| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Firefly luciferase[1]
Luciferase-IN-3 directly targets firefly luciferase, an ATP-dependent enzyme that catalyzes the oxidative decarboxylation of D-luciferin to produce oxyluciferin and emit light. The compound is believed to bind to the active site of the enzyme, interfering with the catalytic cycle and preventing the conversion of luciferin. The reported IC₅0 for firefly luciferase (P. pyralis) is approximately 3.2 microM. Notably, the compound shows no significant inhibitory potency against Renilla reniformis luciferase, demonstrating selectivity for the firefly enzyme. It does not target mammalian enzymes or receptors. |
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| ln Vitro |
In vitro, Luciferase-IN-3 is a potent inhibitor of firefly luciferase activity. The compound inhibits P. pyralis luciferase with an IC₅0 of 3.2 microM in standard cell-free enzyme assays. Under optimized assay conditions (e.g., with 1 uM D-luciferin, 2 mM ATP, and 10 mM MgCl2), the compound significantly reduces light output in a concentration-dependent manner, with near-complete inhibition observed at concentrations above 10-30 uM. Importantly, the inhibitory potency against Renilla luciferase is not significant, making it a selective tool for distinguishing between different luciferase-based reporters in dual-luciferase assays.
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| ln Vivo |
No in vivo activity has been reported for Luciferase-IN-3 as a therapeutic agent. The compound is a chemical probe used exclusively in in vitro assays and not intended for animal administration. It could theoretically be used in bioluminescence imaging studies as a control to validate that signal changes are due to genuine biological modulation rather than direct luciferase inhibition. In such applications, it would be used ex vivo or in cell lysates rather than administered systemically to living animals. No disease-modifying activity or in vivo efficacy studies have been published for this compound.
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| Enzyme Assay |
Cell-free enzyme inhibition assays are used to characterize Luciferase-IN-3. Recombinant firefly luciferase (1-10 ng/mL) is diluted in assay buffer (25 mM Tris-HCl pH 7.8, 2 mM EDTA, 10% glycerol, 1 mM DTT, 0.5 mM ATP, 0.5 mM MgCl2, 0.2 mM coenzyme A). Luciferase-IN-3 is dissolved in DMSO and serially diluted (0.01-100 uM, final DMSO ≤1%) in the same buffer. The reaction is initiated by adding D-luciferin (final concentration 50 uM). Luminescence is measured immediately using a luminometer. The IC₅0 is calculated from the dose-response curve. For Renilla luciferase, coelenterazine is used as the substrate, and the assay buffer is modified (no coenzyme A). This protocol is standard for luciferase inhibitor characterization.
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| Cell Assay |
For cell-based assays, cells (e.g., HEK293 or HeLa) are transiently co-transfected with a firefly luciferase reporter plasmid and a Renilla luciferase control plasmid (for normalization). After 24 hours, cells are treated with Luciferase-IN-3 at concentrations ranging from 0.1-50 uM for 2-4 hours. Cells are then lysed in passive lysis buffer, and luciferase activities are measured using a dual-luciferase assay kit. The IC₅0 for firefly luciferase inhibition in cells is typically higher than in cell-free assays (approximately 1-5 uM) due to cell permeability considerations. The compound is also used to test whether a test compound's effect on luminescence is due to direct luciferase inhibition: co-incubation of the test compound with Luciferase-IN-3 should not further reduce signal if the test compound is also a luciferase inhibitor.
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| Animal Protocol |
No animal experiments have been performed with Luciferase-IN-3 as a test article for efficacy. It is a research chemical and biochemical tool, not a therapeutic agent. If used in vivo, it would be in the context of acute, non-survival experiments for specific research purposes, such as optically validating bioluminescence signals in tissues. For such applications, the compound could be injected locally or systemically at doses of 1-20 mg/kg to rapidly reduce luciferase activity. However, this is not a standard protocol and such use is not well-documented in the literature. For all practical purposes, no standard animal experiments exist for this compound.
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| ADME/Pharmacokinetics |
No pharmacokinetic data are available for Luciferase-IN-3. As a small-molecule inhibitor with molecular weight 292.09 g/mol and a heterocyclic structure containing a brominated furan and an oxadiazole ring, its oral bioavailability, half-life, and metabolic stability have not been characterized. It is not a drug candidate, and no formal ADME studies have been performed. For research use, the compound is supplied as a solid powder and should be stored at -20degC. It is typically dissolved in DMSO for in vitro assays, with a recommended stock concentration of 10-20 mM. Solutions are stable for 6 months at -80degC or 1 month at -20degC.
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| Toxicity/Toxicokinetics |
No formal toxicity studies have been published for Luciferase-IN-3. In cell viability assays using various mammalian cell lines (e.g., HEK293, HeLa, HepG2), the compound shows no significant cytotoxicity at concentrations up to 100 uM (72-hour treatment). The acute oral LD₅0 in rodents has not been determined. As a research chemical, it should be handled with standard laboratory safety precautions including the use of gloves, lab coat, and eye protection. The compound is not intended for human use and its safety profile for systemic administration is unknown. Any in vivo use would require prior safety evaluation.
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| References | |
| Additional Infomation |
Luciferase-IN-3 is not a clinical drug and has no regulatory approval or clinical trial status. It is a research-grade chemical used as a tool in molecular biology and drug discovery. Its primary application is as an inhibitor control in luciferase-based reporter gene assays to identify false-positive hits in high-throughput screening campaigns. By confirming that test compounds do not directly inhibit luciferase, researchers can ensure that observed activity is due to genuine biological modulation of the pathway under investigation. The compound was first characterized in a 2008 study by Auld et al. (J Med Chem 2008;51(8):2372-86) on chemical libraries for luciferase inhibitory activity. It is available for research use only.
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| Molecular Formula |
C11H6BRN3O2
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|---|---|
| Molecular Weight |
292.09
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| CAS # |
690987-97-4
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| Appearance |
Solid Powder
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.4236 mL | 17.1180 mL | 34.2360 mL | |
| 5 mM | 0.6847 mL | 3.4236 mL | 6.8472 mL | |
| 10 mM | 0.3424 mL | 1.7118 mL | 3.4236 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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