Biochem/physiol Actions

Reversible: yes

Primary TargetVprBP

Cell permeable: yes

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.

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Kim, K., et al. 2013. Mol. Cell.52, 459.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)