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JQ1 (+)

Inh 1268524-70-4 (6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid 1,1-dimethylethyl ester

1 image

Catalog No. ABIN7233264

Datasheet as PDF

Application

Inhibition (Inh)

Purpose

Bromodomain inhibitor

Characteristics

JQ1 (+) is a potent BET bromodomain inhibitor and is the active isomer. IC50 = 17.7, 32.6, 76.9 and 12942 nM respectively for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP respectively (data for + isomer). Competitive binding by JQ1 displaces the BRD4 fusion oncoprotein from chromatin, prompting squamous differentiation and specific antiproliferative effects in BRD4-dependent cell lines and patient-derived xenograft models. Induces squamous differentiation in NMC cell lines and inhibits tumor growth in NMC xenografts. Displays reversible contraceptive effects in male mice. Blocks inflammation and bone loss in periodontitis. Reverses CAR T cell extinction.

Purity

>98 %

Chemical Name

(6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid 1,1-dimethylethyl ester

Formula

C23H25ClN4O2S

Solubility

Soluble in DMSO (up to 60 mg/ml) or in Ethanol (up to 46 mg/ml)
Geldanamycin
Inh 30562-34-6 (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-13-hydroxy-8,14,19-trimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1] docosa-1(21),4,6,10,18-pentaen-9-yl carbamate

Radicicol
Inh 12772-57-5

Geldanamycin- FITC
Inh 30562-34-6 (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-13-hydroxy-8,14,19-trimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1] docosa-1(21),4,6,10,18-pentaen-9-yl carbamate

Nicotinamide
Inh 98-92-0 Pyridine-3-carboxylic acid amide

5-Azacytidine
Inh Cell-permeable 320-67-2 4-Amino-1-ß-D-ribofuranosyl-1,3,5-triazin-2(1H)-one

SAHA (Vorinostat)
Inh Cell-permeable 149647-78-9 Suberoylanilide-hydroxamic acid

Phenylbutyrate Na
Inh 1716-12-7 4-Phenylbutyric acid, sodium salt

CI-994
Inh 112522-64-2 4-(Acetylamino)-N-(2-aminophenyl)benzamide

Tranylcypromine hemisulfate (±)
Inh Cell-permeable 13492-01-8 Trans (±)-2-phenylcyclopropanamine, hemisulfate salt

Tenovin-1
Inh 380315-80-0 N-[(4-Acetamidophenyl)carbamothioyl]-4-tert-butylbenzamide

Restrictions

For Research Use only
Format

Powder

Precaution of Use

GHS – Classification
Not a hazardous substance or mixture

Storage

RT
Background

Epigenetics,Proliferation,Bromodomain,Inflammation,Cancer,Posttranslational modification,Chromatin

Molecular Weight

457.0

CAS-No

1268524-70-4