RBN012759
Based on 13 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.33%
- No. CAS: 2360851-29-0
- Fòrmula: C19H23FN2O3S
- Peso molecular:378.46
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) RBN012759
More- Nat Commun. 2022 Aug 27;13(1):5063. [Abstract]
- Phytomedicine. 2026 Jun:155:158100. [Abstract]
- EMBO J. 2026 Jan;45(1):261-277. [Abstract]
- EMBO J. 2025 Aug 20. [Abstract]
- EMBO J. 2025 Apr 7. [Abstract]
- EMBO J. 2024 Jul;43(14):2929-2953. [Abstract]
- J Cell Biol. 2025 Feb 3;224(2):e202401101. [Abstract]
- Clin Immunol. 2022 Sep:242:109094. [Abstract]
- bioRxiv. 2025 Sep 15:2025.09.08.674862. [Abstract]
- bioRxiv. 2024 Sep 4:2023.10.13.562273. [Abstract]
- bioRxiv. 2024 July 01.
- bioRxiv. 2024 May 22.
- The Pennsylvania State University. 2023.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
PARP14 <3 nM (IC50) |
PARP4 10 μM (IC50) |
PARP5a 8 μM (IC50) |
PARP5b 10 μM (IC50) |
PARP6 4 μM (IC50) |
PARP7 4 μM (IC50) |
PARP8 20 μM (IC50) |
PARP10 1 μM (IC50) |
PARP11 1 μM (IC50) |
PARP12 5 μM (IC50) |
PARP15 3 μM (IC50) |
PARP16 6 μM (IC50) |
In Vitro
RBN012759 (0.01-10 μM) decreases the MAR/PAR signal corresponding to PARP14 self MARylation and stabilizes PARP14 protein in a dose-dependent manner in human primary macrophages[1].
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RBN012759 (0.1-10 μM) reduces IL-4 stimulated cytokine secretion in human primary macrophages[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
? RBN012759 (100 mg/kg; p.o.) exhibits moderate orally bioavailability (30%) and short plasma half-life (0.4 h) due to moderate clearance (54 mL/min/kg) and low steady-state volume of distribution (1.4 L/kg) in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2360851-29-0
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Appearance Solid
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Peso molecular 378.46
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Fòrmula C19H23FN2O3S
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Color White to off-white
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SMILES
O=C1NC(CS[C@H]2CC[C@H](O)CC2)=NC3=C1C(F)=CC(OCC4CC4)=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (13)
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Journal Impact Factor
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Most Recent
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Nat Commun
The KU-PARP14 axis differentially regulates DNA resection at stalled replication forks by MRE11 and EXO1. [Abstract]2022 Aug 27;13(1):5063. PMID: 36030235 -
Phytomedicine
Echinacoside modulates PARP14-GLUD1 axis to mediate energy metabolism reprogramming and mitochondrial function in diminished ovarian reserve. [Abstract]2026 Jun:155:158100. PMID: 41895093
RBN012759 purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2026 Jun:155:158100. [Abstract]
RBN012759 (10 μM; 24 h) showed no effect on GLUD1 expression in SVOG cells.
RBN012759 purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2026 Jun:155:158100. [Abstract]
RBN012759 (10 μM; 24 h) significantly increased GDH activity and α-KG levels in SVOG cells.
RBN012759 purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2026 Jun:155:158100. [Abstract]
RBN012759 (10 μM) enhanced PARP14 protein expression, it markedly suppressed GLUD1 MARylation modification in SVOG cells.
RBN012759 purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2026 Jun:155:158100. [Abstract]
RBN012759 (10 μM) effectively suppressed the MARylation modification of GLUD1 in SVOG cells.
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EMBO J
Ubiquitin pathway blockade reveals endogenous ADP-ribosylation marking PARP7 and AHR for degradation. [Abstract]2026 Jan;45(1):261-277. PMID: 41326691
RBN012759 purchased from MedChemExpress. Usage Cited in: EMBO J. 2026 Jan;45(1):261-277. [Abstract]
RBN012759 (PARP14i; 0.5 μM; 24 h) resulted in a reduction of mono-ADPr signal by E1 inhibitor-induced in A549 cells.
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EMBO J
2025 Aug 20. PMID: 40836037 -
EMBO J
Interferon-induced PARP14-mediated ADP-ribosylation in p62 bodies requires the ubiquitin-proteasome system. [Abstract]2025 Apr 7. PMID: 40195501 -
EMBO J
2024 Jul;43(14):2929-2953. PMID: 38834853
RBN012759 purchased from MedChemExpress. Usage Cited in: EMBO J. 2024 Jul;43(14):2929-2953. [Abstract]
RBN012759 (PARP14i; 0.5 μM) resulted in a robust reduction of mono-ADPr signal, strongly suggesting that the majority of interferon-induced ADPr in A549 cells is dependent on PARP14 catalytic activity.
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J Cell Biol
2025 Feb 3;224(2):e202401101. PMID: 39760726 -
Clin Immunol
PARP14 promotes the growth and glycolysis of acute myeloid leukemia cells by regulating HIF-1α expression. [Abstract]2022 Sep:242:109094. PMID: 35944879 -
bioRxiv
2025 Sep 15:2025.09.08.674862. PMID: 41000805 -
bioRxiv
A PARP14/TARG1-Regulated RACK1 MARylation Cycle Drives Stress Granule Dynamics in Ovarian Cancer Cells. [Abstract]2024 Sep 4:2023.10.13.562273. PMID: 37873085 -
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Solvente y solubilidad
In Vitro:
DMSO : 233.33 mg/mL (616.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.50 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureza y Documentación
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Ficha de datos (271 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6423 mL | 13.2114 mL | 26.4229 mL | 66.0572 mL |
| 5 mM | 0.5285 mL | 2.6423 mL | 5.2846 mL | 13.2114 mL | |
| 10 mM | 0.2642 mL | 1.3211 mL | 2.6423 mL | 6.6057 mL | |
| 15 mM | 0.1762 mL | 0.8808 mL | 1.7615 mL | 4.4038 mL | |
| 20 mM | 0.1321 mL | 0.6606 mL | 1.3211 mL | 3.3029 mL | |
| 25 mM | 0.1057 mL | 0.5285 mL | 1.0569 mL | 2.6423 mL | |
| 30 mM | 0.0881 mL | 0.4404 mL | 0.8808 mL | 2.2019 mL | |
| 40 mM | 0.0661 mL | 0.3303 mL | 0.6606 mL | 1.6514 mL | |
| 50 mM | 0.0528 mL | 0.2642 mL | 0.5285 mL | 1.3211 mL | |
| 60 mM | 0.0440 mL | 0.2202 mL | 0.4404 mL | 1.1010 mL | |
| 80 mM | 0.0330 mL | 0.1651 mL | 0.3303 mL | 0.8257 mL | |
| 100 mM | 0.0264 mL | 0.1321 mL | 0.2642 mL | 0.6606 mL |
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