ML241 hydrochloride |
| Catalog No.GC13656 |
p97 ATPase inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2070015-13-1
Sample solution is provided at 25 µL, 10mM.
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IC50: 100 nM
ML241 is identified as a p97 ATPase inhibitor.
The hexameric p97 protein belongs to the type II AAA (ATPase associated with diverse cellular activities) ATPase protein family and is conserved across all eukaryotes and is essential for life
p97 protein, a member of the type II AAA ATPase protein family, is reported to be conservative for nealy all eukaryotes. p97 is also known as valosin-containing protein and Cdc48p in mammals and yeast, respectively, playing key roles in various cellular processes, such as cell division, homotypic fusion of endoplasmic reticulum and Golgi membranes, as well as autophagosome maturations.
In vitro: Both ML241 and its analog ML240 were found to be able to inhibit the degradation of proteasome substrate in a p97-dependent but not a p97-independent manner. ML241 and ML240 could also impaire the endoplasmic-reticulum (ER) associated degradation pathway. ML240 was able to stimulate accumulation of LC3-II potently, inhibit cancer cell growth, and also mobilize the executioner caspases 3 and 7 rapidly, but ML241 was not able to. Further investigation showed that ML240 had broad antiproliferative activity to the NCI-60 panel of cancer cell lines, but lower activity to normal cells. In addition, ML240 could synergize with proteasome inhibitor to inhibit the growth of various colon cancer cell lines. Moreover, both ML241 and ML240 had low off-target activity toward a panel of protein kinases as well as central nervous system targets [1].
In vivo: Currently, there is no animal in vivo data reported.
Clinical trial: Up to now, ML241 is still in the preclinical development stage.
Reference:
[1] Chou TF,Li K,Frankowski KJ,Schoenen FJ,Deshaies RJ. Structure-activity relationship study reveals ML240 and ML241 as potent and selective inhibitors of p97 ATPase. ChemMedChem.2013 Feb;8(2):297-312.
Cell experiment: | HeLa cells stably expressing ODD-luciferase are seeded onto a 96-well white solid bottom plate (5000 cells/well) and cells are grown for 16 h. Cells are treated with DMEM containing MG132 (4 μM) for 1h and washed with 100 μL PBS twice. DMEM containing 2.5% FBS, cycloheximide (50 μg/mL) and ML241 are added into the well. Four 96-well plates are prepared and one of the plates is taken out from incubator at each time point (70, 90, 120, or 150 min). Luciferin (50 μL of 1 mg/mL in PBS) is added into each well containing 50 μL of medium and incubated at room temperature with shaking at 500 rpm for 5 min. Luminescence intensity is determined with 0.1 ms integration time on the Synergy HT Microplate Reader[2]. |
References: [1]. Chou TF, et al. Structure-activity relationship study reveals ML240 and ML241 as potent and selective inhibitors of p97 ATPase. ChemMedChem. 2013 Feb;8(2):297-312. | |
| Cas No. | 2070015-13-1 | SDF | |
| Chemical Name | 2-(2H-benzo[b][1,4]oxazin-4(3H)-yl)-N-benzyl-5,6,7,8-tetrahydroquinazolin-4-amine hydrochlorid | ||
| Canonical SMILES | C1(CNC2=NC(N3CCOC4=CC=CC=C43)=NC5=C2CCCC5)=CC=CC=C1.Cl | ||
| Formula | C23H25ClN4O | M.Wt | 408.92 |
| Solubility | ≥ 40.9mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4455 mL | 12.2273 mL | 24.4547 mL |
| 5 mM | 0.4891 mL | 2.4455 mL | 4.8909 mL |
| 10 mM | 0.2445 mL | 1.2227 mL | 2.4455 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)
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