| ML241p97 ATPase inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
ML241 Dilution Calculator
calculate
ML241 Molarity Calculator
calculate
| Cas No. | 1346528-06-0 | SDF | Download 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 |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
