RBN012759

SKU: orb1305943

Description

RBN012759 is a potent and highly selective inhibitor of PARP14, exhibiting an IC50 of 3 nM and >300-fold selectivity over other PARP family members. This small molecule is a valuable chemical probe for studying PARP14's role in cancer, inflammation, and metabolism in both cellular and animal models.

Research Area

Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 2360851-29-0
• MW: 378.46
• Purity: 99.96% (May vary between batches)
• Formula: C₁₉H₂₃FN₂O₃S
• SMILES: O[C@H]1CC[C@@H](CC1)SCc1nc2cc(OCC3CC3)cc(F)c2c(=O)[nH]1
• Target: PARP
• Solubility: DMSO:12 mg/mL (31.71 mM)

Bioactivity

• Target IC50:
  PARP15:3 μM (IC50)|PARP16:6 μM (IC50)|PARP12:5 μM (IC50)|PARP11:1 μM (IC50)|PARP14:<3 nM (IC50)|PARP6:4 μM (IC50)|PARP5b:10 μM (IC50)|PARP7:4 μM (IC50)|PARP5a:8 μM (IC50)|PARP10:1 μM (IC50)|PARP4:10 μM (IC50)|PARP8:20 μM (IC50)
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• In Vivo:
  METHODS: RBN012759 (500 mg/kg,i.g) twice daily. Investigators collected plasma samples 2 hours after the last dose (i.e., after the penultimate dose) and on the last day to determine plasma levels of RBN012759 using liquid chromatography-mass spectrometry. RESULTS RBN012759 was effective in reducing allergen-induced IgE (immunoglobulin E) overproduction and mucus overproduction. treatment with RBN012759 resulted in a decrease in overall mucus scores in lung tissue, while the number of inflammatory cells recovered from bronchoalveolar lavage fluid (BALF) and the proportion of eosinophils recovered were significantly reduced in the bronchial-alveolar lavage fluid (BALF) of RBN012759-treated mice. were significantly reduced. METHODS: RBN012759 was tested in a C57BL/6 mouse model by oral administration (BID) at doses of 300 mg/kg and 500 mg/kg for 7 days. RESULTS The 500 mg/kg group showed an increase in PARP14 protein levels, while the 300 mg/kg group did not, indicating that RBN012759 can effectively and specifically target PARP14 in vivo at higher doses.
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• In Vitro:
  METHODS: B cells were treated with RBN012759 (1 or 0.33 μM ) and added once daily. Cultures were harvested and counted on day 5 and the supernatant was collected for ELISA. RESULTS RBN012759 induced a decrease in IgE. METHODS: RBN0127599 (0.001-10 μM) was tested in IFN-γ stimulated human primary macrophages and RAW264.7 cells to observe the effect of RBN0127599 on the expression of PARP14 protein in vitro. RESULTS The EC50 value (half-maximal effect concentration) observed in RAW264.7 cells was 10 μM, and in human macrophages it was 8 μM, indicating that RBN0127599 showed effective inhibition of the target PARP14 within these concentration ranges.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

cancer, Inhibitor, inflammatory, inhibit, macrophage, PARP, PARP14, poly ADP ribose polymerase, RBN 012759, RBN012759, RBN-012759, pro-tumor

Compound Identifiers

PubChem CID

138696916