PARP14

PARP14 (poly(ADP-ribose) polymerase 14) is a multidomain mono-ADP-ribosyltransferase that functions as both a writer and reader of ADP-ribosylation and regulates immunity, transcriptional control, and genome stability^[1]^[2]. Mechanistically, PARP14 acts as a transcriptional coactivator of STAT6, promoting IL-4/STAT6-dependent gene expression and supporting T helper 2 (Th2) differentiation, cytokine signaling, and allergic inflammatory responses^[3]^[4]^[5]. Through these activities, PARP14 links cytokine-driven transcriptional programs to immune-cell function and tissue inflammation^[3]^[4]. In disease settings, PARP14 contributes to allergic airway disease and has been implicated in cancer-associated survival pathways, including B-cell malignancies and hepatocellular carcinoma, where it supports cellular fitness and disease progression^[2]^[5]^[6]. Beyond immune regulation, PARP14 promotes homologous recombination and protects cells from replication stress, highlighting an additional role in maintaining genome integrity during DNA replication^[7]. Compared with related PARP isoforms, PARP14 is distinguished by the presence of multiple macrodomains together with a catalytic mono-ADP-ribosyltransferase domain, enabling it to integrate ADP-ribose recognition with ADP-ribose writing functions within a single protein^[1]^[2]. For experimental applications, selective PARP14 inhibitors such as RBN012759 have demonstrated high target selectivity and have been used to suppress PARP14-dependent ADP-ribosylation and attenuate allergic inflammatory phenotypes in vivo, providing useful pharmacological tools for mechanistic and translational research^[8]^[9].

References:

[1]. Đukić N, et al. PARP14 is a PARP with both ADP-ribosyl transferase and hydrolase activities. Sci Adv. 2023 Sep 15;9(37):eadi2687.

[2]. Krishnamurthy P, et al. STAT6 and PARP Family Members in the Development of T Cell-dependent Allergic Inflammation. Immune Netw. 2016 Aug;16(4):201-10.

[3]. Torretta A, et al. PARP14 is a writer, reader, and eraser of mono-ADP-ribosylation. J Biol Chem. 2023 Sep;299(9):105096.

[4]. Eddie AM, et al. Selective Pharmaceutical Inhibition of PARP14 Mitigates Allergen-Induced IgE and Mucus Overproduction in a Mouse Model of Pulmonary Allergic Response. Immunohorizons. 2022 Jul 11;6(7):432-446.

[5]. Iansante V, et al. PARP14 promotes the Warburg effect in hepatocellular carcinoma by inhibiting JNK1-dependent PKM2 phosphorylation and activation. Nat Commun. 2015 Aug 10;6:7882.

[6]. Pasi M, et al. Analyzing ion distributions around DNA: sequence-dependence of potassium ion distributions from microsecond molecular dynamics. Nucleic Acids Res. 2015 Feb 27;43(4):2412-23.

[7]. Brooks DM,et al. Immunomodulatory roles of PARPs: Shaping the tumor microenvironment, et al. Curr Opin Chem Biol. 2023 Dec;77:102402.

PARP14 Verwandte Produkte (17):

By Type:	Pan (8) Selective (6)
By Effects:	Inhibitors (15) Degrader (1) Ligand (1)

Art. -Nr.	Produktname	Wirkung	Reinheit

HY-136979

RBN012759	Inhibitor	99.33%
RBN012759 is a potent, selective and orally active inhibitor of PARP14, with an IC₅₀ of <3 nM. RBN012759 displays 300-fold selectivity over the monoPARPs and 1000-fold selectivity over the polyPARPs. RBN012759 decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants.

HY-148566

OUL232	Inhibitor	99.86%
OUL232 is a potent inhibitor of mono-ARTs PARP7, PARP10, PARP11, PARP12, PARP14, and PARP15. OUL232 is the most potent PARP10 inhibitor described to date (IC₅₀=7.8 nM), as well as the first PARP12 inhibitor ever reported.

HY-150207

RBN-3143	Inhibitor	99.29%
RBN-3143 is a potent and NAD+-competitive catalytic PARP14 inhibitor with an IC₅₀ value of 4 nM. RBN-3143 inhibits PARP14-mediated ADP-ribosylation and stabilizes PARP14 in cell lines. RBN-3143 can be used in research of lung inflammation.

HY-117889

PARP14 inhibitor H10	Inhibitor	99.46%
PARP14 inhibitor H10, compound H 10, is a selective inhibitor against PARP14 (IC₅₀=490 nM), over other PARPs (≈24 fold over PARP1). PARP14 inhibitor H10 induces caspase-3/7-mediated cell apoptosis.

HY-108708

GeA-69	Inhibitor	99.91%
GeA-69 is a selective, allosteric inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) targeting macrodomain 2 (MD2), with a K_d value of 2.1 μM. GeA-69 involves in DNA damage repair mechanisms and prevents recruitment of PARP14 MD2 to sites of laser-induced DNA damage.

HY-183548

XW-17	Ligand
XW-17 is a PARP14 inhibitor with an IC₅₀ of 3.03 nM and selectivity over other PARP family members.XW-17 suppresses PARP14-mediated mono-ADP-ribosylation, engages and stabilizes endogenous PARP14 protein.XW-17 attenuates skin lesions and decreases expression of IL-4, IL-13, IgE, and IL-17A in an atopic dermatitis-like mouse model.XW-17 can be used for the research of atopic dermatitis.

HY-148754

PARP10-IN-3	Inhibitor	98.72%
PARP10-IN-3 is a selective mono‐ADP‐ribosyltransferase PARP10 inhibitor with an IC₅₀ of 480 nM for human PARP10. PARP10-IN-3 reveals potent inhibition on PARP2 and PARP15 with IC₅₀s of 1.7 μM for human PARP2 and human PARP15, respectively.

HY-173679

RBN012811	Degrader	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.

HY-148753

PARP10-IN-2	Inhibitor	98.02%
PARP10-IN-2 is a potent mono‐ADP‐ribosyltransferase PARP10 inhibitor with an IC₅₀ of 3.64 μM for human PARP10. PARP10-IN-2 reveals potent inhibition on PARP2 and PARP15 with IC₅₀s of 27 μM and 11 μM for human PARP2 and human PARP15, respectively.

HY-155993

YCH1899	Inhibitor	99.39%
YCH1899 is an orally active PARP inhibitor, with an IC₅₀< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC₅₀ values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats.

HY-121719

TIQ-A	Inhibitor	99.85%
TIQ-A is a potent TNKS (poly-ART, PARP) inhibitor, with an IC₅₀ of 24 nM for TNKS2. TIQ-A is a potential anti-ischemic agent.

HY-143338

ART-IN-1	Inhibitor	98.91%
ART-IN-1 (compound 7) is a selective PARP inhibitor with IC₅₀s of 19, 22, 2.4, >100, 1.1 µM for PARP2, TNKS2, PARP10, PARP14, PARP15, respectively.

HY-148709

ARTD10/PARP10-IN-1	Inhibitor
ARTD10/PARP10-IN-1 (compound 23) is a potent and non-selective PARP inhibitor, targeting to mono-ADP-ribosyltransferases ARTD7/PARP15, ARTD8/PARP14, ARTD10/PARP10 and poly(ADP-ribose) polymerase-1 (ARTD1/PARP1) with IC₅₀s of 1.7 μM, 1.6 μM, 0.8 μM, and 4.4 μM, respectively.

HY-172806

PARP14 inhibitor 1	Inhibitor
PARP14 inhibitor 1 is an orally active, selective PARP14 inhibitor with an IC₅₀ of 5.52 nM. PARP14 inhibitor 1 exhibits favorable pharmacokinetic properties and in vivo safety. PARP14 inhibitor 1 enhances and stabilizes intracellular endogenous PARP14 protein levels, while effectively reducing the expression levels of IL-4, IL-13 and IL-17A. PARP14 inhibitor 1 can be used in research related to atopic dermatitis.

HY-W294889

OUL245	Inhibitor
OUL245 is a 7-Hydroxy derivative, and a selectively PARP2 inhibitor (IC₅₀=44 nM). OUL245 also inhibits other PARP and TNKS enzymes with IC₅₀s of 2.9-8.8 μM.

HY-176456

PARP14 inhibitor 2	Inhibitor
PARP14 inhibitor 2 (Compound 3) is an orally active and highly selective PARP14 inhibitor with an IC₅₀ value of <30 nM. PARP14 inhibitor 2 inhibits the mono-ADP-ribosyltransferase activity of PARP14 and regulates IFN-γ and IL-4 signaling, reversing protumor macrophage polarization and inhibiting anti-tumor inflammatory responses. PARP14 inhibitor 2 is promising for research of PARP14-related diseases such as tumors, atopic dermatitis and autoimmune diseases.

HY-148710

ARTD10/PARP10-IN-2	Inhibitor
ARTD10/PARP10-IN-2 (compound 19) is a potent and non-selective PARP inhibitor, targeting to mono-ADP-ribosyltransferases ARTD10/PARP10 and poly(ADP-ribose) polymerase-1 ARTD1/PARP1 with IC₅₀s of 2.0 μM, and 9.7 μM, respectively.

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