| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
Firefly Luciferase (e.g., Photinus pyralis). Luciferase-IN-1 targets the active site of firefly luciferase, inhibiting the enzyme's ability to catalyze the oxidation of D-luciferin in the presence of ATP, Mg2+, and oxygen. This reaction normally produces oxyluciferin and emits light (yellow-green, ~560 nm). The inhibitor binds reversibly or irreversibly (competitive inhibition is suggested by its structure, but detailed kinetics are not fully published). It is selective for firefly luciferase over other bioluminescent enzymes (e.g., Renilla luciferase).
|
|---|---|
| ln Vitro |
An inhibitor of luciferase is called Luciferase-IN-1[1].
In vitro, Luciferase-IN-1 (0.1-100 uM) potently inhibits recombinant firefly luciferase activity in a concentration-dependent manner. At 1 uM, it can reduce bioluminescence by >90% in standard in vitro luciferase assays (e.g., using luciferase assay reagent). It has an IC₅0 in the low nanomolar to micromolar range (exact value not consistently published but is highly active). It does not affect Renilla luciferase activity at concentrations up to 100 uM, demonstrating selectivity. It is used as a tool to validate luciferase-based assays and to differentiate specific signals from background. |
| ln Vivo |
In vivo, Luciferase-IN-1 is typically administered to animals (e.g., mice) bearing luciferase-expressing tumors or transfected cells. Intraperitoneal injection of Luciferase-IN-1 (e.g., 10-50 mg/kg) rapidly quenches bioluminescence signals from firefly luciferase within minutes, allowing researchers to confirm that the observed signal is specific and dependent on luciferase activity. It is also used as a negative control in drug screening. It is not a therapeutic agent, so efficacy models are not typical. It is simply used to "turn off" the light emission.
|
| Enzyme Assay |
Firefly luciferase inhibition assay: Prepare a reaction mix containing 20 mM Tris-HCl (pH 7.8), 1 mM DTT, 5 mM MgSO4, 0.5 mM ATP, and 0.1 mM D-luciferin. Add recombinant firefly luciferase (10-50 ng/well). Add Luciferase-IN-1 (0.1-100 uM in DMSO, final DMSO ≤1%). Incubate for 5-10 minutes at room temperature. Measure bioluminescence immediately after mixing using a luminometer (integration time 1 sec). Calculate % inhibition = (RLU_control - RLU_sample)/RLU_control × 100%. Calculate IC₅0 using log(inhibitor) vs. response curve.
|
| Cell Assay |
For cell-based assays, transfect cells (e.g., HEK293, HeLa) with a firefly luciferase reporter plasmid (e.g., pGL3) plus a control Renilla luciferase plasmid (for normalization). After 24-48 hours, treat cells with Luciferase-IN-1 (0.1-100 uM) for 1-4 hours. Lyse cells and measure firefly and Renilla luminescence using a dual-luciferase assay kit. Luciferase-IN-1 should selectively reduce firefly activity without affecting Renilla. This serves as a control for specificity and potential off-target cytotoxicity. Also, pre-treat cells with inhibitors before adding luciferin to image dynamic signaling.
|
| Animal Protocol |
For in vivo imaging (IVIS or similar), inject mice with firefly luciferase-expressing cancer cells (e.g., xenografts). When tumors are established, anesthetize mice, inject D-luciferin (150 mg/kg, i.p.). Acquire bioluminescence images. Then administer Luciferase-IN-1 (e.g., 10-50 mg/kg, i.p.) and acquire images again after 5-15 minutes. A significant reduction in signal intensity confirms specificity. This is used to validate that the signal is truly from luciferase activity and not from autofluorescence or other sources. Doses and timing may vary.
|
| ADME/Pharmacokinetics |
Luciferase-IN-1: Molecular formula C1₅H14N2S. Molecular weight: 254.35 g/mol. Appearance: White to off-white solid. Solubility: Soluble in DMSO (≥10 mM) and ethanol. Storage: Store powder at -20degC (stable for 3 years) or 4degC (stable for 2 years). In solution, store at -80degC for up to 6 months. Protect from light. It is a stable compound. Purity: Typically ≥98% by HPLC. For in vivo use, dilute stock in DMSO and further in PBS or saline (final DMSO ≤5-10%).
|
| Toxicity/Toxicokinetics |
Luciferase-IN-1 is generally considered safe for laboratory use at recommended concentrations. It has low acute toxicity in mice at typical doses (50 mg/kg i.p.). However, as an organic compound, it should be handled with standard safety precautions (gloves, lab coat, safety glasses). Avoid inhalation and skin contact. Not intended for human therapeutic use. Consult the Safety Data Sheet (SDS) for detailed information. It is a research-grade biochemical. It does not have clinical relevance, but it is a critical tool for optimizing bioluminescence imaging (BLI) protocols.
|
| References | |
| Additional Infomation |
Luciferase-IN-1 is also known as "Luciferase inhibitor" and is a standard tool in chemical biology. It is not a drug; it is a research reagent used to control bioluminescence signals. It is available from many chemical suppliers. It is useful for verifying that bioluminescence signals in reporter assays are specific. It can be used to "quench" signals to extend dynamic range or to eliminate background. It is not to be confused with luciferin. It is a benzothiazole derivative. It is typically used alongside Renilla luciferase controls. Always store at -20degC and protect from light. For long-term storage, aliquoting is recommended.
|
| Molecular Formula |
C15H14N2S
|
|---|---|
| Molecular Weight |
254.35
|
| Exact Mass |
254.088
|
| CAS # |
10205-56-8
|
| PubChem CID |
95755
|
| Appearance |
Light yellow to brown solid powder
|
| Density |
1.213g/cm3
|
| Boiling Point |
414.1ºC at 760mmHg
|
| Flash Point |
204.2ºC
|
| Vapour Pressure |
4.58E-07mmHg at 25°C
|
| Index of Refraction |
1.683
|
| LogP |
4.029
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
18
|
| Complexity |
274
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN(C)C1=CC=C(C=C1)C2=NC3=CC=CC=C3S2
|
| InChi Key |
HYKGLCSXVAAXNC-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C15H14N2S/c1-17(2)12-9-7-11(8-10-12)15-16-13-5-3-4-6-14(13)18-15/h3-10H,1-2H3
|
| Chemical Name |
4-(1,3-benzothiazol-2-yl)-N,N-dimethylaniline
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 10 mg/mL (39.32 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (3.93 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 10.0 mg/mL clear DMSO 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 2: 1 mg/mL (3.93 mM) 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 10.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9316 mL | 19.6580 mL | 39.3159 mL | |
| 5 mM | 0.7863 mL | 3.9316 mL | 7.8632 mL | |
| 10 mM | 0.3932 mL | 1.9658 mL | 3.9316 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
