2. PROTAC Epigenetics Cell Cycle/DNA Damage Immunology/Inflammation Stem Cell/Wnt JAK/STAT Signaling Cytoskeleton Anti-infection
  3. PROTACs PARP Interleukin Related STAT Integrin HSV VSV
  4. RBN012811

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).

For research use only. We do not sell to patients.

RBN012811

RBN012811 Chemical Structure

CAS No. : 2569517-30-0

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Customer Review

Based on 1 publication(s) in Google Scholar

RBN012811 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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STAT3 STAT5 STAT6 STAT1

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αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

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HSV-1 HSV-2 HSV

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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]. (Pink: PARP14 Target protein ligand; Blue: Cereblon ligand (HY-10984); Black: linker).

IC50 & Target

Cereblon

 

PARP14

5 (KYSE-27 nM (DC50)

IL-10

 

STAT1

 

In Vitro

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.

RBN012811 Related Antibodies

Western Blot Analysis[1]

Cell Line: KYSE-270 human cancer cells
Concentration: 0.1-1 μM
Incubation Time: 6 h (following 2 h pre-treatment with proteasome inhibitors)
Result: Had its PARP14 degradation prevented by proteasome inhibitors, confirming dependence on the ubiquitin-proteasome pathway.

Western Blot Analysis[1]

Cell Line: KYSE-270 human cancer cells
Concentration: 0.01-0.1 μM
Incubation Time: 24 h (following 2 h pre-treatment with thalidomide)
Result: Had its degradation of PARP14 outcompeted by pre-treatment with thalidomide, confirming direct binding to cereblon to mediate degradation.
Molecular Weight

788.93

Formula

C40H49FN8O6S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2675 mL 6.3377 mL 12.6754 mL
5 mM 0.2535 mL 1.2675 mL 2.5351 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C1

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C2

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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.

  • Protocol 1

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
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
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RBN012811 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RBN0128112569517-30-0RBN 012811RBN-012811PROTACsPARPInterleukin RelatedSTATIntegrinHSVVSVpoly ADP ribose polymerase ILHerpes simplex virusVesicular Stomatitis VirusKYSE-270 cellsPARP14primary human macrophagesA549 cellsSTAT1vesicular stomatitis virusubiquitin-proteasome pathwayIL-10cereblonherpes simplex virus 1Inhibitorinhibitorinhibit

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