VR23

Catalog No.S7933 Batch:S793301

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Technical Data

Formula

C19H16ClN5O6S
Molecular Weight 477.88 CAS No. 1624602-30-7
Solubility (25°C)* In vitro DMSO 31 mg/mL (64.86 mM)
Water 5 mg/mL (10.46 mM)
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 Assay:

[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 Study:

[1]
  • Animal Models

    ATH490 athymic mice engrafted with MDA-MB-231 or RPMI 8226 cancer cells

  • Dosages

    30mg/kg

  • Administration

    i.p.

Selleck's VR23 has been cited by 6 publications

Proteasome inhibition as a therapeutic target for the fungal pathogen Cryptococcus neoformans [ Microbiol Spectr, 2023, 11(5):e0190423] PubMed: 37750732
Proteasome inhibition as a therapeutic target for the fungal pathogen Cryptococcus neoformans [ Microbiol Spectr, 2023, 10.1128/spectrum.01904-23] PubMed: 37750732
LAMP3 inhibits autophagy and contributes to cell death by lysosomal membrane permeabilization [ Autophagy, 2021, 1-19] PubMed: 34802379
Prolonged unfolded protein reaction is involved in the induction of chronic myeloid leukemia cell death upon oprozomib treatment [ Cancer Sci, 2020, 112(1):133-143] PubMed: 33067904
Beta-catenin cleavage enhances transcriptional activation. [ Sci Rep, 2018, 8(1):671] PubMed: 29330435
Comparative Proteomics Reveals Strain-Specific β-TrCP Degradation via Rotavirus NSP1 Hijacking a Host Cullin-3-Rbx1 Complex. [ PLoS Pathog, 2016, 12(10):e1005929] PubMed: 27706223

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.