RBN012759

For research use only.

Catalog No.S8992

RBN012759 Chemical Structure

CAS No. 2360851-29-0

RBN012759 is a potent and selective inhibitor of PARP14 with IC50 of <3 nM and 5 nM for human catalytic domain and mouse catalytic domain, respectively. RBN012759 contributes to anti-tumor immune response.

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Biological Activity

Description RBN012759 is a potent and selective inhibitor of PARP14 with IC50 of <3 nM and 5 nM for human catalytic domain and mouse catalytic domain, respectively. RBN012759 contributes to anti-tumor immune response.
Targets
human PARP14 [2]
(Cell-free assay)
mouse PARP14 [2]
(Cell-free assay)
<3 nM 5 nM
In vitro

RBN012759 is a sufficiently soluble, highly permeable, low efflux and potent inhibitor of human and mouse PARP14 with high PARP family selectivity. RBN012759 treatment of human primary macrophages decreases the MAR/PAR signal corresponding to PARP14 self-MARylation and stabilizes PARP14 protein in a dose-dependent manner. Treatment of primary human macrophages with RBN012759 leads to decreased IL-4 driven M2-like gene expression, suggesting that PARP14 inhibition results in a less immunosuppressive phenotype. [2]

In vivo

RBN012759 has moderate clearance and oral bioavailability in mice. RBN012759 is well-tolerated in mice with repeat dosing up to 500 mg/kg BID (75-fold coverage of the PARP14 mouse). [2]

Protocol

Solubility (25°C)

In vitro DMSO 76 mg/mL (200.81 mM)
Ethanol 5 mg/mL (13.21 mM)
Water 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.

Chemical Information

Molecular Weight 378.46
Formula

C19H23FN2O3S

CAS No. 2360851-29-0
Storage powder
in solvent
Synonyms N/A

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

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Dilution Calculator

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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PARP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID