(+)-JQ1

Modify Date: 2026-07-12 20:18:37

(+)-JQ1 structure	Common Name	(+)-JQ1
	CAS Number	1268524-70-4	Molecular Weight	456.988
	Density	1.3±0.1 g/cm3	Boiling Point	610.4±65.0 °C at 760 mmHg
	Molecular Formula	C₂₃H₂₅ClN₄O₂S	Melting Point	N/A
	MSDS	USA	Flash Point	322.9±34.3 °C

Use of (+)-JQ1

(+)-JQ-1 is a BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)).

This table lists Chinese names, IUPAC names and various aliases of this chemical substance.

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
Synonym	More Synonyms

This table contains bioactivity, target information and biological‑assay experimental data of this compound.

Description	(+)-JQ-1 is a BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)).
Related Catalog	Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain Research Areas >> Cancer
Target	IC50: 77/33 nM (BRD4(1/2))[1]
In Vitro	(+)-JQ1 represents a potent, highly specific and Kac competitive inhibitor for the BET family of bromodomains. (+)-JQ1 (100 nM, 48 h) prompts squamous differentiation exhibited by cell spindling, flattening and increased expression of keratin. (+)-JQ1 (250 nM) induces rapid expression of keratin in treated NMC 797 cells compared to (-)-JQ1 (250 nM) and vehicle controls, as determined by quantitative immunohistochemistry.(+)-JQ1 (250 nM) elicits a time-dependent induction of strong (3+) keratin staining of treated NMC 797 cells, compared to (-)-JQ1 (250 nM)[1]. (+)-JQ1 is a potent thienodiazepine inhibitor (Kd=90 nM) of the BET family coactivator protein BRD4, which is implicated in the pathogenesis of cancer via transcriptional control of the MYC oncogene. Dose-ranging studies of (+)-JQ1 demonstrates potent inhibition of H4Kac4 binding with a IC50 value of 10 nM for murine BRDT(1) and 11 nM for human BRDT(1)[2].
In Vivo	Matched cohorts of mice with established tumors are randomized to treatment with (+)-JQ1 (50 mg/kg) or vehicle, administered by daily intraperitoneal injection. Prior to randomization, and after four days of therapy, mice are evaluated by FDG-PET imaging. A marked reduction in FDG uptake is observed with (+)-JQ1 treatment. Tumor-volume measurements confirm a reduction in tumor growth with JQ1 treatment. Pharmacokinetic studies of (+)-JQ1 are performed in CD1 mice following intravenous and oral administration. Mean plasma concentration-time profiles of (+)-JQ1 after intravenous dosing (5 mg/kg). The pharmacokinetic parameters for intravenous (+)-JQ1 demonstrate excellent drug exposure (AUC=2090 hrng/mL) and an approximately one hour half-life (T1/2). Mean plasma concentration-time profiles of (+)-JQ1 after oral dosing (10 mg/kg). The pharmacokinetic parameters for oral (+)-JQ1 demonstrate excellent oral bioavailability (F=49%), peak plasma concentration (Cmax=1180 ng/mL) and drug exposure (AUC=2090 hrng/mL)[1].
Cell Assay	NUT midline carcinoma patient cell lines (797 and 11060) are plated in T-25 flasks and grown in DMEM (797) or RPMI (11060) containing 10 % fetal bovine serum and 1 % Penicillin/Streptomycin. Cells are treated with either 250 nM (+)-JQ1, 250 nM (-)-JQ1 or the equivalent volume of DMSO (0.025%). At the desired time point, 2×106 cells are spun at 500× g for 5 minutes at 4°C and washed with PBS. Pellets are resuspended in 1 mL of cold PBS and added dropwise while gently vortexing to 9 mL 70 % ethanol in a 15 mL polypropylene centrifuge tube. Fixed cells are then frozen at -20°C overnight. The next day, cells are centrifuged at 500× g for 10 minutes at 4°C and washed with 3 mL of cold PBS. Cells are resuspended in 500 μL of propidium iodide staining solution (0.2 mg/mL RNAse A, 0.02 mg/mL propidium iodide, 0.1 % Triton-X in PBS) and incubated for 20 minutes at 37°C. Samples are then transferred to ice and analyzed on a BD FACS Canto II. Histograms are generated and cell cycle analysis is performed using FlowJo flow cytometry analysis software[1].
Animal Admin	Mice[1] Matched cohorts of mice with established tumors are randomized to treatment with (+)-JQ1 (50 mg/kg) or vehicle, administered by daily intraperitoneal injection. Male CD1 mice (24-29 g) are treated with a single dose of (+)-JQ1 at 5 mg/kg for intravenous tail vein injection studies and 10 mg/kg for oral gavage studies. Approximately 150 μL of blood are taken from animals by retro-orbital puncture under anesthesia with Isoflurane into EDTA tubes at pre-specified time intervals: 0.033, 0.083, 0.25, 0.5, 1, 2, 4, 5, 8 and 24 hours. Three animals are analyzed per time point. Blood samples are put on ice and centrifuged to obtain plasma samples (2000× g, 5 min under 4°C) within 15 minutes post-sampling. Plasma samples are stored at approximately -70°C until analysis is performed. Mice are provided free access to food and water throughout the study. Rats[2] Adult male Sprague-Dawley rats are treated with vehicle or (+)-JQ1 (10 mg/kg). Treatment is administered IP at 1/100 body mass. Rats are checked twice-daily for mortality and weighed on days 1, 3, 7, 14, and 21. The treatment regimen utilized 4 days of 50 mg/kg JQ1 administered daily which is decreased to 10 mg/kg twice daily for the remainder of the study due to the appearance of adverse effects in a subset of animals. For all animals completing 3 weeks of treatment, testis mass, sperm motility, and sperm counts are determined as described for mouse studies. In brief, testes are fixed in Bouin’s and prepared for histology. The other half is minced in warm M16 buffer and used for sperm counts and motility studies.
References	[1]. Filippakopoulos P, et al. Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73. [2]. Matzuk MM, et al. Small-molecule inhibition of BRDT for male contraception. Cell. 2012 Aug 17;150(4):673-84. [3]. Peirs S, et al. Targeting BET proteins improves the therapeutic efficacy of BCL-2 inhibition in T-cell acute lymphoblastic leukemia. Leukemia. 2017 Feb 3. [4]. T?gel L, et al. Dual Targeting of Bromodomain and Extraterminal Domain Proteins, and WNT or MAPK Signaling, Inhibits c-MYC Expression and Proliferation of Colorectal Cancer Cells. Mol Cancer Ther. 2016 Jun;15(6):1217-26. [5]. Sahni JM, et al. Bromodomain and Extraterminal Protein Inhibition Blocks Growth of Triple-negative Breast Cancers through the Suppression of Aurora Kinases. J Biol Chem. 2016 Nov 4;291(45):23756-23768. [6]. Nakamura Y, et al. Targeting of super-enhancers and mutant BRAF can suppress growth of BRAF-mutant colon cancer cells via repression of MAPK signaling pathway. Cancer Lett. 2017 Aug 28;402:100-109. [7]. Bhattacharyya S, et al. Altered hydroxymethylation is seen at regulatory regions in pancreatic cancer and regulates oncogenic pathways. Genome Res. 2017 Nov;27(11):1830-1842. [8]. Lv B, et al. Enhancement of adenovirus infection and adenoviral vector-mediated gene delivery by bromodomain inhibitor JQ1. Sci Rep. 2018 Aug 1;8(1):11554. doi: 10.1038/s41598-018-28421-x. [9]. Huang X, et al. Targeting Epigenetic Crosstalk as a Therapeutic Strategy for EZH2-Aberrant Solid Tumors. Cell. 2018 Sep 20;175(1):186-199.e19. doi: 10.1016/j.cell.2018.08.058. Epub 2018 Sep 13.

This table shows physicochemical parameters including melting point, boiling point, density, solubility and optical rotation. Missing data is marked as N/A.

Density	1.3±0.1 g/cm3
Boiling Point	610.4±65.0 °C at 760 mmHg
Molecular Formula	C₂₃H₂₅ClN₄O₂S
Molecular Weight	456.988
Flash Point	322.9±34.3 °C
Exact Mass	456.138672
PSA	97.61000
LogP	4.49
Appearance of Characters	white to beige
Vapour Pressure	0.0±1.7 mmHg at 25°C
Index of Refraction	1.657
InChIKey	DNVXATUJJDPFDM-KRWDZBQOSA-N
SMILES	Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=NC(CC(=O)OC(C)(C)C)c1nnc(C)n1-2
Storage condition	2-8°C
Water Solubility	DMSO: soluble20mg/mL, clear

This table covers safety warnings, protective measures, incompatible substances and disposal guidelines for this compound.

RIDADR	NONH for all modes of transport

This table presents publicly reported synthetic routes, reaction conditions, reactants and product information of the compound.

1H-Thieno[2,3-e...

CAS#:1268524-67-9

Acethydrazide

CAS#:1068-57-1

~90%

(+)-JQ1

CAS#:1268524-70-4

Learn More

Literature: WO2011/143657 A1, ; Page/Page column 82-83 ;

(2-amino-4,5-di...

CAS#:50508-66-2

(+)-JQ1

CAS#:1268524-70-4

Learn More

Literature: WO2011/143657 A1, ;

4-Chlorobenzoyl...

CAS#:4640-66-8

(+)-JQ1

CAS#:1268524-70-4

Learn More

Literature: WO2011/143657 A1, ;

2-Methyl-2-prop...

CAS#:1268524-65-7

(+)-JQ1

CAS#:1268524-70-4

Learn More

Literature: WO2011/143657 A1, ;

Butanoic acid, ...

CAS#:1268524-66-8

(+)-JQ1

CAS#:1268524-70-4

Learn More

Literature: WO2011/143657 A1, ;

This table lists upstream starting materials and downstream derivative products related to this chemical.

Precursor 4
CAS#:1268524-67-9 1H-Thieno[2,3-e... CAS#:1068-57-1 Acethydrazide CAS#:50508-66-2 (2-amino-4,5-di... CAS#:4640-66-8 4-Chlorobenzoyl...
DownStream 0

This table lists relevant public references with title, journal and publication metadata for this compound.

Epigenetic chemical probes. Müller S and Brown PJ

Clin. Pharmacol. Ther. 92(6) , 689-93, (2012)

This table contains target information, in‑vitro & in‑vivo assay data for this compound.

Name: Primary qHTS assay for inhibitors of alpha-synuclein gene (SNCA) expression
Source: NCGC
External Id: SNCA-p-activity-luciferase

Name: Antiproliferative activity against human TY82 cells after 72 hrs by CCK8 assay
Source: ChEMBL
Target: N/A
External Id: CHEMBL4130834

Name: Thermal Shift Assay. Domain: start/stop: E122-S403
Source: ChEMBL
Target: Aurora kinase A
External Id: CHEMBL5067447

Name: Ratio of drug concentration in unbound HEK293 cell to media
Source: ChEMBL
Target: N/A
External Id: CHEMBL4312051

Name: Permeability of compound in 5% DMSO after 7 hrs by PAMPA
Source: ChEMBL
Target: N/A
External Id: CHEMBL4312050

Name: Inhibition of BRD4 in human H1229 cells transfected with HPV-E2 assessed as transrepr...
Source: ChEMBL
Target: Bromodomain-containing protein 4
External Id: CHEMBL4312049

Name: Inhibition of BRD4 in human MX1 cells assessed as decrease in cell proliferation afte...
Source: ChEMBL
Target: Bromodomain-containing protein 4
External Id: CHEMBL4312048

Name: Inhibition of BRD4 (unknown origin) by TR-FRET assay
Source: ChEMBL
Target: Bromodomain-containing protein 4
External Id: CHEMBL4312047

Name: Inhibition of BRD3 (unknown origin) by TR-FRET assay
Source: ChEMBL
Target: Bromodomain-containing protein 3
External Id: CHEMBL4312046

Name: Inhibition of BRD2 (unknown origin) by TR-FRET assay
Source: ChEMBL
Target: Bromodomain-containing protein 2
External Id: CHEMBL4312045

Total 3350, Current Page 1 of 335

This table collects all English aliases, systematic names and CAS‑related synonyms of the compound.

(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

JQ1

2-Methyl-2-propanyl [(6S)-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

UNII-1MRH0IMX0W

(+)-JQ-1

This section contains frequently‑asked‑questions about this compound, including basic parameters, properties, storage conditions and corresponding answers.

Q: What is the LogP of (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?

A: LogP of (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 is 4.49.

Q: What is the boiling point of (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?

A: Boiling point of (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 is 610.4±65.0 °C at 760 mmHg.

Q: What is the polar surface area (PSA) of (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?

A: Polar surface area (PSA) of (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 is 97.61000.

Q: What is the molecular weight of (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?

A: Molecular weight of (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 is 456.988.

Q: What is the molecular formula of (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?

A: Molecular formula of (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 is C23H25ClN4O2S.

Q: What is the SMILES notation of (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?

A: SMILES notation of (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 is Cc1sc2c(c1C)C(c1ccc(Cl)cc1)=NC(CC(=O)OC(C)(C)C)c1nnc(C)n1-2.

Q: How is the water solubility of (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?

A: Water solubility of (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: DMSO: soluble20mg/mL, clear.

Q: What English synonyms does (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 have?

A: English synonyms of (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: (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, JQ1, 2-Methyl-2-propanyl [(6S)-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, UNII-1MRH0IMX0W, (+)-JQ-1.

Q: What is the English name of (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?

A: The English name of (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 is (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.

Q: What is the CAS number of (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?

A: CAS number of (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 is 1268524-70-4.

This table lists manufacturers and suppliers of this compound, including vendor names and product supply reference information.

Shanghai Nianxing Industrial Co., Ltd

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.

Shanghai Nianxing Industrial Co., Ltd
China
Product Name: (+)-JQ1
Price: Check
Purity: 99.0%
Delivery: 10 Day
Contact: Yang
Email: sales@echemcloud.com

Get all suppliers and price by the below link:

(+)-JQ1 suppliers

Price: $92/10mM*1mLinDMSO

Reference only. check more (+)-JQ1 price

(+)-JQ1

Use of (+)-JQ1

Names

(+)-JQ1 Biological Activity

Chemical & Physical Properties

Safety Information

Synthetic Route

Precursor & DownStream

Articles1

(+)-JQ1Bioassay

Synonyms

(+)-JQ1 | FAQ

(+)-JQ1factory

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.