Home Proteases Proteasome inhibitor VR23

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VR23 Proteasome inhibitor

Cat.No.S7933

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 Proteasome inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 477.88

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S793301 DMSO]31 mg/mL]false]Water]5 mg/mL]false]Ethanol]Insoluble]false Purity: 99.04%
99.04

Chemical Information, Storage & Stability

Molecular Weight 477.88 Formula

C19H16ClN5O6S

 Storage (From the date of receipt)
CAS No. 1624602-30-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1CN(CCN1C2=C3C=CC(=CC3=NC=C2)Cl)S(=O)(=O)C4=C(C=C(C=C4)[N+](=O)[O-])[N+](=O)[O-]

Solubility

In vitro
Batch:

DMSO : 31 mg/mL (64.86 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 5 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Mechanism of Action

Targets/IC50/Ki
Trypsin-like proteasomes [1]
(in Hela cells)
1 nM
Chymotrypsin-like proteasomes [1]
(in Hela cells)
100 nM
Caspase-like proteasomes [1]
(in Hela cells)
3 μM
In vitro
In HeLa cells, VR23 induces ubiquitinated proteins accumulation. In RPMI 8226 and KAS 6 cells, this compound inhibits cell growth with IC50 of 2.94 and 1.46 μM, respectively. It is also equally effective on both bortezomib (BTZ)-sensitive and -resistant RPMI 8226 and ANBL6 cells. When used in combination of bortezomib in the cells above, this chemical shows synergistic effects on cell growth inhibition. In addition, it selectively induces cancer cell apoptosis by causing the accumulation of ubiquitinated cyclin E. [1]
Kinase Assay
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).
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. This compound also reduces adverse effects caused by paclitaxel in mice. [1]
References

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