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VLX1570

Chemical Structure : VLX1570

CAS No.: 1431280-51-1

VLX1570 (VLX 1570;VLX-1570)

Catalog No.: PC-43050Not For Human Use, Lab Use Only.

VLX1570 is a small molecule b-AP15 analog that fucttion as proteasome deubiquitinase inhibitor with IC50 of 10 uM, interacts at the active sites of the proteasome DUBs USP14 and UCHL5.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

VLX1570 is a small molecule b-AP15 analog that fucttion as proteasome deubiquitinase inhibitor with IC50 of 10 uM, interacts at the active sites of the proteasome DUBs USP14 and UCHL5.
VLX1570 demonstrates cytotoxicity in survival assays in HCT116 colon cancer cells with IC50 of 0.58 uM, shows no inhibitory activity on a panel of recombinant non-proteasome DUBs, recombinant kinases, or caspase-3.
VLX1570 decreases cell viability in chemotherapy resistant endometrial cancer cells consistent with cell cycle arrest and caspase-3 mediated apoptosis.
VLX1570 decreases tumor burden and prolongs survival in WM-xenografted mice.

Physicochemical Properties

M.Wt 469.3944
Formula C23H17F2N3O6
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 32 mg/mL

Chemical Name/SMILES

4H-Azepin-4-one, 3,5-bis[(4-fluoro-3-nitrophenyl)methylene]hexahydro-1-(1-oxo-2-propen-1-yl)-

References

1. Wang X, et al. Chem Biol Drug Des. 2015 Nov;86(5):1036-48.

2. Vogel RI, et al. Oncotarget. 2016 May 24;7(21):30962-76.

3. Shukla N, et al. Cancer Res. 2016 Aug 1;76(15):4525-34.

4. Wang X, et al. Sci Rep. 2016 Jun 6;6:26979. doi: 10.1038/srep26979.

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