[CAS NO. 1624602-30-7]  VR23

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PRODUCTS SPECIFICATIONS [1624602-30-7]

Store
Catalog
SLK-S7933
Brand
Selleck
CAS
1624602-30-7

DESCRIPTION [1624602-30-7]

Overview

MDLMFCD28502093
Molecular Weight477.88
Molecular FormulaC19H16ClN5O6S
SMILESO=S(N1CCN(C2=CC=NC3=CC(Cl)=CC=C23)CC1)(C4=CC=C([N+]([O-])=O)C=C4[N+]([O-])=O)=O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.0926 mL10.4629 mL20.9258 mL
5 mM0.4185 mL2.0926 mL4.1852 mL
10 mM0.2093 mL1.0463 mL2.0926 mL
50 mM0.0419 mL0.2093 mL0.4185 mL

Description

VR23 is a potent inhibitor with 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 nM100 nM3 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.

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.