| Identification | Back Directory | [Name]
MSC1094308 | [CAS]
2219320-08-6 | [Synonyms]
MSC1094308
4,4-Bis(4-fluorophenyl)-N-[(6-fluoro-2,3,4,9-tetrahydro-1H-carbazol-3-yl)methyl]-1-butanamine | [Molecular Formula]
C29H29F3N2 | [MDL Number]
MFCD31814427 | [MOL File]
2219320-08-6.mol | [Molecular Weight]
462.55 |
| Chemical Properties | Back Directory | [Boiling point ]
610.4±55.0 °C(Predicted) | [density ]
1.211±0.06 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Sealed in dry,2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
Solid | [pka]
16.91±0.40(Predicted) | [color ]
Off-white to pink |
| Hazard Information | Back Directory | [Uses]
MSC1094308 is a non-competitive and reversible VPS4B/p97 (VCP) (I/II type AAA ATPase) allosteric inhibitor, with IC50 values of 0.71 μM and 7.2 μM for VPS4B and p97, respectively[1]. MSC1094308 inhibits the D2 ATPase activity by binding to a agentable hotspot of p97. MSC1094308 can be used in study of cancer[1]. | [Biological Activity]
MSC1094308 binding to drugable hotspot of p97 has the ability to block the D2 ATPase activity.''MSC1094308 is a reversiblenon-ATP-competitivetype I AAA ATPase VPS4B-selective allosteric inhibitor (IC50 = 0.71 μM) with =10-fold reduced potency toward the type II AAA ATPase VCP/p97 and NSF (IC50 = 7.2 and >40 μMrespectively). MSC1094308 specifically inhibits p97-mediated Ub-GFP degradation without affecting proteasome-dependent ODD-luc degradation using a dual reporter HeLa cell line (10 μM) and exhibits comparable efficacy as DBeQ against 50 ng/mL TNFα-induced IKBα degradation in HeLa cells (10 μM). | [References]
[1] P?hler R, et al. A Non-Competitive Inhibitor of VCP/p97 and VPS4 Reveals Conserved Allosteric Circuits in Type I and II AAA ATPases. Angew Chem Int Ed Engl. 2018 Feb 5;57(6):1576-1580. DOI:10.1002/anie.201711429 |
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| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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