| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
ML-60218 targets RNA polymerase III (Pol III), the enzyme responsible for transcribing small non-coding RNAs such as tRNAs, 5S rRNA, and other small RNAs. By inhibiting Pol III, ML-60218 disrupts transcription of these essential RNA molecules.
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| ln Vitro |
Combining SAHA with ML-60218 inhibits cycle cell processes and induces cell switching, which improves the inhibition of human pancreatic cancer cell proliferation. In PANC-1 and BxPC-3 cells, ML-60218 reverses SAHA-stimulated tRNA expression. HDACs' capacity to produce cytokines and cell cycle factors is improved by ML-60218 [2]. Using blocked tyrosine kinase (DLP) in an in vitro stress assay, ML-60218 demonstrated cytokine-inducing activity, suggesting that its target is viral. It was discovered that ML-60218 hinders VP6's capacity to form higher-order structures, which produces the protein's DLP outer layer without compromising its ability to trimerize. Electron examination of DLP treated with ML-60218 revealed structures that were dangerously damaged. NSP5 was dephosphorylated as a result of viroplasm destruction (10 μM) mediated by ML-60218 [3].
In vitro, ML-60218 inhibits RNA polymerase III with IC50 values of 27 µM for the human enzyme and 32 µM for S. cerevisiae Pol III. It disrupts already assembled viroplasms and hampers the formation of new ones without requiring de novo transcription of cellular RNAs. |
| ln Vivo |
Cellular and in vivo studies for ML-60218 are limited. As a tool compound, it is used to study the biological functions of Pol III. Its ability to inhibit Pol III in cells has been demonstrated, but detailed in vivo efficacy data are not widely available.
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| Enzyme Assay |
The in vitro enzyme inhibition assay for ML-60218 involves measuring the activity of purified RNA polymerase III in the presence of the compound. The assay typically uses a DNA template containing a Pol III-specific promoter, and the incorporation of radiolabeled nucleotides is monitored. The IC50 is determined by plotting the percentage of remaining activity against compound concentration.
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| Cell Assay |
Cellular assays for ML-60218 involve treating cells with the compound and measuring the levels of Pol III transcripts (e.g., tRNAs, 5S rRNA) by quantitative RT-PCR or Northern blot analysis. The inhibition of Pol III activity is assessed by the reduction in the abundance of these small RNAs.
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| Animal Protocol |
In vivo animal studies for ML-60218 are not well-documented. As a research tool, it is primarily used in cell-based assays to study Pol III function.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of ML-60218 have not been extensively characterized. It is a small molecule with a molecular weight of 452.38 g/mol and a molecular formula of C19H15Cl2N3O2S2. Solubility and ADME data are limited.
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| Toxicity/Toxicokinetics |
Toxicity data for ML-60218 are limited. It is a research-grade compound, and comprehensive toxicological evaluations have not been published.
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| References | |
| Additional Infomation |
ML-60218 is a chemical probe developed for studying RNA polymerase III function. It has not entered clinical trials. Its mechanism involves broad-spectrum inhibition of Pol III, making it a valuable tool for investigating the role of Pol III in transcription and cellular physiology.
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| Molecular Formula |
C19H15CL2N3O2S2
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|---|---|
| Molecular Weight |
452.37
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| Exact Mass |
450.998
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| CAS # |
577784-91-9
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| PubChem CID |
2824289
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| Appearance |
Colorless to light yellow liquid
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
632.3±65.0 °C at 760 mmHg
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| Flash Point |
336.2±34.3 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.715
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| LogP |
6.83
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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 |
28
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| Complexity |
662
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C2=NN(C)C(=C2)NS(=O)(=O)C3=CC=CC=C3Cl)SC4=C1C=C(C=C4)Cl
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| InChi Key |
BVBDTTLISMIOJY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H15Cl2N3O2S2/c1-11-13-9-12(20)7-8-16(13)27-19(11)15-10-18(24(2)22-15)23-28(25,26)17-6-4-3-5-14(17)21/h3-10,23H,1-2H3
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| Chemical Name |
2-chloro-N-[5-(5-chloro-3-methyl-1-benzothiophen-2-yl)-2-methylpyrazol-3-yl]benzenesulfonamide
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| Synonyms |
ML 60218; ML60218; ML-60218
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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 : ~100 mg/mL (~221.05 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.53 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.5 mg/mL (5.53 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 | 2.2106 mL | 11.0529 mL | 22.1058 mL | |
| 5 mM | 0.4421 mL | 2.2106 mL | 4.4212 mL | |
| 10 mM | 0.2211 mL | 1.1053 mL | 2.2106 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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