[CAS NO. 2360851-29-0] RBN012759

Name: RBN012759
Brand: Arctom Scientific
SKU: SLK-S8992

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PRODUCTS SPECIFICATIONS [2360851-29-0]

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Catalog

SLK-S8992

Brand

Selleck

CAS

2360851-29-0

DESCRIPTION [2360851-29-0]

Overview

MDL	-
Molecular Weight	378.46
Molecular Formula	C19H23FN2O3S
SMILES	FC1=C2C(=CC(OCC3CC3)=C1)NC(CS[C@@H]4CC[C@@H](O)CC4)=NC2=O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.6423 mL	13.2114 mL	26.4229 mL
5 mM	0.5285 mL	2.6423 mL	5.2846 mL
10 mM	0.2642 mL	1.3211 mL	2.6423 mL
50 mM	0.0528 mL	0.2642 mL	0.5285 mL

Description

RBN012759 is a potent and selective inhibitor of 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.

References

[1] Laurie Schenkel, et al. Cancer Res 2020;80(16 Suppl):Abstract nr 1038.
[2] Laurie Schenkel, et al. AACR Annual Meeting 2020.