1268524-70-4
(6s)-6-(2-Tert-butoxy-2-oxoethyl)-4-(4-chlorophenyl)-2,3,9-trimethyl-6,7-dihydrothieno[3,2-F][1,2,4]triazolo[4,3-A][1,4]diazepin-10-ium
CAS: 1268524-70-4
Molecular Formula: C23H25ClN4O2S
1268524-70-4 - Names and Identifiers
1268524-70-4 - Physico-chemical Properties
| Molecular Formula | C23H25ClN4O2S |
| Molar Mass | 456.99 |
| Density | 1.33 |
| Melting Point | >205°C (dec.) |
| Boling Point | 610.4±65.0 °C(Predicted) |
| Solubility | DMSO: soluble20mg/mL, clear |
| Appearance | powder |
| Color | white to beige |
| pKa | 2.05±0.60(Predicted) |
| Storage Condition | 2-8°C |
| Stability | Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months. |
| In vitro study | The ()-JQ1 enantiomer binds directly to the Kac binding site of the BET bromodomain domain. ()-JQ1(500 nM) competes with chromatin for binding to BRD4, resulting in NMC cell differentiation and growth arrest. Reduction by Ki67 staining demonstrated that ()-JQ1(500 nM) attenuated the rapid proliferation of the NMC 797 and Per403 cell lines. ()-JQ1(500 nM) effectively reduced the expression of BRD4 target gene in NMC 797 cells. ()-JQ1 inhibited the viability of NMC 11060 cells with an IC50 of 4 nM. ()-JQ1 acts on MM cell line and strongly inhibits MYC expression. ()-JQ1 inhibited KMS-34 and LR5 proliferation with IC50 of 68 nM and 98 nM, respectively. ()-JQ1(500 nM) treatment of MM.1S cells resulted in a significant decrease in the proportion of cells in the S phase, followed by increased cell arrest in the G0/G1 phase. ()-JQ1(500 nM) was stained by β-galactosidase, resulting in significant cell senescence. ()-JQ1(800 nM) treatment of CD138 patient-derived MM samples significantly reduced cell viability. ()-JQ1 inhibited the growth of LP-1 cells with a GI50 of 98 nM. ()-JQ1(625 nM) resulted in an increase in the percentage of LP-1 cells in the G0/G1 phase. () -JQ1(500 nM) acts on LP-1 cells to inhibit MYC, BRD4 and CDK9 expression. ()-JQ1(1 μm) activates HIV transcription by treating latently infected Jurkat T cells. ()-JQ1(50 μm) acts on Jurkat and HeLa cells to primarily stimulate Tat-dependent HIV transcription. ()-JQ1(5 μm) acts on J-Lat A2 cells to induce dissociation of Brd4, thereby allowing Tat to recruit SEC to the HIV promoter, inducing Pol II CTD phosphorylation and Virus transcription. The ()-JQ1 enantiomer binds directly to the Kac binding site of the BET bromodomain domain. ()-JQ1(500 nM) competes with chromatin for binding to BRD4, resulting in NMC cell differentiation and growth arrest. Reduction by Ki67 staining demonstrated that ()-JQ1(500 nM) attenuated the rapid proliferation of the NMC 797 and Per403 cell lines. ()-JQ1(500 nM) effectively reduced the expression of BRD4 target gene in NMC 797 cells. ()-JQ1 inhibited the viability of NMC 11060 cells with an IC50 of 4 nM. ()-JQ1 acts on MM cell line and strongly inhibits MYC expression. ()-JQ1 inhibited KMS-34 and LR5 proliferation with IC50 of 68 nM and 98 nM, respectively. ()-JQ1(500 nM) treatment of MM.1S cells resulted in a significant decrease in the proportion of cells in the S phase, followed by increased cell arrest in the G0/G1 phase. ()-JQ1(500 nM) was stained by β-galactosidase, resulting in significant cell senescence. ()-JQ1(800 nM) treatment of CD138 patient-derived MM samples significantly reduced cell viability. ()-JQ1 inhibited the growth of LP-1 cells with a GI50 of 98 nM. ()-JQ1(625 nM) resulted in an increase in the percentage of LP-1 cells in the G0/G1 phase. ()-JQ1(500 nM) inhibited the expression of MYC, BRD4 and CDK9 in LP-1 cells. ()-JQ1(1 μm) activates HIV transcription by treating latently infected Jurkat T cells. ()-JQ1(50 μm) acts on Jurkat and HeLa cells to primarily stimulate Tat-dependent HIV transcription. ()-JQ1(5 μm) acts on J-Lat A2 cells to induce dissociation of Brd4, thereby allowing Tat to recruit SEC to the HIV promoter, inducing Pol II CTD phosphorylation and Virus transcription. |
| In vivo study | ()-JQ1(50 mg/kg) inhibits tumor growth in mice bearing NMC 797 xenografts. ()-JQ1(50 mg/kg) erases the NUT nuclear spots of mice bearing NMC 797 xenografts, consistent with competitive binding to nuclear chromatin. ()-JQ1(50 mg/kg) treatment of NMC 797 xenografts significantly induced (grade 31) keratin expression. ()-JQ1(50 mg/kg) treatment of the mouse model carrying NMC xenograft tumor promotes differentiation, tumor regression, and prolongs life. ()-Treatment of SCID beige mice with orthotopically transplanted tumors by intravenous injection of mm.1s-luc cells with JQ1(50 mg/kg) significantly prolonged the overall survival of the mice compared to control animals. ()-JQ1(50 mg/kg, intraperitoneal injection) treatment of mice carrying Raji transplanted tumor significantly improved the life span of mice. ( )-JQ1(50 mg/kg) inhibits tumor growth in mice bearing NMC 797 xenografts. ()-JQ1(50 mg/kg) erases the NUT nuclear spots of mice bearing NMC 797 xenografts, consistent with competitive binding to nuclear chromatin. ()-JQ1(50 mg/kg) treatment of NMC 797 xenografts significantly induced (grade 31) keratin expression. ()-JQ1(50 mg/kg) treatment of the mouse model carrying NMC xenograft tumor promotes differentiation, tumor regression, and prolongs life. ()-Treatment of SCID beige mice with orthotopically transplanted tumors by intravenous injection of mm.1s-luc cells with JQ1(50 mg/kg) significantly prolonged the overall survival of the mice compared to control animals. ()-JQ1(50 mg/kg, intraperitoneal injection) treatment of mice carrying Raji transplanted tumor significantly improved the life span of mice. |
1268524-70-4 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.188 ml | 10.941 ml | 21.882 ml |
| 5 mM | 0.438 ml | 2.188 ml | 4.376 ml |
| 10 mM | 0.219 ml | 1.094 ml | 2.188 ml |
| 5 mM | 0.044 ml | 0.219 ml | 0.438 ml |
Last Update：2024-01-02 23:10:35
1268524-70-4 - Reference Information
| biological activity | ( )-JQ1 is a BET bromodomain inhibitor that acts on BRD4(2),IC50 is 33 nM, and binds to all Bromodomain domains of the BET family, but not to Bromodomain domains outside the BET family. ( )-JQ1 is a BET bromodomain inhibitor that acts on BRD4(1/2). in cell-free test, IC50 is 77 nM/33 nM, which binds to all bromine domains of BET family, but not to bromine domains outside BET family. ()-JQ1 can inhibit cell proliferation by inducing autophagy. ()-JQ1 can inhibit the expression of target genes of Nuclear receptor binding SET domain protein 3 (NSD3). |
| in vitro study | ( )-JQ1 enantiomer directly binds to the Kac binding site of the BET bromodomain domain. ()-JQ1(500 nM) competitively binds to chromatin to BRD4, leading to NMC cell differentiation and growth arrest. Reduced by Ki67 staining, it was demonstrated that (+)-JQ1(500 nM) attenuated the rapid proliferation of NMC 797 and Per403 cell lines. ()-JQ1(500 nM) acts on NMC 797 cells to effectively reduce the expression of BRD4 target genes. ()-JQ1 acts on NMC 11060 cells and inhibits cell viability with IC50 of 4 nM. ()-JQ1 acts on MM cell lines and strongly inhibits MYC expression. (+)-JQ1 inhibited KMS-34 and LR5 proliferation with IC50 of 68 nM and 98 nM, respectively. ()-JQ1(500 nM) treatment of MM.1S cells resulted in a significant decrease in the proportion of S-phase cells, followed by an increase in cell arrest in G0/G1 phase. (+)-JQ1(500 nM) was stained by β-galactosidase, resulting in marked cellular senescence. ()-JQ1(800 nM) treated MM samples derived from CD138 patients, significantly reducing cell viability. (+)-JQ1 inhibited LP-1 cell growth with a GI50 of 98 nM. ()-JQ1(625 nM) resulted in an increase in the percentage of LP-1 cells in the G0/G1 phase. ()-JQ1(500 nM) acts on LP-1 cells to inhibit MYC, BRD4 and CDK9 expression. (+)-JQ1(1 μM) processes latent infected Jurkat T cells to activate HIV transcription. (+)-JQ1(50 μM) acts on Jurkat and HeLa cells, mainly stimulating Tat-dependent HIV transcription. (+)-JQ1(5 μM) acts on J-Lat A2 cells, inducing Brd4 dissociation, allowing Tat to recruit SEC to the HIV promoter, inducing Pol II CTD phosphorylation and viral transcription. ()-JQ1 enantiomer directly binds to Kac binding site of BET bromodomain domain. ()-JQ1(500 nM) competitively binds to chromatin to BRD4, leading to NMC cell differentiation and growth arrest. Reduced by Ki67 staining, it was demonstrated that (+)-JQ1(500 nM) attenuated the rapid proliferation of NMC 797 and Per403 cell lines. ()-JQ1(500 nM) acts on NMC 797 cells to effectively reduce the expression of BRD4 target genes. ()-JQ1 acts on NMC 11060 cells and inhibits cell viability with IC50 of 4 nM. ()-JQ1 acts on MM cell lines and strongly inhibits MYC expression. (+)-JQ1 inhibited KMS-34 and LR5 proliferation with IC50 of 68 nM and 98 nM, respectively. ()-JQ1(500 nM) treatment of MM.1S cells resulted in a significant decrease in the proportion of S-phase cells, followed by an increase in cell arrest in G0/G1 phase. (+)-JQ1(500 nM) was stained by β-galactosidase, resulting in marked cellular senescence. ()-JQ1(800 nM) treated MM samples derived from CD138 patients, significantly reducing cell viability. (+)-JQ1 inhibited LP-1 cell growth with a GI50 of 98 nM. ()-JQ1(625 nM) resulted in an increase in the percentage of LP-1 cells in the G0/G1 phase. ()-JQ1(500 nM) acts on LP-1 cells to inhibit MYC, BRD4 and CDK9 expression. (+)-JQ1(1 μM) processes latent infected Jurkat T cells to activate HIV transcription. (+)-JQ1(50 μM) acts on Jurkat and HeLa cells, mainly stimulating Tat-dependent HIV transcription. (+)-JQ1(5 μM) acts on J-Lat A2 cells, inducing Brd4 dissociation, allowing Tat to recruit SEC to the HIV promoter, inducing Pol II CTD phosphorylation and viral transcription. |
| in vivo study | ( )-JQ1(50 mg/kg) treated mice carrying NMC 797 transplanted tumor to inhibit tumor growth. ()-JQ1(50 mg/kg) erases NUT nuclear spots in mice carrying NMC 797 transplanted tumors, consistent with competitive binding to nuclear chromatin. ()-JQ1(50 mg/kg) treated NMC 797 transplanted tumor and significantly induced (grade 31) keratin expression. ()-JQ1(50 mg/kg) treated the mouse model carrying NMC transplanted tumor to promote differentiation, tumor decline and prolong life. ()-JQ1(50 mg/kg) treatment of intravenous injection of MM.1S-luc cells, carrying orthotopic transplantation tumor of SCID beige mice, compared with the control group of animals, significantly prolonged the overall survival of mice. ()-JQ1(50 mg/kg, intraperitoneal injection) treated mice carrying Raji transplanted tumor, which significantly improved the lifespan of mice. ( )-JQ1(50 mg/kg) treated mice carrying NMC 797 transplanted tumor to inhibit tumor growth. ()-JQ1(50 mg/kg) erases NUT nuclear spots in mice carrying NMC 797 transplanted tumors, consistent with competitive binding to nuclear chromatin. ()-JQ1(50 mg/kg) treated NMC 797 transplanted tumor and significantly induced (grade 31) keratin expression. ()-JQ1(50 mg/kg) treated the mouse model carrying NMC transplanted tumor to promote differentiation, tumor decline and prolong life. ()-JQ1(50 mg/kg) treatment of intravenous injection of MM.1S-luc cells, carrying orthotopic transplantation tumor of SCID beige mice, compared with the control group of animals, significantly prolonged the overall survival of mice. ()-JQ1(50 mg/kg, intraperitoneal injection) treated mice carrying Raji transplanted tumor, which significantly improved the lifespan of mice. |
| features | ( )-JQ1 is more effective than (-)-JQ1. |
| target | TargetValue BRD4 (2) (Cell-free assay) 33 nM BRD4 (1) (Cell-free assay) 77 nM |
| Target | Value |
| BRD4 (2) (Cell-free assay) | 33 nM |
| BRD4 (1) (Cell-free assay) | 77 nM |
Last Update：2024-04-09 01:59:58
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Product Name: (S)-(+)-Tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4] Visit Supplier Webpage Request for quotationCAS: 1268524-70-4
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