UPF-1069 | PARP-2 inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $55.00 | ||
| 25 mg | $170.00 |
UPF-1069 (1048371-03-4) is a selective PARP-2 inhibitor (IC50=0.3 μM and ~ 27-fold selective against PARP-1).1,2 Increases apoptosis in hippocampal slices but protects cortical cells in models of post-ischemic brain damage.3 Blocks the interaction between PARP-2 and FOXA1, attenuating androgen receptor-mediated gene expression and inhibiting androgen receptor-positive prostate cancer growth.4
References/Citations:
1) Pellicciari et al. (2008), On the way to selective PARP-2 inhibitors. Design, synthesis, and preliminary evaluation of a series of isoquinolinone derivatives; Chem. Med. Chem., 3 914
2) Thorsell et al. (2017), Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors; J. Med. Chem., 60 1262
3) Moroni et al. (2009), Selective PARP-2 inhibitors increase apoptosis in hippocampal slices but protect cortical cells in models of post-ischaemic brain damage; Br. J. Pharmacol., 157 854
4) Gui et al. (2019), Selective targeting of PARP-2 inhibits androgen receptor signaling and prostate cancer growth through disruption of FOXA1 function; Proc. Natl. Acad. Sci. USA, 116 14573
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
UPF-1069 (1048371-03-4) is a selective PARP-2 inhibitor (IC50=0.3 μM and ~ 27-fold selective against PARP-1).1,2 Increases apoptosis in hippocampal slices but protects cortical cells in models of post-ischemic brain damage.3 Blocks the interaction between PARP-2 and FOXA1, attenuating androgen receptor-mediated gene expression and inhibiting androgen receptor-positive prostate cancer growth.4
References/Citations:
1) Pellicciari et al. (2008), On the way to selective PARP-2 inhibitors. Design, synthesis, and preliminary evaluation of a series of isoquinolinone derivatives; Chem. Med. Chem., 3 914
2) Thorsell et al. (2017), Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors; J. Med. Chem., 60 1262
3) Moroni et al. (2009), Selective PARP-2 inhibitors increase apoptosis in hippocampal slices but protect cortical cells in models of post-ischaemic brain damage; Br. J. Pharmacol., 157 854
4) Gui et al. (2019), Selective targeting of PARP-2 inhibits androgen receptor signaling and prostate cancer growth through disruption of FOXA1 function; Proc. Natl. Acad. Sci. USA, 116 14573
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