RBN012811
Based on 1 Customer Validation
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.
(Pink: PARP14 Target protein ligand; Blue: Cereblon ligand (HY-10984); Black: linker).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.79%
- CAS 番号: 2569517-30-0
- 分子式: C40H49FN8O6S
- 分子量:788.93
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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Cereblon |
PARP14 5 (KYSE-27 nM (DC50) |
IL-10 |
STAT1 |
RBN012811 (0.001-10 μM; 24 h) selectively degrades endogenous PARP14 in KYSE-270 cells with a DC50 of 5 nM[1].
RBN012811 (0.01-1 μM; 24 or 72 h) causes a dose-dependent reduction in IL-10 production in IL-4-stimulated primary human macrophages[1].
RBN012811 (500 nM; 48 h) treatment of chronic IFNγ-pre-treated A375, 501-Mel, MC38, and YUMM2.1 cells depletes PARP14 protein, enhances IFNγ signalling markers, and does not significantly reduce cell growth[2].
RBN012811 (1 μM; 1-6 h) degrades PARP14 and eliminates IFNγ-induced ADPr condensates in A549 cells[3].
RBN012811 (1 μM; overnight pre-treatment) increases HSV-1 replication and immediate early gene expression in human A549 cells by depleting PARP14 protein[4].
RBN012811 (1 μM; 10 hpi, added at 1 hpi) reduces VSV-GFP replication in human A549-ACE2 cells by depleting PARP14 protein[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KYSE-270 human cancer cells
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Concentration:0.1-1 μM
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Incubation Time:6 h (following 2 h pre-treatment with proteasome inhibitors)
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Result:Had its PARP14 degradation prevented by proteasome inhibitors, confirming dependence on the ubiquitin-proteasome pathway.
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Cell Line:KYSE-270 human cancer cells
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Concentration:0.01-0.1 μM
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Incubation Time:24 h (following 2 h pre-treatment with thalidomide)
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Result:Had its degradation of PARP14 outcompeted by pre-treatment with thalidomide, confirming direct binding to cereblon to mediate degradation.
化学情報
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CAS 番号 2569517-30-0
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性状 Solid
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分子量 788.93
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分子式 C40H49FN8O6S
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Color Light yellow to yellow
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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
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (126.75 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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
純度とドキュメンテーション
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データシート (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[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]
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. 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 |
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| DMSO | 1 mM | 1.2675 mL | 6.3377 mL | 12.6754 mL | 31.6885 mL |
| 5 mM | 0.2535 mL | 1.2675 mL | 2.5351 mL | 6.3377 mL | |
| 10 mM | 0.1268 mL | 0.6338 mL | 1.2675 mL | 3.1688 mL | |
| 15 mM | 0.0845 mL | 0.4225 mL | 0.8450 mL | 2.1126 mL | |
| 20 mM | 0.0634 mL | 0.3169 mL | 0.6338 mL | 1.5844 mL | |
| 25 mM | 0.0507 mL | 0.2535 mL | 0.5070 mL | 1.2675 mL | |
| 30 mM | 0.0423 mL | 0.2113 mL | 0.4225 mL | 1.0563 mL | |
| 40 mM | 0.0317 mL | 0.1584 mL | 0.3169 mL | 0.7922 mL | |
| 50 mM | 0.0254 mL | 0.1268 mL | 0.2535 mL | 0.6338 mL | |
| 60 mM | 0.0211 mL | 0.1056 mL | 0.2113 mL | 0.5281 mL | |
| 80 mM | 0.0158 mL | 0.0792 mL | 0.1584 mL | 0.3961 mL | |
| 100 mM | 0.0127 mL | 0.0634 mL | 0.1268 mL | 0.3169 mL |
RBN012811 関連分類
HY-173679 関連分類
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