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Chemical Structure : RBN012759
CAS No.: 2360851-29-0
Catalog No.: PC-49520Not For Human Use, Lab Use Only.
RBN012759 (RBN-012759) is a potent and highly selective PARP14 chemical probe inhibitor with biochemical IC50 of 3 nM in TR-FRET assays, >300-fold selectivity over all PARP family members.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $248 | In stock | |
| 10 mg | $398 | In stock | |
| 25 mg | $598 | In stock | |
| 50 mg | $898 | In stock | |
| 100 mg | Get quote |
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RBN012759 (RBN-012759) is a potent and highly selective PARP14 chemical probe inhibitor with biochemical IC50 of 3 nM in TR-FRET assays, >300-fold selectivity over all PARP family members.
RBN-012759 is an in vivo chemical probe that selectively engages PARP14 in tissue.
RBN-012759 shows binding affinity for PARP14 with Kd value of 2 nM determined by surface plasmon resonance (SPR), inhibits mouse PARP14 TR-FRET probe displacement assay with an IC50 value of 5 nM, which is comparable with its human PARP14 potency (IC50=3 nM).
RBN-012759 rubustly inhibits PARP14-specific self-MARylation in IFN-γ-stimulated primary human macrophages.
RBN-012759 reversed IL-4-driven gene expression in M2-like macrophages, including CD209, MMP-1 and CLTC. RBN-012759 also decreased the protein level of three M2-like proteins, IL-10, CCL24, and IL1-ra, in the supernatants of IL-4-stimulated macrophages.
RBN012759 induced antitumor inflammation in kidney cancer tumor explant models, elicited similar gene expression changes.
| M.Wt | 378.46 | |
| Formula | C19H23FN2O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
7-(cyclopropylmethoxy)-5-fluoro-2-((((1r,4r)-4-hydroxycyclohexyl)thio)methyl)quinazolin-4(3H)-one |
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1. Laurie B Schenkel , et al. Cell Chem Biol. 2021 Aug 19;28(8):1158-1168.e13.
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