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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

Biological Activity In vitro In vivo Characteristic
(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
(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
Chemical 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
jq01;S-JQ1;(+)-JQ-1;(+)-JQ1, >=99%;BroModoMain Inhibitor, (+)-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;tert-butyl (S)-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;(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;(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]
CBNumber:
CB72572988
Molecular Formula:
C23H25ClN4O2S
Formula Weight:
456.9882
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 Properties

Density 
1.33
storage temp. 
2-8°C
solubility 
DMSO: soluble20mg/mL, clear
form 
powder
color 
white to beige

SAFETY

(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 More Price(6)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich SML1524 (+)-JQ1 ≥98% (HPLC) 1268524-70-4 5mg $159 2018-11-13 Buy
Sigma-Aldrich SML1524 (+)-JQ1 ≥98% (HPLC) 1268524-70-4 25mg $582 2018-11-13 Buy
Cayman Chemical 11187 (+)-JQ1 ≥98% 1268524-70-4 1mg $39 2018-11-13 Buy
Cayman Chemical 11187 (+)-JQ1 ≥98% 1268524-70-4 5mg $146 2018-11-13 Buy
Cayman Chemical 11187 (+)-JQ1 ≥98% 1268524-70-4 10mg $215 2018-11-13 Buy

(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,Uses,Production

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.

(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 Preparation Products And Raw materials

Raw materials

Preparation Products


(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 Suppliers

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Jilin Province Yanshen Technology Co., Ltd.
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View Lastest Price from (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 manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-08-15 (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
1268524-70-4
US $1.00 / KG 1G 98% 100KG career henan chemical co

1268524-70-4((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)Related Search:


  • 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
  • (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
  • (+)-JQ1, >=99%
  • (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]
  • tert-butyl (S)-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
  • jq01
  • (S)-tert-Butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno-[3,2-f][1,2,4]triazolo[4,3-a][1
  • S-JQ1
  • -
  • (+)-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:
  • 1268524-70-4
  • Epigenetics
  • Apis
  • Inhibitors
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