ML241 |
| Catalog No.GC11749 |
p97 ATPase inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1346528-06-0
Sample solution is provided at 25 µL, 10mM.
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IC50: 100 nM
ML241 is identified as a potent and selective inhibitors of p97 ATPase.
The p97 AAA (ATPase associated with diverse cellular activities), also called VCP (valosin-containing protein), is an critical therapeutic target for cancer and neurodegenerative diseases. p97 plays important roles in a broad array of cellular processes, such as degradation of misfolded membrane and secretory proteins, homotypic fusion of endoplasmic reticulum and Golgi membranes, membrane transport, Golgi membrane reassembly, cell division, regulation of myofibril assembly, regulation of protein aggregates, as well as autophagosome maturation.
In vitro: Previous study showed that both ML241 and its analog ML240 were able to inhibit p97 ATPase with IC(50) values of around 100 nM. Both ML241 and ML240 could inhibit degradation of a p97-dependent but not a p97-independent proteasome substrate in a dual-reporter cell line. In addition, both ML241 and ML240 could impair the endoplasmic-reticulum-associated degradation (ERAD) pathway. Unexpectedly, ML240 could potently stimulate the accumulation of LC3-II within minutes, inhibit cancer cell growth, and mobilize the executioner caspases 3 and 7 rapidly, whereas ML241 could not [1].
In vivo: Currently, there is no animal in vivo data published.
Clinical trial: Up to now, ML241 is still in the preclinical development stage.
Reference:
[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. | 1346528-06-0 | SDF | |
| Chemical Name | 2-(2H-benzo[b][1,4]oxazin-4(3H)-yl)-N-benzyl-5,6,7,8-tetrahydroquinazolin-4-amine | ||
| Canonical SMILES | C1(CNC2=NC(N3CCOC4=CC=CC=C43)=NC5=C2CCCC5)=CC=CC=C1 | ||
| Formula | C23H24N4O | M.Wt | 372.46 |
| Solubility | Soluble 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 | 2.6849 mL | 13.4243 mL | 26.8485 mL |
| 5 mM | 0.537 mL | 2.6849 mL | 5.3697 mL |
| 10 mM | 0.2685 mL | 1.3424 mL | 2.6849 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)
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