| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
This compound directly targets the inactive zymogen forms of executioner caspases, procaspase-3 and procaspase-6. It has EC50 values of 2.4 ± 0.2 µM for procaspase-3 and 2.8 ± 0.3 µM for procaspase-6. It does not activate procaspases-1 or -7.
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| ln Vitro |
Combine Procaspase-3/6 activator 1 (compound 1541) with 100 nM of Procaspase-3 (100 nM to 100 μM). The samples were analyzed by Ac-DEVD-AFC after 4 hours at 37°C. Procaspase-3 was triggered to exhibit activity at low doses of 1541 (EC50 = 2.4 μM), while procaspase-3 was inhibited at high concentrations (IC50 = 34.0 μM) [1]. Compound 1541) is the activator 1 of procaspase-3/6 caspase activity. -3, like procaspase-3, has an equivalent inhibitory action (IC50 = 35 μM][1].
In vitro, CASP3 Activator 1541 activates procaspase-3 and -6, leading to the induction of cell death. It non-covalently self-assembles into chemical fibrils, which are believed to be the active form that promotes caspase activation. It also inhibits mature caspase-3 with an IC50 of 34 µM. |
| ln Vivo |
In vivo data for CASP3 Activator 1541 is not extensively reported. As an activator of apoptosis, its in vivo activity would be related to the induction of cell death in target tissues, such as tumors. It has shown promising results in preclinical studies for cancer treatment.
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| Enzyme Assay |
The in vitro assay for CASP3 Activator 1541 measures its ability to activate procaspase-3 and -6. This is typically performed using a biochemical assay where the proenzyme is incubated with the compound, and the generation of active caspase is measured using a fluorogenic substrate.
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| Cell Assay |
In vitro cell-based assays are performed in cancer cell lines to assess the compound's ability to induce apoptosis. Cells are treated with the activator, and cell death is measured using viability assays. The activation of caspases is confirmed by Western blotting for cleaved caspase-3 and its substrates.
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| Animal Protocol |
In vivo studies would involve administering CASP3 Activator 1541 to tumor-bearing mice in a xenograft model. Tumor growth would be monitored, and the induction of apoptosis in tumor tissue would be confirmed by analyzing markers of cell death, such as cleaved caspase-3.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of CASP3 Activator 1541 are not detailed in the literature. As a research compound, its primary use is in vitro, and its in vivo PK properties would need to be determined for therapeutic development.
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| Toxicity/Toxicokinetics |
Toxicological data for CASP3 Activator 1541 is not available. As an inducer of apoptosis, its safety profile would be critical for any therapeutic application. Off-target effects could lead to significant toxicity.
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| References | |
| Additional Infomation |
CASP3 Activator 1541 is a valuable research tool for studying the mechanisms of apoptosis and for developing new cancer therapies that directly activate the cell death machinery. Its unique mechanism of action, involving non-covalent self-assembly, offers a novel approach to inducing apoptosis.
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| Molecular Formula |
C24H17N3O4
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|---|---|
| Molecular Weight |
411.42
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| Exact Mass |
411.122
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| CAS # |
1100353-03-4
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| PubChem CID |
43816622
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.441
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
726
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=CC2=C1OC(=O)C(=C2)C(=O)NC3=CC=CC(=C3)C4=CN5C=CC=CC5=N4
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| InChi Key |
PQLVYQVWNPGJML-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H17N3O4/c1-30-20-9-5-7-16-13-18(24(29)31-22(16)20)23(28)25-17-8-4-6-15(12-17)19-14-27-11-3-2-10-21(27)26-19/h2-14H,1H3,(H,25,28)
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| Chemical Name |
N-(3-imidazo[1,2-a]pyridin-2-ylphenyl)-8-methoxy-2-oxochromene-3-carboxamide
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| Synonyms |
CASP3-Activator-1541; CASP3-Activator 1541; CASP3 Activator-1541
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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 : ~1 mg/mL (~2.43 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 | 2.4306 mL | 12.1530 mL | 24.3061 mL | |
| 5 mM | 0.4861 mL | 2.4306 mL | 4.8612 mL | |
| 10 mM | 0.2431 mL | 1.2153 mL | 2.4306 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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