehensive toxicological evaluation would be required, including acute and repeat-dose toxicity studies. Standard laboratory safety precautions should be observed when handling this compound.
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| References | |
| Additional Infomation |
Oct4 inducer-1 (OAC-3) is a research compound and not an approved drug. No clinical trials or regulatory approvals exist for this compound. It is commercially available from various suppliers for research use only. The compound's primary value lies in its utility as a tool for stem cell research, particularly for enhancing iPSC generation efficiency. By activating Oct4 and Nanog promoters, Oct4 inducer-1 enables more efficient and faster reprogramming of somatic cells, facilitating studies on pluripotency, cell differentiation, and regenerative medicine. The compound is also used in anti-aging research.
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| Molecular Formula |
C15H11FN2O
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| Molecular Weight |
254.26
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| Exact Mass |
254.085
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| CAS # |
182564-41-6
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| PubChem CID |
2814506
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| Appearance |
Light brown to brown solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
374.9±22.0 °C at 760 mmHg
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| Flash Point |
180.5±22.3 °C
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| Vapour Pressure |
0.0±0.8 mmHg at 25°C
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| Index of Refraction |
1.721
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| LogP |
2.77
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
19
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| Complexity |
328
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1C(=O)NC2=CC3=C(C=C2)NC=C3)F
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| InChi Key |
RQJUZWRDCVBOMH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H11FN2O/c16-12-3-1-10(2-4-12)15(19)18-13-5-6-14-11(9-13)7-8-17-14/h1-9,17H,(H,18,19)
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| Chemical Name |
4-fluoro-N-(1H-indol-5-yl)benzamide
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: 250 mg/mL (983.25 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9330 mL | 19.6649 mL | 39.3298 mL | |
| 5 mM | 0.7866 mL | 3.9330 mL | 7.8660 mL | |
| 10 mM | 0.3933 mL | 1.9665 mL | 3.9330 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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