| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
SW-155246 targets DNA methyltransferase 1 (DNMT1), the enzyme responsible for maintaining DNA methylation patterns during DNA replication. DNMT1 is a key epigenetic regulator involved in gene silencing, genomic stability, and cellular differentiation. By selectively inhibiting DNMT1 over DNMT3 isoforms, SW-155246 enables the study of maintenance methylation pathways without interfering with de novo methylation. The compound's non-quinone sulfonamide scaffold provides a clean, redox-independent mechanism of action.
|
|---|---|
| ln Vitro |
SW-155246 is a selective DNMT1 inhibitor with an IC50 of 1.2 µM against human DNMT1 and 38 µM against murine DNMT3 isoforms. Unlike many DNMT1-targeting compounds identified from high-throughput screens, SW-155246 is a non-quinone sulfonamide that does not generate reactive oxygen species or rely on redox cycling. This distinct mechanism and selectivity profile make it a specialized tool for investigating maintenance methylation pathways and validating DNMT1-specific epigenetic interventions.
|
| ln Vivo |
In vivo, SW-155246 promotes anti-tumor immune responses by modulating the tumor microenvironment. It holds significant potential as a therapeutic agent in oncology, particularly for cancers that rely on STAT3 signaling for growth and resistance to conventional therapies. The compound's selectivity for DNMT1 and its redox-independent mechanism suggest a favorable safety profile for in vivo applications. Specific in vivo efficacy data and detailed animal model studies are not extensively documented.
|
| Enzyme Assay |
The in vitro enzyme assay for SW-155246 typically involves measuring the inhibition of DNMT1 and DNMT3A/3B enzymatic activity. Recombinant DNMT enzymes are incubated with varying concentrations of SW-155246 (typically 0.001-100 µM) in the presence of a DNA substrate and the methyl donor S-adenosylmethionine (SAM). The enzymatic activity is measured by monitoring the incorporation of methyl groups into DNA using radiometric or fluorescence-based assays. The IC50 values are determined by plotting the percentage of inhibition against compound concentration.
|
| Cell Assay |
In vitro cellular assays for SW-155246 typically involve treating cancer cell lines with the compound at concentrations ranging from 0.1 to 10 µM for 24-72 hours. Global DNA methylation levels are assessed by ELISA or LC-MS. Gene expression changes are measured by qPCR or RNA-seq. Cell viability and proliferation are evaluated using MTT, CCK-8, or CellTiter-Glo assays. The compound is dissolved in DMSO as a stock solution and diluted in cell culture medium.
|
| Animal Protocol |
In vivo animal studies for SW-155246 typically involve administration to mice via oral gavage or intraperitoneal injection at doses determined from preliminary studies. Tumor xenograft models are used to evaluate antitumor efficacy. Tumor growth is monitored by caliper measurements. DNA methylation and gene expression changes in tumors are assessed by bisulfite sequencing or qPCR. The compound's effects on the tumor microenvironment and immune responses are evaluated by immunohistochemistry and flow cytometry.
|
| ADME/Pharmacokinetics |
SW-155246 has a molecular weight of 378.8 g/mol and formula C16H11ClN2O5S. It is a non-quinone sulfonamide compound. The compound is soluble in DMSO and other organic solvents. Recommended storage is long-term in a cool, dry place. Purity is typically >95%. Detailed PK parameters such as half-life, Cmax, AUC, and bioavailability would require experimental determination.
|
| Toxicity/Toxicokinetics |
SW-155246 is intended for research use only and is not approved for human therapeutic applications. As a DNMT1 inhibitor, the compound may affect normal epigenetic regulation, which could contribute to potential toxicity. Standard preclinical toxicity assessments would include acute toxicity studies in rodents, repeated-dose toxicity studies, and assessment of off-target effects. The compound's redox-independent mechanism may reduce the risk of oxidative stress-related toxicity.
|
| References | |
| Additional Infomation |
SW-155246 (CAS 420092-79-1) is a selective inhibitor of DNA methyltransferase 1 (DNMT1) with an IC50 of 1.2 µM and a 30-fold preference over DNMT3 isoforms (IC50 = 38 µM). It has a molecular weight of 378.8 g/mol and formula C16H11ClN2O5S. The compound is a non-quinone sulfonamide that does not generate reactive oxygen species. SW-155246 promotes anti-tumor immune responses and is used in cancer and epigenetics research. It is also known as 4-chloro-N-(4-hydroxy-1-naphthalenyl)-3-nitro-benzenesulfonamide.
|
| Molecular Formula |
C16H11N2O5SCL
|
|---|---|
| Molecular Weight |
378.787
|
| Exact Mass |
378.007
|
| CAS # |
420092-79-1
|
| PubChem CID |
3718032
|
| Appearance |
Light brown to brown solid powder
|
| Density |
1.6±0.1 g/cm3
|
| Boiling Point |
613.2±65.0 °C at 760 mmHg
|
| Flash Point |
324.6±34.3 °C
|
| Vapour Pressure |
0.0±1.8 mmHg at 25°C
|
| Index of Refraction |
1.731
|
| LogP |
3.94
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
25
|
| Complexity |
590
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
JDYDEJYIVZNWQU-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H11ClN2O5S/c17-13-6-5-10(9-15(13)19(21)22)25(23,24)18-14-7-8-16(20)12-4-2-1-3-11(12)14/h1-9,18,20H
|
| Chemical Name |
4-chloro-N-(4-hydroxynaphthalen-1-yl)-3-nitrobenzenesulfonamide
|
| 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 : ~250 mg/mL (~660.00 mM)
|
|---|---|
| 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 | 2.6400 mL | 13.1999 mL | 26.3999 mL | |
| 5 mM | 0.5280 mL | 2.6400 mL | 5.2800 mL | |
| 10 mM | 0.2640 mL | 1.3200 mL | 2.6400 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
