DC Chemicals Limited
China
Product Name: UPF 1069
Price: $400.0/100mg $800.0/250mg $1800.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: 5-(2-Oxo-2-phenylethoxy)-3,4-dihydroisoquinolin-1(2H)-one
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

1048371-03-4

1048371-03-4 structure

1048371-03-4 structure

Name: UPF 1069
Chemical Name: 5-phenacyloxy-2H-isoquinolin-1-one
CAS Number: 1048371-03-4
Molecular Formula: C₁₇H₁₃NO₃
Molecular Weight: 279.290
Catalog: Biochemical Inhibitor DNA damage PARP inhibitor
Create Date: 2018-12-17 08:49:51
Modify Date: 2024-01-02 21:10:38
UPF 1069 is a PARP inhibitor, with IC50s of 8 and 0.3 μM for PARP-1 and PARP-2, respectively.

Name	5-phenacyloxy-2H-isoquinolin-1-one
Synonyms	5-(2-Oxo-2-phenylethoxy)isoquinolin-1(2H)-one 1(2H)-Isoquinolinone, 5-(2-oxo-2-phenylethoxy)- UPF 1069 5-(2-Oxo-2-phenylethoxy)-1(2H)-isoquinolinone

Description	UPF 1069 is a PARP inhibitor, with IC50s of 8 and 0.3 μM for PARP-1 and PARP-2, respectively.
Related Catalog	Research Areas >> Cancer
Target	PARP-2:0.3 μM (IC50) PARP-1:8 μM (IC50)
In Vitro	UPF 1069 (Compound 55) is a PARP inhibitor, with IC50s of 8 and 0.3 μM for PARP-1 and PARP-2, respectively[1]. UPF 1069 (1 µM) reduces the residual PARP activity by approximately 80% of PARP-1-deficient fibroblasts, but only slightly inhibits the enzymic activity in wild-type fibroblasts. UPF 1069 (0.1-1 µM) markedly enhances CA1 hippocampal damage. UPF 1069 (10 µM) also exacerbates oxygen-glucose deprivation (OGD) damage in organotypic hippocampal slices. However, UPF 1069 alleviates the damage cuased by OGD in mixed cortical cell cultures, shows a potent neuroprotective activity both at a concentration (1 µM) selectively acting on PARP-2 and at a concentration (10 µM) inhibiting both PARP-1 and PARP-2 activities[2].
Kinase Assay	PARP activity is evaluated by utilizing commercially available recombinant bovine PARP-1 and mouse PARP-2. Briefly, the enzymatic reaction is carried out in 100 µL of 50 mM Tris-HCl (pH 8.0) containing 5 mM MgCl2, 2 mM dithiothreitol, 10 µg sonicated calf thymus DNA, 0.2 µCi [adenine-2,8-3H]NAD and recombinant enzyme PARP-1 or PARP-2 (0.03 U per sample). Different concentrations of the putative inhibitors are added, and the mixture is incubated for 1 h at 37°C. The reaction is terminated by adding 1 mL of 10% trichloroacetic acid (w/v) and centrifuged. Pellets are then washed twice with 1 mL of H2O and resuspended in 1 mL of 0.1 M NaOH. The radioactivity incorporated from [adenine-2,8-3H]NAD into proteins is evaluated by liquid scintillation spectrometry[2].
References	[1]. Pellicciari R, et al. On the way to selective PARP-2 inhibitors. Design, synthesis, and preliminary evaluation of a series of isoquinolinone derivatives. ChemMedChem. 2008 Jun;3(6):914-23. [2]. Moroni F, et al. Selective PARP-2 inhibitors increase apoptosis in hippocampal slices but protect cortical cells in models of post-ischaemic brain damage.

Density	1.3±0.1 g/cm3
Boiling Point	570.3±50.0 °C at 760 mmHg
Melting Point	166-168 °C
Molecular Formula	C₁₇H₁₃NO₃
Molecular Weight	279.290
Flash Point	298.7±30.1 °C
Exact Mass	279.089539
PSA	59.42000
LogP	2.22
Vapour Pressure	0.0±1.6 mmHg at 25°C
Index of Refraction	1.618
Storage condition	Store at RT

Hazard Codes	Xn
Risk Phrases	22