5.09667
VprBP Inhibitor, B32B3
Synonym(s):
VprBP Inhibitor, B32B3, Vpr Binding protein Inhibitor
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About This Item
Empirical Formula (Hill Notation):
C19H17N5S
CAS Number:
Molecular Weight:
347.44
UNSPSC Code:
12352200
assay
≥98% (HPLC)
form
powder
potency
500 nM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
light yellow
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Cell permeable: yes
Primary Target
VprBP
VprBP
Reversible: yes
Disclaimer
Toxicity: Standard Handling (A)
General description
A cell permeable, potent, selective, and ATP-competitive inhibitor of Vpr (HIV-1) binding protein (VprBP) that preferentially targets cancer cells expressing VprBP and blocks phosphorylation of H2A at Thr120 (IC50 = 500 nM in DU-145 human prostate cancer cells) and reduces cell proliferation. However, it has minimal effect on normal human prostate MLC cells lacking VprBP. Exhibits over 100-fold greater selectivity for VprBP over a panel of 33 other protein kinases. Shown to reduce xenograft tumor progression in nude mice injected with DU-145 cells (~5 mg/kg, i.p. twice a week for 3 weeks). Displays moderately desirable pharmacokinetic properties with t1/2= 7 h and Cmax of 1 µM.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Other Notes
Kim, K., et al. 2013. Mol. Cell.52, 459.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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