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Purity: ≥98%
ML241 HCl is a novel and potent p97 inhibitor which inhibits p97 ATPase with an IC50 value of 100 nM. In a dual-reporter cell line, ML241 restricted the breakdown of a p97-dependent proteasome substrate but not a p97-independent one. Additionally, ML241 hampered the endoplasmic reticulum-associated degradation pathway (ERAD). Because it promotes the proteasome's degradation of ubiquinated proteins and aids in the maturation of autophagosomes, AAA ATPase p97 is essential for preserving protein homeostasis in eukaryotic cells. There is a chance that ML241 can treat cancer.
| Targets |
p97 ATPase ( IC50 = 0.11 μM ); UbG76V–GFP ( IC50 = 3.5 μM )
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| ln Vitro |
ML241 hydrochloride is a strong p97 modulator with an IC50 value of 100 nM that inhibits p97 ATPase. With a Ki of 0.35 μM, ML241 hydrochloride inhibits p97 in relation to ATP. About 170 species of rest examined were not significantly inhibited by ML241 hydrochloride (20 μM). UbG76V-GFP is stabilized by ML241 hydrochloride, with an IC50 of 3.5 μM[1]. After 24 hours and 72 hours, respectively, the GI50s of ML241 hydrochloride on cytotoxic HCT15 and SW403 cells were 53 and 33 μM and 13 and 12 μM [2].
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| Cell Assay |
HeLa cells that are stable in their expression of ODD-luciferase are seeded (5000 cells/well) onto a 96-well white solid bottom plate and allowed to grow for 16 hours. Following a one-hour treatment with DMEM containing MG132 (4 μM), cells are twice washed with 100 μL PBS. In the well, cycloheximide (50 μg/mL), ML241, and DMEM containing 2.5% FBS are added. One of the four 96-well plates that have been prepared is removed from the incubator at each time interval (70, 90, 120, or 150 minutes). Each well holds 50 μL of medium. Luciferin (50 μL of 1 mg/mL in PBS) is added and incubated for 5 minutes at room temperature with 500 rpm shaking. The Synergy HT Microplate Reader uses an integration time of 0.1 ms to determine luminosity intensity[2].
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| 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.
[2]. Chou TF, et al. Selective, reversible inhibitors of the AAA ATPase p97. Probe Reports from the NIH Molecular Libraries Program. April 14, 2011 |
| Molecular Formula |
C23H25CLN4O
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| Molecular Weight |
408.93
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| Exact Mass |
408.17
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| Elemental Analysis |
C, 67.56; H, 6.16; Cl, 8.67; N, 13.70; O, 3.91
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| CAS # |
2070015-13-1
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
C1CCC2=C(C1)C(=NC(=N2)N3CCOC4=CC=CC=C43)NCC5=CC=CC=C5.Cl
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| InChi Key |
DYHMHNNBOLCULH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H24N4O.ClH/c1-2-8-17(9-3-1)16-24-22-18-10-4-5-11-19(18)25-23(26-22)27-14-15-28-21-13-7-6-12-20(21)27;/h1-3,6-9,12-13H,4-5,10-11,14-16H2,(H,24,25,26);1H
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| Chemical Name |
N-benzyl-2-(2,3-dihydro-1,4-benzoxazin-4-yl)-5,6,7,8-tetrahydroquinazolin-4-amine;hydrochloride
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| Synonyms |
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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 |
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| 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) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4454 mL | 12.2270 mL | 24.4541 mL | |
| 5 mM | 0.4891 mL | 2.4454 mL | 4.8908 mL | |
| 10 mM | 0.2445 mL | 1.2227 mL | 2.4454 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.
ML240 and ML241 impair the endoplasmic-reticulum-associated degradation (ERAD) pathway, and only ML240 impairs the autophagy pathway and induces apoptosis. |
Michaelis–Menten plots for inhibition of p97 ATPase activity by a) ML240 and b) ML241.ChemMedChem.2013 Feb;8(2):297-312. |
ML240 induces activation of caspases 3 and 7 and apoptosis.ChemMedChem.2013 Feb;8(2):297-312. |
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