UPF 1069

Catalog No.S8038 Batch:S803801

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Technical Data

Formula

C17H13NO3
Molecular Weight 279.29 CAS No. 1048371-03-4
Solubility (25°C)* In vitro DMSO 56 mg/mL (200.5 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM. It is ~27-fold selective against PARP1.
Targets
PARP2 [1] PARP1 [1]
0.3 μM 8.0 μM
In vitro UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM while inhibiting PARP1 with IC50 of 8 μM. [1]
In vivo In organotypic hippocampal slices, PARP-2 inhibition with UPF-1069 (0.01-1 mM) causes a concentration-dependent exacerbation (up to 155%) of oxygen-glucose deprivation (OGD)-induced CA1 pyramidal cell death. Higher concentrations, acting on both PARP-1 and PARP-2, have no effect on OGD injury. In mouse mixed cortical cells exposed to OGD, UPF-1069 (1-10 mM) significantly reduces post-ischaemic damage. [1]
Features The most selective PARP2 inhibitor available to date.

Protocol (from reference)

Selleck's UPF 1069 has been cited by 9 publications

The interplay of TARG1 and PARG protects against genomic instability [ Cell Rep, 2023, 42(9):113113] PubMed: 37676774
Haploinsufficiency of ZNF251 causes DNA-PKcs-dependent resistance to PARP inhibitors in BRCA1-mutated cancer cells [ Res Sq, 2023, rs.3.rs-2688694] PubMed: 37066268
Haploinsufficiency of ZNF251 causes DNA-PKcs-dependent resistance to PARP inhibitors in BRCA1-mutated cancer cells [ Res Sq, 2023, rs.3.rs-2688694] PubMed: 37066268
Control of replication stress and mitosis in colorectal cancer stem cells through the interplay of PARP1, MRE11 and RAD51 [ Cell Death Differ, 2021, 10.1038/s41418-020-00733-4] PubMed: 33531658
Response of Breast Cancer Cells to PARP Inhibitors Is Independent of BRCA Status. [ J Clin Med, 2020, 30;9(4)] PubMed: 32235451
Enabling drug discovery for the PARP protein family through the detection of mono-ADP-ribosylation [ Biochem Pharmacol, 2019, 10.1016/j.bcp.2019.05.007] PubMed: 31075269
DNA‑PKcs PARylation regulates DNA‑PK kinase activity in the DNA damage response. [ Mol Med Rep, 2019, 20(4):3609-3616] PubMed: 31485633
Inhibition of Parp1 by BMN673 Effectively Sensitizes Cells to Radiotherapy by Upsetting the Balance of Repair Pathways Processing DNA Double-Strand Breaks [ Mol Cancer Ther, 2018, 17(10):2206-2216] PubMed: 29970481
Dual Inhibitors of PARPs and ROCKs. [ ACS Omega, 2018, 3(10):12707-12712] PubMed: 30411017

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.