AdipoGen Life Sciences

VR23 [Proteasome Inhibitor]

Product Code:
 
AG-CR1-3676
Product Group:
 
Inhibitors and Activators
Regulatory Status:
 
RUO
Shipping:
 
Ambient
Storage:
 
-20°C
1 / 1
Chemical Structure
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Chemical Structure

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Further Information

Alternate Names/Synonyms:
7-Chloro-4-[4-[(2,4-dinitrophenyl)sulfonyl]-1-piperazinyl]quinoline
Appearance:
White solid.
CAS:
1624602-30-7
EClass:
32160000
Form (Short):
liquid
GHS Symbol:
GHS07
Handling Advice:
Keep cool and dry.
Hazards:
H315, H319, H335
InChi:
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
InChiKey:
PDQVZPPIHADUOO-UHFFFAOYSA-N
Long Description:
Chemical. CAS: 1624602-30-7. Formula: C19H16ClN5O6S. MW: 477.9. Synthetic. Potent selective and reversible chloroquine derivative 20S proteasome inhibitor (all proteolytic subunits). Targets the trypsin-like beta2 subunit of the constitutive 20S proteasome (IC50=1nM). Cross-reacts and inhibits the chymotrypsin-like beta5 subunit (IC50=50-100nM) and the caspase-like/peptidyl-glutamyl peptide-hydrolyzing (PGPH) beta1 subunit (IC50=3µM). Anticancer compound effective in cell-based assays and against multiple myeloma and metastatic breast cancer in vivo. In vitro, induces cell cycle arrest and apoptosis in human cancer cell lines including multiple myeloma, as well as in bortezomib-resistent multiple myeloma cells, but with minimal effects on non-cancerous cells.
MDL:
MFCD28502093
Molecular Formula:
C19H16ClN5O6S
Molecular Weight:
477.9
Other data:
Note: Warming and sonication may be required when dissolving the compound in the solvent of choice. Stock solutions are stable for at least 1 month when stored at -20°C.
Package Type:
Plastic Vial
Precautions:
P280, P302, P352, P304, P340, P305, P351, P338, P332, P337, P313, P405
Product Description:
Potent selective and reversible chloroquine derivative 20S proteasome inhibitor (all proteolytic subunits). Targets the trypsin-like beta2 subunit of the constitutive 20S proteasome (IC50=1nM). Cross-reacts and inhibits the chymotrypsin-like beta5 subunit (IC50=50-100nM) and the caspase-like/peptidyl-glutamyl peptide-hydrolyzing (PGPH) beta1 subunit (IC50=3µM). Anticancer compound effective in cell-based assays and against multiple myeloma and metastatic breast cancer in vivo. In vitro, induces cell cycle arrest and apoptosis in human cancer cell lines including multiple myeloma, as well as in bortezomib-resistent multiple myeloma cells, but with minimal effects on non-cancerous cells.
Purity:
>98% (HPLC)
Signal word:
Warning
SMILES:
O=S(N1CCN(C2=C(C=CC(Cl)=C3)C3=NC=C2)CC1)(C4=CC=C([N+]([O-])=O)C=C4[N+]([O-])=O)=O
Solubility Chemicals:
Soluble in DMSO (10mg/ml) or DMF. Poorly soluble in aqueous solutions.
Transportation:
Non-hazardous
UNSPSC Category:
Biochemical Reagents
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.

References

VR23: A Quinoline-Sulfonyl Hybrid Proteasome Inhibitor That Selectively Kills Cancer via Cyclin E-Mediated Centrosome Amplification: S. Pundir, et al.; Cancer Res. 75, 4164 (2015)