VR23

Catalog No.S7933

For research use only.

VR23 is a potent proteasome inhibitor with IC50 of 1 nM, 50-100 nM, and 3 μM for trypsin-like proteasomes, chymotrypsin-like proteasomes, and caspase-like proteasomes, respectively.

VR23 Chemical Structure

CAS No. 1624602-30-7

Selleck's VR23 has been cited by 4 Publications

Purity & Quality Control

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Biological Activity

Description VR23 is a potent proteasome inhibitor with IC50 of 1 nM, 50-100 nM, and 3 μM for trypsin-like proteasomes, chymotrypsin-like proteasomes, and caspase-like proteasomes, respectively.
Targets
Trypsin-like proteasomes [1]
(in Hela cells)
Chymotrypsin-like proteasomes [1]
(in Hela cells)
Caspase-like proteasomes [1]
(in Hela cells)
1 nM 100 nM 3 μM
In vitro

In HeLa cells, VR23 induces ubiquitinated proteins accumulation. In RPMI 8226 and KAS 6 cells, VR23 inhibits cell growth with IC50 of 2.94 and 1.46 μM, respectively. VR23 is also equally effective on both bortezomib (BTZ)-sensitive and -resistant RPMI 8226 and ANBL6 cells cells. When used in combination of bortezomib in the cells above, VR23 shows synergistic effects on cell growth inhibition. In addition, VR23 selectively induces cancer cell apoptosis by causing the accumulation of ubiquitinated cyclin E. [1]

In vivo In ATH490 athymic mice engrafted with MDA-MB-231 metastatic breast cancer cells, VR23 (30mg/kg, i.p.) shows effective antitumor and antiangiogenic activities. VR23 also reduces adverse effects caused by paclitaxel in mice. [1]

Protocol (from reference)

Kinase Assay:

[1]

  • Proteasome assay:

    Exponentially growing cells on a 96-well clustered plate are treated with different concentrations of drugs or left untreated (control) for 6 hours. Proteasomes extracted with 0.5% NP40 buffer are mixed with equal amounts of samples in 100 μL total volume, and then incubated with 25 μmol/L of fluorogenic substrates (LRR- specific for trypsin-like activity, LLE-specific for caspase-like activity, and SUVY-specific for chymotrypsin-like activity) in black-bottom 96-well plates at 37°C. Fluorescence is monitored every 5 minutes at the wavelength of 360 nm (excitation) and 480 nm (emission).

Cell Research:

[1]

  • Cell lines: RPMI 8226, KAS 6, 184B5, and MCF10A cells; bortezomib-resistant RPMI 8226 cells and bortezomib-resistant ANBL6 cells
  • Concentrations: ~20 μM
  • Incubation Time: --
  • Method:

    Clonogenic and SRB assays are carried out. IC50 values are calculated using a sigmoidal dose-response curve (variable slope) using a Graph Pad Prism V 4.02 version.

Animal Research:

[1]

  • Animal Models: ATH490 athymic mice engrafted with MDA-MB-231 or RPMI 8226 cancer cells
  • Dosages: 30mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 477.88
Formula

C19H16ClN5O6S

CAS No. 1624602-30-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CCN1C2=C3C=CC(=CC3=NC=C2)Cl)S(=O)(=O)C4=C(C=C(C=C4)[N+](=O)[O-])[N+](=O)[O-]

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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