1. Cell Cycle/DNA Damage
    Epigenetics
  2. PARP

UPF 1069 

Cat. No.: HY-14478 Purity: 98.88%
Handling Instructions

UPF 1069 is a PARP inhibitor, with IC50s of 8 and 0.3 μM for PARP-1 and PARP-2, respectively.

For research use only. We do not sell to patients.

UPF 1069 Chemical Structure

UPF 1069 Chemical Structure

CAS No. : 1048371-03-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 119 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 348 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

UPF 1069 is a PARP inhibitor, with IC50s of 8 and 0.3 μM for PARP-1 and PARP-2, respectively.

IC50 & Target[1][2]

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].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 3.5805 mL 17.9025 mL 35.8051 mL
5 mM 0.7161 mL 3.5805 mL 7.1610 mL
10 mM 0.3581 mL 1.7903 mL 3.5805 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[2]

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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

279.29

Formula

C₁₇H₁₃NO₃

CAS No.

1048371-03-4

SMILES

O=C1NC=CC2=C1C=CC=C2OCC(C3=CC=CC=C3)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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UPF 1069
Cat. No.:
HY-14478
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