[CAS NO. 1431280-51-1] VLX1570
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PRODUCTS SPECIFICATIONS [1431280-51-1]
Store
Catalog
SLK-S8288
Brand
Selleck
CAS
1431280-51-1
DESCRIPTION [1431280-51-1]
Overview
| MDL | MFCD28502165 |
|---|---|
| Molecular Weight | 469.39 |
| Molecular Formula | C23H17F2N3O6 |
| SMILES | O=C1/C(CN(C(C=C)=O)CC/C1=C/C2=CC=C(F)C([N+]([O-])=O)=C2)=C\C3=CC=C(F)C([N+]([O-])=O)=C3 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
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 mg | 5 mg | 10 mg | |
| 1 mM | 2.1304 mL | 10.6521 mL | 21.3042 mL |
| 5 mM | 0.4261 mL | 2.1304 mL | 4.2608 mL |
| 10 mM | 0.2130 mL | 1.0652 mL | 2.1304 mL |
| 50 mM | 0.0426 mL | 0.2130 mL | 0.4261 mL |
Description
VLX1570 is a competitive inhibitor of proteasome activity, with an IC50 of ~10 μM in vitro.
Targets
| DUB [1] (Cell-free assay) |
| ~10 μM |
In vitro
VLX1570 is an analogue of b-AP15 that shows higher potency and improved solubility. VLX1570 preferentially inhibits proteasomal DUB activity while not inhibiting the activities of a panel of non-proteasomal DUBs. VLX1570 binds to and inhibits the activity of ubiquitin-specific protease-14 (USP14) in vitro, with comparatively weaker inhibitory activity towards UCHL5 (ubiquitin-C-terminal hydrolase-5). Treatment of multiple myeloma cells with VLX1570 induces the accumulation of proteasome-bound high molecular weight polyubiquitin conjugates and an apoptotic response. VLX1570 induces the expression of the chaperone HSP70B′, the oxidative stress marker Hmox-1, and the ER stress marker XBP-1s. VLX1570 is retained in cells after removal of drug and that USP14 was engaged by drug 17 hours after wash-out, as evidenced by thermal stabilization and persistent enzyme inhibition.
In vivo
VLX1570 is an inhibitor of proteasome DUB activity currently in clinical trials for relapsed multiple myeloma. Treatment with VLX1570 is found to lead to extended survival in xenograft models of multiple myeloma. The in vivo IC50 for inhibition of proteasome DUB activity and induction of apoptosis is <1 μM, with multiple myeloma cells showing greater levels of sensitivity compared to other tumor types. The lower IC50 for activity in vivo is presumably due to rapid drug uptake and enrichment in cells.
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