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| Targets |
Firefly luciferase-IN-1 specifically targets the enzyme firefly luciferase. This enzyme catalyzes the oxidation of its substrate, D-luciferin, in the presence of ATP, Mg2+, and oxygen, producing light. By potently and reversibly inhibiting this enzyme, the compound effectively quenches the bioluminescent signal, making it an excellent tool for controlling reporter gene expression in biological experiments.
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| ln Vitro |
In vitro, Firefly luciferase-IN-1 demonstrates exceptional potency, with an IC50 of 0.25 nM. This indicates that it inhibits firefly luciferase activity at sub-nanomolar concentrations. Its high potency and reversible nature make it a valuable tool for precise modulation of luciferase-based assays, allowing for temporal control of the bioluminescent signal.
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| ln Vivo |
Specific in vivo data for Firefly luciferase-IN-1 are not reported in the available literature. As a luciferase inhibitor, its primary application is in in vitro biochemical and cell-based assays to control reporter signals. In vivo use would be limited, but it could potentially be applied in animal models where luciferase is used as a reporter, though such studies are not detailed.
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| Enzyme Assay |
The primary assay for Firefly luciferase-IN-1 is a standard luciferase activity assay. In this assay, purified firefly luciferase enzyme is incubated with its substrates (D-luciferin, ATP, Mg2+) and varying concentrations of the inhibitor. The resulting light output is measured using a luminometer. The IC50 value of 0.25 nM is determined from the dose-response curve.
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| Cell Assay |
In cellular studies, Firefly luciferase-IN-1 is used in cells that have been engineered to express firefly luciferase as a reporter gene. Cells are treated with the inhibitor, and the reduction in bioluminescence is measured. This allows researchers to finely control the reporter signal, which is useful for assays like drug screening or studying gene expression dynamics.
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| Animal Protocol |
Specific in vivo protocols for Firefly luciferase-IN-1 are not available. If used in vivo, it would be administered to animals expressing a luciferase reporter to study the compound's pharmacokinetics or to modulate the signal for imaging purposes.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic (PK) data for Firefly luciferase-IN-1 are not reported. The compound has a molecular formula of C19H16O3 and a molecular weight of 292.33 g/mol. It is a small molecule, suggesting potential for good bioavailability. The powder is stable for up to 3 years when stored at -20°C.
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| Toxicity/Toxicokinetics |
Specific toxicological data for Firefly luciferase-IN-1 are not reported. As a research compound, it is for laboratory use only and is not intended for human therapeutic use.
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| References |
[1]. Li Y, et al. Identification of 2-Benzylidene-tetralone Derivatives as Highly Potent and Reversible Firefly Luciferase Inhibitors. ACS Med Chem Lett. 2022 Jan 20;13(2):304-311.
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| Additional Infomation |
Firefly luciferase-IN-1 is a highly potent and reversible inhibitor of firefly luciferase with an IC50 of 0.25 nM. It is used as a research tool to control bioluminescent signals in luciferase-based assays. Its molecular formula is C19H16O3, and it has a molecular weight of 292.33. It has no clinical applications and is for research use only.
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| Molecular Formula |
C19H16O3
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|---|---|
| Molecular Weight |
292.33
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| Exact Mass |
292.109
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| CAS # |
2765796-41-4
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| PubChem CID |
163214103
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
471
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC=C(C=C1)/C=C/2\CCC3=C(C2=O)C=CC(=C3)C(=O)O
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| InChi Key |
HEEMJVLKXPNKTL-XNTDXEJSSA-N
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| InChi Code |
InChI=1S/C19H16O3/c1-12-2-4-13(5-3-12)10-15-7-6-14-11-16(19(21)22)8-9-17(14)18(15)20/h2-5,8-11H,6-7H2,1H3,(H,21,22)/b15-10+
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| Chemical Name |
(6E)-6-[(4-methylphenyl)methylidene]-5-oxo-7,8-dihydronaphthalene-2-carboxylic acid
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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 | 3.4208 mL | 17.1040 mL | 34.2079 mL | |
| 5 mM | 0.6842 mL | 3.4208 mL | 6.8416 mL | |
| 10 mM | 0.3421 mL | 1.7104 mL | 3.4208 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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