VR23
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MedKoo CAT#: 407205

CAS#: 1624602-30-7

Description: VR23 is a potent and selective inhibitor of trypsin-like proteasomes (IC50 = 1 nmol/L), chymotrypsin-like proteasomes (IC50 = 50-100 nmol/L), and caspase-like proteasomes (IC50 = 3 μmol/L). The primary molecular target of VR23 was β2 of the 20S proteasome catalytic subunit. Notably, VR23 was structurally distinct from other known proteasome inhibitors and selectively killed cancer cells by apoptosis, with little effect on noncancerous cells. VR23 was effective in vivo in controlling multiple myelomas and metastatic breast cancer cells, in the latter case also enhancing the antitumor activity of paclitaxel while reducing its side effects.


Chemical Structure

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VR23
CAS# 1624602-30-7

Theoretical Analysis

MedKoo Cat#: 407205
Name: VR23
CAS#: 1624602-30-7
Chemical Formula: C19H16ClN5O6S
Exact Mass: 477.05098
Molecular Weight: 477.876
Elemental Analysis: C, 47.75; H, 3.37; Cl, 7.42; N, 14.66; O, 20.09; S, 6.71

Price and Availability

Size Price Availability Quantity
10.0mg USD 150.0 Ready to ship
25.0mg USD 250.0 Ready to ship
50.0mg USD 450.0 Ready to ship
100.0mg USD 650.0 Ready to ship
200.0mg USD 850.0 Ready to ship
500.0mg USD 1450.0 Ready to ship
1.0g USD 2450.0 2 weeks
2.0g USD 4250.0 2 weeks
5.0g USD 7950.0 2 weeks
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Synonym: VR23, VR-23, VR 23

IUPAC/Chemical Name: 7-chloro-4-(4-((2,4-dinitrophenyl)sulfonyl)piperazin-1-yl)quinoline

InChi Key: PDQVZPPIHADUOO-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H16ClN5O6S/c20-13-1-3-15-16(11-13)21-6-5-17(15)22-7-9-23(10-8-22)32(30,31)19-4-2-14(24(26)27)12-18(19)25(28)29/h1-6,11-12H,7-10H2

SMILES Code: O=S(N1CCN(C2=CC=NC3=CC(Cl)=CC=C32)CC1)(C4=C(C=C(C=C4)[N+]([O-])=O)[N+]([O-])=O)=O

Appearance: Yellow solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Biological target: VR23 inhibits the activities of trypsin-like proteasomes (IC50=1 nM), chymotrypsin-like proteasomes (IC50=50-100 nM), and caspase-like proteasomes (IC50=3 μM).
In vitro activity: A clonogenic assay showed that very few MCF7 cells survived for 2 weeks at 1.5 μmol/L of VR23 (Supplementary Fig. S1A). Data from flow cytometry showed that the treatment of MCF7 with 2.7or 8.0 μmol/L of VR23 resulted in 23.7% or 38.1% sub-G1 DNA content within 48 hours after treatment, respectively (Supplementary Fig. S1B). In contrast, the flow cytometry profiles of MCF10A cells were not notably different between the sham control and VR23-treated samples, up to 8 μmol/L and 72 hours after treatment (Supplementary Fig. S1C). These data demonstrate that, unlike MCF7, the noncancer MCF10A is much more resistant to VR23, which is consistent with data shown in Fig. 1C. Reference: Cancer Res. 2015 Oct 1;75(19):4164-75. https://cancerres.aacrjournals.org/content/75/19/4164.long
In vivo activity: To determine the anti-inflammatory effects of VR23, the level of TNF-α in the BALF was measured 24 h after the mouse was treated with 0.4 mg of LPS. This study found that VR23 effectively reduces the level of TNF-α (Fig. 4A). Furthermore, VR23 at 30 mg per kilogram of body weight completely inhibited cell invasion into the bronchoalveolar space (Fig. 4B). LPS-induced lung injury can lead to lung tissue inflammation due to the influx of immune cells into the alveolar space. To gain insight into this aspect, this studyexamined the effects of VR23 on lung tissue sections stained with H&E. The resultant histopathological data show that alveolar inflammation caused by LPS is largely prevented when animals are treated with 30 mg/kg VR23 (Fig. 4D). DEX treatment also showed a similar result (Fig. 4D). This suggests that the anti-inflammatory activities of VR23 observed in the cell culture system can be translated into a preclinical model. Reference: J Immunol. 2020 Feb 15;204(4):788-795. https://www.jimmunol.org/content/204/4/788.long

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 21.61 45.22
DMF 2.0 4.19
DMF:PBS (pH 7.2) (1:2) 0.3 0.63
Water 5.0 10.46

Preparing Stock Solutions

The following data is based on the product molecular weight 477.876 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Durkin A, Vu HY, Lee H. The VR23 Antitumor Compound Also Shows Strong Anti-Inflammatory Effects in a Human Rheumatoid Arthritis Cell Model and Acute Lung Inflammation in Mice. J Immunol. 2020 Feb 15;204(4):788-795. doi: 10.4049/jimmunol.1900531. Epub 2020 Jan 8. PMID: 31915262. 2. Pundir S, Vu HY, Solomon VR, McClure R, Lee H. VR23: A Quinoline-Sulfonyl Hybrid Proteasome Inhibitor That Selectively Kills Cancer via Cyclin E-Mediated Centrosome Amplification. Cancer Res. 2015 Oct 1;75(19):4164-75. doi: 10.1158/0008-5472.CAN-14-3370. Epub 2015 Aug 3. PMID: 26238784.
In vitro protocol: 1. Durkin A, Vu HY, Lee H. The VR23 Antitumor Compound Also Shows Strong Anti-Inflammatory Effects in a Human Rheumatoid Arthritis Cell Model and Acute Lung Inflammation in Mice. J Immunol. 2020 Feb 15;204(4):788-795. doi: 10.4049/jimmunol.1900531. Epub 2020 Jan 8. PMID: 31915262. 2. Pundir S, Vu HY, Solomon VR, McClure R, Lee H. VR23: A Quinoline-Sulfonyl Hybrid Proteasome Inhibitor That Selectively Kills Cancer via Cyclin E-Mediated Centrosome Amplification. Cancer Res. 2015 Oct 1;75(19):4164-75. doi: 10.1158/0008-5472.CAN-14-3370. Epub 2015 Aug 3. PMID: 26238784.
In vivo protocol: 1. Durkin A, Vu HY, Lee H. The VR23 Antitumor Compound Also Shows Strong Anti-Inflammatory Effects in a Human Rheumatoid Arthritis Cell Model and Acute Lung Inflammation in Mice. J Immunol. 2020 Feb 15;204(4):788-795. doi: 10.4049/jimmunol.1900531. Epub 2020 Jan 8. PMID: 31915262. 2. Pundir S, Vu HY, Solomon VR, McClure R, Lee H. VR23: A Quinoline-Sulfonyl Hybrid Proteasome Inhibitor That Selectively Kills Cancer via Cyclin E-Mediated Centrosome Amplification. Cancer Res. 2015 Oct 1;75(19):4164-75. doi: 10.1158/0008-5472.CAN-14-3370. Epub 2015 Aug 3. PMID: 26238784.

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 1: Pundir S, Vu HY, Solomon VR, McClure R, Lee H. VR23: A Quinoline-Sulfonyl Hybrid Proteasome Inhibitor That Selectively Kills Cancer via Cyclin E-Mediated Centrosome Amplification. Cancer Res. 2015 Oct 1;75(19):4164-75. doi:10.1158/0008-5472.CAN-14-3370. Epub 2015 Aug 3. PubMed PMID: 26238784.

VR23

10.0mg / USD 150.0