(+)-JQ-1 (Synonyms: JQ1)

Cat. No.: HY-13030 Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

(+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC₅₀s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy.

For research use only. We do not sell to patients.

(+)-JQ-1 Chemical Structure

CAS No. : 1268524-70-4

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10 mM * 1 mL in DMSO	USD 77	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 212 publication(s) in Google Scholar

Other Forms of (+)-JQ-1:

(R)-(-)-JQ1 Enantiomer In-stock
JQ-1 (carboxylic acid) In-stock

183 Publications Citing Use of MCE (+)-JQ-1

IHC

: (+)-JQ-1 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2022 Nov 11;41(1):321. [Abstract]; The expression of BRD4 and MYC proteins are each downregulated by JQ1 (0.5 µM; 24 h) or panobinostat (PAN; 10 nM; 24 h) alone, and more profoundly by the combination of these two inhibitors in in MB HD-MB03 and D-283 cells.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Res. 2019 Jan 1;79(1):251-262. [Abstract]; Cleavage of PARP is assessed by western blotting with the treatment of JQ 1.

: (+)-JQ-1 purchased from MCE. Usage Cited in: EBioMedicine. 2019 Jun;44:419-430. [Abstract]; Immunoblots (IB) are done to detect γH2AX and DNA repair proteins, Ku80 and RAD51 using UAB-PA4 or UAB-PA16 tumors harvested from mice 24 h following final treatment. Quantitation by densitometry of results is shown below each IB image.

: (+)-JQ-1 purchased from MCE. Usage Cited in: EBioMedicine. 2019 Jun;44:419-430. [Abstract]; Panc1 or MiaPaCa2 cells are exposed to JQ1 (0.5, 1, 5, or 10 μM) for 48 h, and immunoblotted for γH2AX.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Eur J Pharm Biopharm. 2019 Jan;134:96-106. [Abstract]; Western blot of cleaved Caspase-3 and cleaved PARP-1 in AML cells with the treatment of NL101 and BMN673.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Eur J Pharm Biopharm. 2019 Jan;134:96-106. [Abstract]; Western blot analysis of p21 and G2/M regulatory molecules, cyclin B1, CDC2, p-CDC2 (Tyr-15) and CDC25A in the treatment of NL101 and BMN673.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Cell. 2018 Sep 20;175(1):186-199.e19. [Abstract]; Cells are treated with EPZ-6438 (1 μM) or GSK126 (1 μM) for 6 days. Protein levels are analyzed by immunoblotting. Cells are treated with EPZ-6438 (1 μM), JQ1 (0.25 μM) alone or combination for 6 days. Protein levels are analyzed by immunoblotting.

: (+)-JQ-1 purchased from MCE. Usage Cited in: EMBO Mol Med. 2018 Apr;10(4). pii: e8163. [Abstract]; Western blot analysis of MYC and FGFR3 expression in lysates from MGH-U3 and RT112 cells treated with (+)-JQ1 (1 or 4 μM) for 48 h. Anti-actin antibody is used as a loading control. Pan-FGFR inhibitor, PD173074 (50 nM and 1 μM), and inactive enantiomer (-)-JQ1 (4 μM) are used as controls.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Lett. 2018 Oct 28;435:44-54. [Abstract]; H157, H1299, and HCT116 cells are harvested for preparation of whole-cell protein lysates and subsequent Western blotting to detect the indicated proteins.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Lett. 2018 Apr 28;420:195-207. [Abstract]; Shh-Light 2 cells are transfected with Gli1 or Gli2 plasmids and the expression of proteins are analyzed by Western blot. Positive control JQ1, CBC and CBD inhibit Gli1 and Gli2 overexpression induced Gli luciferase activity, GDC-0499 and GANT61 have no effects.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Lett. 2018 Apr 10;419:64-74. [Abstract]; ESCC cell lines are treated with 500 nM JQ1 for 48 h, whole cell lysates are analyzed by western blotting. The expressions of p21 and p27 are further upregulated by JQ1 concomitant with cell cycle arrest at G1 phase.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129. [Abstract]; The effects of treatment with the indicated epigenetic inhibitors on cleaved PARP (Clv-PARP) expression in both PC9/ER and HCC827/ER cells. β-actin is used as a loading control.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Oncogene. 2018 Aug;37(33):4611-4625. [Abstract]; ARID1A Western blot analysis of ARID1A protein levels in the ES2 polyclonal ARID1A knockout clone and ES2/OVCA429 monoclonal ARID1A knockout clones.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Oncogene. 2018 Aug;37(33):4611-4625. [Abstract]; The OVCA429 cells are subjected to Western blot analysis for the indicated proteins. ACTIN servea as a loading control.

: (+)-JQ-1 purchased from MCE. Usage Cited in: J Med Chem. 2018 Jan 25;61(2):504-513. [Abstract]; Protein degradation profile of VHL-based BET degraders. Sub-confluent HeLa cells are treated for 24 h with varying concentration of test compounds JQ1(Compound 3), I-BET726 (Compound 4). Protein extracts are separated by SDS-PAGE and then analyzed by Western blot. Proteins Brd4, Brd3, Brd2 and β-actin are probed for JQ1and I-BET726 with specific antibodies.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Oct;156:511-523. [Abstract]; Western blot detection of the p-TEFb component CDK9, Cyclin T1 and CDK9 phosphorylation on Thr186, as well as its downstream RNA poly II CTD and phosphate CTD after J-Lat 10.6 cells are treated with PR-957 in dose-dependent manner.

: (+)-JQ-1 purchased from MCE. Usage Cited in: J Mol Cell Cardiol. 2018 Dec 7;127:83-96. [Abstract]; The expression of EndMT-related proteins, VE-cadherin, CD31, vimentin, α-SMA and FSP1, were compared among Ctrl, JQ1(-), JQ1, TGF-β1, and TGF-β1+JQ1 groups in both HUVECs and MAECs.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Sci Rep. 2018 Aug 1;8(1):11554. [Abstract]; A549 cells are mock-treated (0.1% DMSO in culture medium) or treated with RVX-208 at 500 nM, PFI-1 at 500 nM, JQ1 at 300 nM, or with 300 nM (-)-JQ1, an inactive enantiomer of JQ1. The cells are then infected with Ad2 at 1 PFU/cell for 24 h. Viral hexon and penton base (PB) protein is detected by immunoblotting analysis.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Biol Ther. 2018 May 4;19(5):407-415. [Abstract]; NSCLC cells are treated with 0-8 μM JQ1 for 24h, then the whole-cell lysates are prepared and subjected to western blot assay.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Oncotarget. 2018 May 1;9(33):23003-23017. [Abstract]; The expression of MYC protein is markedly repressed in JQ1-treated ccRCC cells (2.5 and 5 μM) in comparison with that in mock cells. β-Actin is used as a loading control. Densitometry analyses using ImageJ software are performed.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Leukemia. 2017 Oct;31(10):2037-2047. [Abstract]; Immunoprecipitation with anti-BIM antibody illustrates the increased binding of BIM to BCL-2 after JQ1 treatment.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Lett. 2017 Aug 28;402:100-109. [Abstract]; Expression and activation statuses of signal proteins in three BRAFV600E-mutant colon cancer cell lines treated with either RG7204, JQ1, or their combination. Phosphorylation of CRAF and AKT is suppressed by JQ1 in RKO cells and possibly in Colo205 cells (green arrow heads).

: (+)-JQ-1 purchased from MCE. Usage Cited in: Genome Res. 2017 Nov;27(11):1830-1842. [Abstract]; Ki67 immunohistochemistry and H&E stained sections from representative xenograft per treatment arm. A marked decrease in the proliferation marker Ki67 is observed in xenografts treated with JQ1.

: (+)-JQ-1 purchased from MCE. Usage Cited in: J Cell Biochem. 2017 Aug;118(8):2182-2192. [Abstract]; JQ1 induces G0/G1 cell cycle arrest and apoptosis of chondrosarcoma cells via regulating p21, p27, Cyclin E2, and Cyclin D1 expression. (A and B) JQ1 regulates the expression of cell cycle regulators such as p21, p27, Cyclin E2, and Cyclin D1. SW 1353 and Hs 819.T cells are seeded into a 6-well plate for 72 h, then the cells are treated with different concentrations of JQ1 (JQ1#1: 200 nM; JQ1#2: 2 μM; JQ1#3: 20 μM) for another 24 h. Total cell lysate is used for the analysis of protein expressio

: (+)-JQ-1 purchased from MCE. Usage Cited in: Metabolism. 2016 Oct;65(10):1478-88. [Abstract]; The BRD4 protein level in the liver is significantly suppressed by force-feeding fructose or glucose with (+)-JQ1. Protein levels of Brd4 in the liver of mice force-fed with glucose or fructose, with or without (+)-JQ1. Quantification of protein levels is performed by normalization against the level of β-actin (n = 6).

: (+)-JQ-1 purchased from MCE. Usage Cited in: PLoS Pathog. 2016 Oct 20;12(10):e1005950. [Abstract]; Dose effect of JQ1 on HSV infection. Vero cells are treated with JQ1 at concentrations as indicated. HSV-1 or HSV-2 at 1 MOI are used. The samples are used for protein expression analysis by western blot.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Mol Cancer Ther. 2016 Jun;15(6):1217-26. [Abstract]; JQ1-mediated c-MYC repression correlates with growth inhibition. BETi preferentially inhibit c-MYC protein expression in sensitive cell lines. JQ1-sensitive GP5D, HT29 and LIM1215 cells and JQ1-resistant KM12, SW480 and HuTu80 cells where treated with JQ1 (500 nM) for 2-24 hours and c-MYC protein expression determined by western blot.

: (+)-JQ-1 purchased from MCE. Usage Cited in: J Biol Chem. 2016 Nov 4;291(45):23756-23768. [Abstract]; BET inhibition blocks growth of TNBC cells without consistently downregulating MYC. Western blot analysis of MYC expression levels in TNBC cell lines treated for 24 hours with vehicle or 500 nM JQ1. Values on the western blot are relative to the vehicle-treated 1143 sample following normalization to β-actin.

: (+)-JQ-1 purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2016 Dec;1859(12):1527-1537. [Abstract]; JQ1 treatment decreases β-catenin levels in HCT116 cells, but increases TAZ protein. When cells reach confluence, they are serum-starved overnight and pretreated with DMSO or JQ1 (500 nM) for 1 hour, followed by growth medium (containing 10% serum) stimulation for 24 hours.

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Description

(+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC₅₀s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2))^[1]. (+)-JQ-1 also activates autophagy^[2].

IC₅₀ & Target

IC50: 77/33 nM (BRD4(1/2))^[1]

In Vitro

(+)-JQ-1 represents a potent, highly specific and Kac competitive inhibitor for the BET family of bromodomains. (+)-JQ-1 (100 nM, 48 h) prompts squamous differentiation exhibited by cell spindling, flattening and increased expression of keratin. (+)-JQ-1 (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.(+)-JQ-1 (250 nM) elicits a time-dependent induction of strong (3+) keratin staining of treated NMC 797 cells, compared to (-)-JQ1 (250 nM)^[1]. De-repression of autophagy genes is observed almost immediately after (+)-JQ-1 addition^[2]. (+)-JQ-1 is a potent thienodiazepine inhibitor (K_d=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 (+)-JQ-1 demonstrates potent inhibition of H4Kac4 binding with a IC₅₀ value of 10 nM for murine BRDT(1) and 11 nM for human BRDT(1)^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 hr*ng/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 (C_max=1180 ng/mL) and drug exposure (AUC=2090 hr*ng/mL)^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

456.99

Appearance

Solid

Formula

C₂₃H₂₅ClN₄O₂S

CAS No.

1268524-70-4

SMILES

O=C(C[C@H]1C2=NN=C(N2C3=C(C(C4=CC=C(C=C4)Cl)=N1)C(C)=C(S3)C)C)OC(C)(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : ≥ 45 mg/mL (98.47 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1882 mL	10.9412 mL	21.8823 mL
5 mM	0.4376 mL	2.1882 mL	4.3765 mL
10 mM	0.2188 mL	1.0941 mL	2.1882 mL

*Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.47 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.47 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.47 mM); Clear solution

*All of the co-solvents are available by MCE.

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (287 KB) SDS (252 KB)

COA (258 KB) HNMR (165 KB) LCMS (367 KB) Elemental Analysis Report (116 KB)

Handling Instructions (2659 KB)

References

[1]. Filippakopoulos P, et al. Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73. [Content Brief]

[2]. Sakamaki JI, et al. Bromodomain Protein BRD4 Is a Transcriptional Repressor of Autophagy and LysosomalFunction. Mol Cell. 2017 May 18;66(4):517-532.e9. [Content Brief]

[3]. Matzuk MM, et al. Small-molecule inhibition of BRDT for male contraception. Cell. 2012 Aug 17;150(4):673-84. [Content Brief]

Cell Assay ^[1]	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. 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]^[3]	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. Rats^[3] 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Filippakopoulos P, et al. Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73. [Content Brief] [2]. Sakamaki JI, et al. Bromodomain Protein BRD4 Is a Transcriptional Repressor of Autophagy and LysosomalFunction. Mol Cell. 2017 May 18;66(4):517-532.e9. [Content Brief] [3]. Matzuk MM, et al. Small-molecule inhibition of BRDT for male contraception. Cell. 2012 Aug 17;150(4):673-84. [Content Brief]

(+)-JQ-1 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

(+)-JQ-11268524-70-4JQ1JQ 1JQ-1Epigenetic Reader DomainAutophagyLigands for Target Protein for PROTACTarget Protein-binding MoietyInhibitorinhibitorinhibit

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(+)-JQ-1 (Synonyms: JQ1)

Customer Review

Other Forms of (+)-JQ-1:

(+)-JQ-1 Related Antibodies

183 Publications Citing Use of MCE (+)-JQ-1

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References

Customer Review

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