SR9011
Based on 8 publication(s) in Google Scholar
SR9011 is a REV-ERBα/β agonist with IC50s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.78%
- No. CAS: 1379686-29-9
- Fòrmula: C23H31ClN4O3S
- Peso molecular:479.04
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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) SR9011
More- Cancer Res. 2022 Apr 15;82(8):1503-1517. [Abstract]
- Acta Pharmacol Sin. 2019 Jan;40(1):26-34. [Abstract]
- Free Radical Bio Med. 2019 Dec;145:312-320. [Abstract]
- Br J Pharmacol. 2021 Jan;178(2):328-345. [Abstract]
- Cell Prolif. 2021 Mar;54(3):e12988. [Abstract]
- J Clin Endocrinol Metab. 2025 Mar 17;110(4):991-1002. [Abstract]
- J Pharm Biomed Anal. 2021 Feb 20:195:113870. [Abstract]
- Drug Test Anal. 2021 Feb;13(2):283-298. [Abstract]
Customer Validation & Images
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WB
Actividad biológica
IC50: 790 nM (Rev-ErbBα), 560 nM (Rev-ErbBβ)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
560 nM
Compound: SR9011
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Increased REV-ERB-beta LBD dependent repressor activity in HEK293 cell reporter assay
Increased REV-ERB-beta LBD dependent repressor activity in HEK293 cell reporter assay
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[PMID: 22460951] |
| HEK293 | IC50 |
620 nM
Compound: SR9011
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REV-ERB-alpha mediated transcriptional suppression at Bmal1 promoter in HEK293 cell reporter assay
REV-ERB-alpha mediated transcriptional suppression at Bmal1 promoter in HEK293 cell reporter assay
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[PMID: 22460951] |
| HEK293 | IC50 |
790 nM
Compound: SR9011
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Increased REV-ERB-alpha LBD dependent repressor activity in HEK293 cell reporter assay
Increased REV-ERB-alpha LBD dependent repressor activity in HEK293 cell reporter assay
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[PMID: 22460951] |
SR9011 dose-dependently increases the REV-ERB-dependent repressor activity assessed in HEK293 cells expressing a chimeric Gal4 DNA Binding Domain (DBD) - REV-ERB ligand binding domain (LBD) α or β and a Gal4-responsive luciferase reporter (REV-ERBα IC50=790 nM, REV-ERBβ IC50=560 nM). SR9011 potently and efficaciously suppresses transcription in a cotransfection assay using full-length REV-ERBα along with a luciferase reporter driven by the Bmal1 promoter (SR9011 IC50=620 nM). SR9011 suppresses the expression ofBMAL1 mRNA in HepG2 cells in a REV-ERBα/β-dependent manner[1] SR9011 suppresses proliferation of the breast cancer cell lines regardless of their ER or HER2 status. SR9011 appears to pause the cell cycle of the breast cancer cells prior to M phase. Cyclin A (CCNA2) is identified as a direct target gene of REV-ERB suggesting that suppression of expression of this cyclin by SR9011 may mediate the cell cycle arrest. Treatment with SR9011 results in an increase in cells in the G0/G1 phase and a decrease of cells in S and G2/M phase suggesting that activation of REV-ERB may be resulting in decreased transition from G1 to S phase and/or from S to G2/M phase[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1379686-29-9
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Appearance Solid
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Peso molecular 479.04
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Fòrmula C23H31ClN4O3S
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Color Off-white to yellow
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SMILES
O=C(N1CC(CN(CC2=CC=C(Cl)C=C2)CC3=CC=C([N+]([O-])=O)S3)CC1)NCCCCC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Cancer Res
Disrupting Circadian Rhythm via the PER1-HK2 Axis Reverses Trastuzumab Resistance in Gastric Cancer. [Abstract]2022 Apr 15;82(8):1503-1517. PMID: 35255118 -
Acta Pharmacol Sin
Pharmacological activation of REV-ERBα represses LPS-induced microglial activation through the NF-κB pathway. [Abstract]2019 Jan;40(1):26-34. PMID: 29950615
SR9011 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2019 Jan;40(1):26-34. [Abstract]
BV2 cells are pretreated with different doses of SR9011 (0-10 μM) for 4 h and then exposed to LPS (100 ng/mL) for 12 h. Cell lysates are analyzed by Western blot for iNOS, COX-2, and GAPDH. The relative band intensities of iNOS and COX-2 to GAPDH are analyzed
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Free Radical Bio Med
2019 Dec;145:312-320. PMID: 31585206 -
Br J Pharmacol
Targeted inhibition of Rev-erb-α/β limits ferroptosis to ameliorate folic acid-induced acute kidney injury. [Abstract]2021 Jan;178(2):328-345. PMID: 33068011 -
Cell Prolif
Circadian clock genes promote glioma progression by affecting tumour immune infiltration and tumour cell proliferation. [Abstract]2021 Mar;54(3):e12988. PMID: 33442944 -
J Clin Endocrinol Metab
2025 Mar 17;110(4):991-1002. PMID: 39359072 -
J Pharm Biomed Anal
Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]2021 Feb 20:195:113870. PMID: 33453569 -
Drug Test Anal
High-throughput liquid chromatography tandem mass spectrometry assay as initial testing procedure for analysis of total urinary fraction. [Abstract]2021 Feb;13(2):283-298. PMID: 32852861
Solvente y solubilidad
DMSO : ≥ 43 mg/mL (89.76 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (5.22 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.
Protocolo
MCF10A, MDA-MB-231, MCF-7, MDA-MB-361, SKBR3, BT474 cells are plated in 6-well plates one day before treatment. The MTT cell proliferation assays are performed. Briefly, 3×103 to 5 × 103 cells per well are plated in 96-well plates. Twenty-four hours later, cells are treated with SR9011 (0, 2, 4, 6, 8 and 10 μM) or DMSO. Seventy-two hours after treatment, the cells are labeled with 1.2 mM MTT and incubated for 4 hours. DMSO is then added and readings are taken on a plate reader at 540 nm[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
For circadian gene expression experiments male C57BL6 mice (8-10 weeks of age) are either maintained on a L:D (12h:12h) cycle or on constant darkness. At circadian time (CT) 0 animals are administered a single dose of 100 mg/kg SR9011 (i.p.) and groups of animals (n=6) are sacrificed at CT0, CT6, CT12 and CT18. Gene expression is determined by real time QPCR.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Solt LA, et al. Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. Nature. 2012 Mar 29;485(7396):62-8. [Content Brief]
[2]. Wang Y, et al. Anti-proliferative actions of a synthetic REV-ERBα/β agonist in breast cancer cells. Biochem Pharmacol. 2015 Aug 15;96(4):315-22. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0875 mL | 10.4375 mL | 20.8751 mL | 52.1877 mL |
| 5 mM | 0.4175 mL | 2.0875 mL | 4.1750 mL | 10.4375 mL | |
| 10 mM | 0.2088 mL | 1.0438 mL | 2.0875 mL | 5.2188 mL | |
| 15 mM | 0.1392 mL | 0.6958 mL | 1.3917 mL | 3.4792 mL | |
| 20 mM | 0.1044 mL | 0.5219 mL | 1.0438 mL | 2.6094 mL | |
| 25 mM | 0.0835 mL | 0.4175 mL | 0.8350 mL | 2.0875 mL | |
| 30 mM | 0.0696 mL | 0.3479 mL | 0.6958 mL | 1.7396 mL | |
| 40 mM | 0.0522 mL | 0.2609 mL | 0.5219 mL | 1.3047 mL | |
| 50 mM | 0.0418 mL | 0.2088 mL | 0.4175 mL | 1.0438 mL | |
| 60 mM | 0.0348 mL | 0.1740 mL | 0.3479 mL | 0.8698 mL | |
| 80 mM | 0.0261 mL | 0.1305 mL | 0.2609 mL | 0.6523 mL |
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