Sr9011 Smars CAS#1379686-29-9 pure powder Material
| SR9011 is a REV-ERBα/β agonist with IC50s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively. | |
| IC50 & Target | IC50: 790 nM (Rev-ErbBα), 560 nM (Rev-ErbBβ)[1] |
|---|---|
(In Vitro) | 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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Sr9011 Smars CAS#1379686-29-9 pure powder Material
| SR9011 is a REV-ERBα/β agonist with IC50s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively. | |
| IC50 & Target | IC50: 790 nM (Rev-ErbBα), 560 nM (Rev-ErbBβ)[1] |
|---|---|
(In Vitro) | 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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