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Product Details

UPF-1069 | PARP-2 inhibitor

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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Catalog#  10-3779-0005

$55.00
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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.
 
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CAS:
1048371-03-4
Catalog Number:
10-3779
Activity:
PPAR-2 inhibitor
Chemical Name:
5-(2-Oxo-3-phenylethoxy)-1(2H)-isoquinolinone
Molecular Weight:
279.29
Molecular Formula:
C17H13NO3
Solubility:
Soluble in DMSO (up to 40 mg/ml).
Physical Properties:
Off-white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20° (des.)
Stability:
Stable for 2 years as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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