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Chemical Structure| 1048371-03-4 Chemical Structure| 1048371-03-4

Structure of UPF 1069
CAS No.: 1048371-03-4

Chemical Structure| 1048371-03-4

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UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM, which is ~27-fold selective against PARP1.

Synonyms: GKT237841

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Product Details of UPF 1069

CAS No. :1048371-03-4
Formula : C17H13NO3
M.W : 279.29
SMILES Code : O=C1NC=CC2=C1C=CC=C2OCC(C3=CC=CC=C3)=O
Synonyms :
GKT237841
MDL No. :MFCD14051631
InChI Key :JJWMRRNGWSITSQ-UHFFFAOYSA-N
Pubchem ID :25015515

Safety of UPF 1069

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P280-P305+P351+P338

Related Pathways of UPF 1069

epigenetics
DNA

Isoform Comparison

Biological Activity

Target
  • PARP1

    PARP1, IC50:8.0 μM

  • PARP2

    PARP2, IC50:0.3 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
PARP2 FL 1000 nM Evaluation of UPF 1069 inhibition on PARP2 FL, IC50 of 1000 nM J Med Chem. 2017 Feb 23;60(4):1262-1271.
PARP1 FL 145 nM Evaluation of UPF 1069 inhibition on PARP1 FL, IC50 of 145 nM J Med Chem. 2017 Feb 23;60(4):1262-1271.
PARP3 FL 1300 nM Evaluation of UPF 1069 inhibition on PARP3 FL, IC50 of 1300 nM J Med Chem. 2017 Feb 23;60(4):1262-1271.
PARP14 ART 5700 nM Evaluation of UPF 1069 inhibition on PARP14 ART, IC50 of 5700 nM J Med Chem. 2017 Feb 23;60(4):1262-1271.
PARP10 FL 7100 nM Evaluation of UPF 1069 inhibition on PARP10 FL, IC50 of 7100 nM J Med Chem. 2017 Feb 23;60(4):1262-1271.
Human Dermal Fibroblasts (HDFs) 10 mM 2 h To verify the repair effect of low-dose ALA-PDT on photoaged HDFs by inhibiting the BER signaling pathway. The results showed that UPF1069 significantly increased the proportion of SA-β-gal-positive cells, increased the proportion of G2/M phase cells, and increased the expression of aging-related proteins P16, P21, P53, while decreasing the expression of the BER pathway key protein MUTYH. J Cell Mol Med. 2024 Jul;28(14):e18536.
mouse mixed cortical cell cultures 1–10 μM 60 min UPF-1069 at 1–10 mmol·L⁻¹ significantly reduced post-ischaemic damage in mouse mixed cortical cells exposed to OGD. Br J Pharmacol. 2009 Jul;157(5):854-62.
rat organotypic hippocampal slices 0.01–1 μM 20–30 min UPF-1069 at 0.01–1 mmol·L⁻¹ caused a concentration-dependent exacerbation (up to 155%) of OGD-induced CA1 pyramidal cell death. Br J Pharmacol. 2009 Jul;157(5):854-62.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.58mL

0.72mL

0.36mL

17.90mL

3.58mL

1.79mL

35.81mL

7.16mL

3.58mL

References

 

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