Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
Other Sizes |
|
MSC1094308 (MSC-1094308) is a novel and potent allosteric inhibitor of the type II AAA ATPase. AAA ATPases play critical roles in a variety of cellular processes necessary for survival and growth.
Targets |
VPS4B ( IC50 = 0.71 μM ); p97 ( IC50 = 7.2 μM )
|
---|---|
ln Vitro |
In HCT116 cells, polyubiquitin accumulation is induced by MSC1094308 (10 μM; 8 hours) as a biomarker of homeostatic inhibition [1].
|
Cell Assay |
Western Blot Analysis[1]
Cell Types: HCT116 cells Tested Concentrations: 10 µM Incubation Duration: 8 h Experimental Results: Resulting in the accumulation of polyubiquitinated proteins (biomarkers of degradation inhibition). |
References |
[1]. Pöhler 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.
|
Molecular Formula |
C₂₉H₂₉F₃N₂
|
---|---|
Molecular Weight |
462.55
|
Exact Mass |
462.23
|
Elemental Analysis |
C, 75.30; H, 6.32; F, 12.32; N, 6.06
|
CAS # |
2219320-08-6
|
Appearance |
Solid powder
|
SMILES |
C1CC2=C(CC1CNCCCC(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F)C5=C(N2)C=CC(=C5)F
|
InChi Key |
OCZIMUMAPGQEBH-UHFFFAOYSA-N
|
InChi Code |
InChI=1S/C29H29F3N2/c30-22-8-4-20(5-9-22)25(21-6-10-23(31)11-7-21)2-1-15-33-18-19-3-13-28-26(16-19)27-17-24(32)12-14-29(27)34-28/h4-12,14,17,19,25,33-34H,1-3,13,15-16,18H2
|
Chemical Name |
4,4-bis(4-fluorophenyl)-N-[(6-fluoro-2,3,4,9-tetrahydro-1H-carbazol-3-yl)methyl]butan-1-amine
|
Synonyms |
MSC-1094308; MSC1094308; MSC 1094308
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO: ~50 mg/mL (~108.1 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1619 mL | 10.8096 mL | 21.6193 mL | |
5 mM | 0.4324 mL | 2.1619 mL | 4.3239 mL | |
10 mM | 0.2162 mL | 1.0810 mL | 2.1619 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.