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| 10mg |
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| 25mg |
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| Targets |
MS7972 targets the interaction between the tumor suppressor p53 and CREB-binding protein (CREBBP). CREBBP is a transcriptional coactivator that possesses histone acetyltransferase (HAT) activity and is essential for the function of many transcription factors, including p53. The p53-CREBBP interaction is critical for p53's ability to activate the transcription of genes involved in cell cycle arrest, DNA repair, and apoptosis. By blocking this interaction, MS7972 can inhibit the transcriptional activity of p53.
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| ln Vitro |
When MS7972 is added to CBP BRD, resonance energy transfer causes emission at 445 nm and CBP BRD to be quenched [1].
In vitro, MS7972 potently disrupts the p53-CREBBP interaction. At a concentration of 50 μM, it can almost completely block this bromodomain (BRD) interaction. This demonstrates its high efficacy in inhibiting this specific protein-protein interaction. The compound's ability to block this interaction makes it a useful tool for studying the functional consequences of disrupting p53-mediated transcription. It can be used to investigate the role of the p53-CREBBP interaction in various cellular processes. |
| ln Vivo |
In vivo data for MS7972 are not extensively reported in publicly available sources. As a modulator of the p53 pathway, it holds potential for studying the role of p53 in tumor suppression and other biological processes in animal models. Its ability to block the p53-CREBBP interaction could be used to investigate the consequences of inhibiting p53 transcriptional activity in vivo. Further studies are needed to characterize its in vivo efficacy, pharmacokinetic properties, and safety profile.
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| Enzyme Assay |
In vitro assays for MS7972 typically involve protein-protein interaction studies. These can be performed using techniques such as AlphaScreen, fluorescence polarization, or surface plasmon resonance (SPR). In these assays, recombinant p53 and CREBBP proteins (or their interacting domains) are incubated with varying concentrations of the compound. The extent of interaction is measured, and the compound's potency (IC₅₀) is determined from dose-response curves. The compound's ability to inhibit the interaction can be confirmed by other biochemical methods like co-immunoprecipitation.
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| Cell Assay |
For cell-based assays, cell lines (e.g., cancer cells with wild-type p53) are cultured in standard media. Cells are seeded in multi-well plates and treated with MS7972 at various concentrations for a defined period. Following treatment, the effects on p53 transcriptional activity are assessed by measuring the expression of p53 target genes (e.g., p21, MDM2, BAX) using RT-PCR or Western blotting. Cell viability and proliferation are measured using standard assays. Apoptosis can be assessed by measuring caspase activity or using flow cytometry. All experiments include appropriate vehicle controls and are performed in triplicate.
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| Animal Protocol |
In vivo, MS7972 may be administered to rodents for efficacy studies in cancer models. The compound is formulated in a suitable vehicle and administered via routes like intraperitoneal (IP) injection. Dosing regimens would be determined based on preliminary pharmacokinetic and tolerability studies. Endpoints for efficacy studies could include measuring tumor growth inhibition, analyzing the expression of p53 target genes in tumor tissue, and assessing markers of apoptosis and cell proliferation. All procedures must be conducted in accordance with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for MS7972 are not extensively reported in public sources. The compound has a molecular weight of 227.26 and is soluble in DMSO. It is typically stored as a powder at -20°C. For in vivo applications, it would be formulated in a suitable vehicle to ensure adequate exposure. A comprehensive ADME profile is essential for interpreting results from in vivo studies.
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| Toxicity/Toxicokinetics |
Toxicological data for MS7972 are limited. As a modulator of the p53 pathway, its safety profile requires careful evaluation. The compound is for research use only and is not for human consumption. Potential toxicity could arise from on-target effects on p53 function. Comprehensive toxicology studies would be required for any future therapeutic application.
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| References | |
| Additional Infomation |
MS7972 is a research-grade chemical probe, and its primary application is in the study of the p53 signaling pathway. Its ability to block the p53-CREBBP interaction makes it a valuable tool for dissecting the molecular mechanisms of p53-mediated transcription. The compound is not an approved drug and has not entered clinical trials. It is commercially available from various chemical suppliers for research purposes only.
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| Molecular Formula |
C14H13NO2
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|---|---|
| Molecular Weight |
227.259
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| Exact Mass |
227.094
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| Elemental Analysis |
C, 73.99; H, 5.77; N, 6.16; O, 14.08
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| CAS # |
352553-42-5
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| Related CAS # |
352553-42-5
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| PubChem CID |
853608
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.3
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
17
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| Complexity |
352
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(=O)N1C2=CC=CC=C2C3=C1C(=O)CCC3
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| InChi Key |
MIGJEXKBUJPKJF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H13NO2/c1-9(16)15-12-7-3-2-5-10(12)11-6-4-8-13(17)14(11)15/h2-3,5,7H,4,6,8H2,1H3
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| Chemical Name |
9-acetyl-3,4-dihydro-2H-carbazol-1-one
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| Synonyms |
MS7972; MS 7972; MS-7972
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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) |
DMSO: 45~100 mg/mL(198.0~440.0 mM)
Ethanol: ~11 mg/mL(~48.4 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.4002 mL | 22.0012 mL | 44.0025 mL | |
| 5 mM | 0.8800 mL | 4.4002 mL | 8.8005 mL | |
| 10 mM | 0.4400 mL | 2.2001 mL | 4.4002 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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