![(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]diazepin-6-yl)acetate](https://img.chemicalbook.inhttps://img.chemicalbook.com/ProductImageEN/2018-8/Large/63316eb0-d554-4853-9d8b-77af49db8342.gif)
![(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]diazepin-6-yl)acetate](https://img.chemicalbook.inhttp://img.chemicalbook.com/ProductImageEN/2018-8/Small/63316eb0-d554-4853-9d8b-77af49db8342.gif)
![(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]diazepin-6-yl)acetate](https://img.chemicalbook.inhttp://img.chemicalbook.com/ProductImageEN/2018-8/Small/c80f35a4-eb9f-4c71-b9f3-370954fc8fdb.jpg)
(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]diazepin-6-yl)acetate
| Price | USD1.00 |
| Packge | 1KG |
- Min. Order:1G
- Supply Ability:100KG
- Time:2019-07-06
Product Details
- 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]diazepin-6-yl)acetate
- CAS No.1268524-70-4
- MFC23H25ClN4O2S
- MW456.99
- Appearancepowderwhite to beige
- density 1.33
- storage temp. 2-8°C
- Boiling point 610.4±65.0 °C(Predicted)
- Melting point >205°C (dec.)
AD68
| (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]diazepin-6-yl)acetate Basic information |
| 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]diazepin-6-yl)acetate |
| Synonyms: | (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]diazepin-6-yl)acetate;(+)-JQ-1;BroModoMain Inhibitor, (+)-JQ1;(S)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-triMethyl-6H-thienol[3,2-f][1,2,4]troazolo[4,3-a][1,4]diazepin-6-yl)acetate[(+)-6];(+)-JQ1,(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]diazepin-6-yl)acetate;(+)-JQ1,(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]diazepin-6-yl)acetate CAS：;6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid, 4-(4-chlorophenyl)-2,3,9-triMethyl-, 1,1-diMethylethyl ester, (6S)-;(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]diazepin-6-yl)acetate (+)-JQ-1 |
| CAS: | 1268524-70-4 |
| MF: | C23H25ClN4O2S |
| MW: | 456.9882 |
| EINECS: | |
| Product Categories: | Epigenetics;Apis;Inhibitors |
| Mol File: | 1268524-70-4.mol |
![(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]diazepin-6-yl)acetate Structure](http://www.chemicalbook.com/CAS/GIF/1268524-70-4.gif) |
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| (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]diazepin-6-yl)acetate Chemical Properties |
| density | 1.33 |
| storage temp. | 2-8°C |
| solubility | DMSO: soluble20mg/mL, clear |
| color | white to beige |
| (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]diazepin-6-yl)acetate Usage And Synthesis |
| Biological Activity | (+)-JQ1 is a BET bromodomain inhibitor that acts on BRD4 (2) with C50 being 33nM. Except the BET family, (+)-JQ1 does not bind to the Bromodomain structure domain of other family. |
| In vitro | (+)-JQ1 enantiomer can bind to directly the Kac binding site of BET bromodomain structure domain. (+)-JQ1 (500nM) and chromatin competitively bind to BRD4, leading to NMC cell differentiation and growth standstill. The Ki67 staining decrease proves that (+)-JQ1(500nM) weakens the rapid proliferation of NMC 797 and Per403 cell system. (+)-JQ1(500nM) acts on NMC 797 cells, effectively reducing the expression of BRD4 target gene. (+)-JQ1acts on NMC11060 cells inhibiting cell activity with IC50 being 4nM. (+)-JQ1 acts on MM cell system and strongly inhibits MYC expression. (+)-JQ1 inhibits the proliferation of KMS-34 and LR5 with IC50 being 68nM and 98nM respectively. After being treated by (+)-JQ1(500nM), the proportion of MM.1S cell in S phase decrease and more cells stasis in the G0/G1 phase. (+)-JQ1(500nM) dyed by β-galactosidase results in significant cell senescence. In the CD138+-derived MM sample treated by (+)-JQ1(800nM), the cell activity significantly decrease. (+)-JQ1 inhibits LP-1 cell growth with GI50 being 98nM. (+)-JQ1 (625nM) resulted in an increase in the proportion of LP-1 cells at G0/G1 phase. (+)-JQ1 (500nM) acts on LP-1 cells inhibiting MYC, BRD4 and CDK9 expression. (+)-JQ1 (1 μM) deals with latent infection of Jurkat T cells and activates HIV transcription. (+)-JQ1 (50μM) acts on Jurkat and HeLa cells, primarily stimulating Tat-dependent HIV transcription. (+)-JQ1 (5 μM) acts on J-Lat A2 cell inducing Brd4 dissociation, allowing Tat to recruit SEC to the HIV promoter and inducing Pol II CTD phosphorylation and viral transcription. |
| In vivo | (+)-JQ1(50mg /kg) treats mice with NMC797 transplanted tumors inhibiting tumor growth. (+)-JQ1(50mg/kg) erases NUT nuclear spots in mice with NMC797 transplanted tumors, consistent with competitive binding to nuclear chromatin. (+)-JQ1 (50mg/kg) treats NMC797 transplanted tumor, significantly inducing (31grade) keratin expression. (+)-JQ1(50mg/kg) treats mouse model carrying NMC transplanted tumor, promoting differentiation, tumor decline and prolonging life. (+)-JQ1(50mg/kg) treats MM.1S-luc+ cells through intravenous injection. Compared with animals in control group, the life of SCID beige mice carrying orthotopic transplanted tumors significantly extends. Through intraperitoneal injection (+)-JQ1(50mg/kg) can prolong the life of mice carrying Raji xenograft greatly. |
| Characteristic | (+)-JQ1 is more effective than (-)-JQ1. |
| Uses | BET bromodomain inhibitor JQ1 activates HIV latency through antagonizing Brd4 inhibition of Tat-transactivation. |
Company Profile Introduction
Henan CoreyChem Co., Ltd, based on the original Zhengzhou Cote Chemical Research Institute, be brave in absorbing highly educated talents & overseas returnees; actively responded to Zhengzhou City High-tech Zone Government’s Special Care Policy, reorganized and founded in National University of Science and Technology Park, which is a high-tech, stock enterprise of high-end chemical Custom synthesis;The park was created by the People's Government of Henan Province, and proved by Ministry of Education and the National Science & Technology, taking the construction mode of "many college a park, and common development", mainly depends on Zhengzhou University and Henan University’s scientific research and talent advantage to set up Universities, scientific research institute and enterprise scientific research achievements transformation platform, to make high-tech enterprises incubate, is the new high-tech talent gathering base, high and new technology industry enterprise radiation base, colleges and universities technological innovation base.
Henan Coreychem Co., Ltd, facing global High-tech pharmaceutical raw materials, high complex new type intermediates, fine chemicals custom synthesis, scale-up production and Rare chemicals trade. Corey have well-equipped machine, strong technical force and considerate marketing team service. We also have rich experience advantage in basic research, small scale process development, scale-up, industrial technology development & production and cost control.
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- Since:2014-12-17
- Address: No.967,15th Floor,Unit 7, Building 1, No.70 of DianChang Road, High-tech Development Zone, Zhengzho
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