2569517-30-0
Chemical Structure
RBN012811
- CAS No.: 2569517-30-0
- Formula:C40H49FN8O6S
- Molecular Weight:788.93
InChIKey: HTRNIXWEXIRUMI-UHFFFAOYSA-N
SMILES: O=C1N=C(CSC2CCN(CC2)CC(NCCCCCCNC3=CC=CC(C(N4C5C(NC(CC5)=O)=O)=O)=C3C4=O)=O)NC6=CC(NC7CCCC7)=CC(F)=C16
Biological Activity: RBN012811 is a highly selective PROTAC-based PARP14 degrader. RBN012811 forms a ternary complex with cereblon by binding to the NAD+ site of PARP14, and mediates the specific degradation of PARP14 via the ubiquitin-proteasome pathway (IC50=10 nM). RBN012811 effectively depletes endogenous PARP14 in various cell lines and primary human macrophages, thereby downregulating IL-10 production and IFN-β mRNA levels, increasing phosphorylated STAT1 levels to enhance inflammatory signaling, and inhibiting interferon-induced ADPr condensate formation. RBN012811 also modulates viral replication, exhibiting increased HSV1 replication while reducing VSV replication. RBN012811 has important application value in research related to cancer and viral infections[1][2][3][4].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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RBN012811 | 98.79% | RBN012811 is a highly selective PROTAC-based PARP14 degrader. RBN012811 forms a ternary complex with cereblon by binding to the NAD+ site of PARP14, and mediates the specific degradation of PARP14 via the ubiquitin-proteasome pathway (IC50=10 nM). RBN012811 effectively depletes endogenous PARP14 in various cell lines and primary human macrophages, thereby downregulating IL-10 production and IFN-β mRNA levels, increasing phosphorylated STAT1 levels to enhance inflammatory signaling, and inhibiting interferon-induced ADPr condensate formation. RBN012811 also modulates viral replication, exhibiting increased HSV1 replication while reducing VSV replication. RBN012811 has important application value in research related to cancer and viral infections. | ||||||||||||||||||||
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- [1]. Wigle TJ, et al. Targeted Degradation of PARP14 Using a Heterobifunctional Small Molecule. Chembiochem. 2021;22(12):2107-2110. [Content Brief]
- [2]. Wong CW, et al. PARP14 inhibition restores PD-1 immune checkpoint inhibitor response following IFNγ-driven acquired resistance in preclinical cancer models. Nat Commun. 2023;14(1):5983. Published 2023 Sep 26. [Content Brief]
- [3]. Raja R, et al. Interferon-induced PARP14-mediated ADP-ribosylation in p62 bodies requires the ubiquitin-proteasome system. EMBO J. 2025;44(10):2741-2773. [Content Brief]
- [4]. Parthasarathy S, et al. PARP14 is an interferon-induced host factor that promotes IFN production and affects the replication of multiple viruses. mBio. 2025;16(10):e0229925. [Content Brief]
Keywords
