MV151
MV151 (Bodipy TMR-Ahx3L3VS) is a Proteasome-specific Fluorescent probe and proteasome inhibitor. MV151 covalently and irreversibly binds to the catalytic N-terminal threonine of active proteasome and immunoproteasome subunits, blocking proteolytic activity.
For research use only. We do not sell to patients.
- CAS No.: 945611-88-1
- Formula: C59H91BF2N8O9S
- Molecular Weight:1137.27
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
MV151 (10 µM; 1 h) labels active proteasome subunits in platelet and HeLa lysates, and its labeling of β2/β2i and the ~22-kDa catalytic subunits is heat-labile[4].
MV151 uniformly labels the active β1, β2, and β5 subunits of purified 20S proteasomes, and as little as 3 ng is detectable by in-gel fluorescence[5].
MV151 (0.01-10 µM; 1 h) labels all constitutive and immunoproteasome active subunits in HeLa and EL-4 lysates starting from 10 nM and saturates at 1 µM[5].
MV151 (500 nM; 1 h) labels proteasomes in MelJuSo Ub-R-GFP cells within 1 h, and pre-incubation with MG132 (HY-13259) blocks both in-gel labeling and cellular fluorescence[5].
MV151 labels the β1, β2, and β5 proteasome active sites in H9c2 rat cardiomyocytes, and this binding is competitively inhibited by MS in a concentration-dependent manner[10].
MV151 (2 μM; 1 h) labels β5 of the mutant Pf20Sβ5A49S; in the presence of TDI4258, the β5 signal increases relative to the wild type, whereas in the presence of WHZ-04, the β5 signal decreases[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57Bl/6 UbG76V-GFP/1 transgenic (adult, sex- and age-matched)[5]
-
Dosage:20 mmol/kg body weight
-
Administration:i.p.; single injection; 24 hr post-dose
-
Result:UbG76V-GFP reporter accumulated in liver and pancreas.
All cells with reporter accumulation contained very high fluorescence.
In-gel fluorescence showed labeling of proteasome catalytic subunits in liver and pancreas homogenates.
Spleen homogenates showed labeling of both constitutive and inducible proteasome catalytic subunits.
Chemical Information
-
CAS No. 945611-88-1
-
Molecular Weight 1137.27
-
Formula C59H91BF2N8O9S
-
SMILES
O=C(CCC1=C(C)[N-]2[B+3]([F-])([F-])[N]3=C(C4=CC=C(OC)C=C4)C=CC3=CC2=C1C)NCCCCCC(NCCCCCC(NCCCCCC(N[C@H](C(N[C@H](C(N[C@H](/C=C/S(C)(=O)=O)CC(C)C)=O)CC(C)C)=O)CC(C)C)=O)=O)=O
-
Synonyms
Bodipy TMR-Ahx3L3VS
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)