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

Name: (+)-JQ-1
Brand: MedChemExpress
SKU: HY-13030
Rating: 5.0 (259 reviews)

Cat. No.: HY-13030 Purity: 99.90%: FAQs
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(+)-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 ready for reconstitution	USD 77	In-stock	Estimated Time of Arrival: December 31
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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 259 publication(s) in Google Scholar

Other Forms of (+)-JQ-1:

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

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

IHC

: (+)-JQ-1 purchased from MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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]

Cellular Effect

Cell Line	Type	Value	Description	References
697	EC₅₀	0.09 μM Compound: 1; (+)-JQ1	Cytotoxicity against human 697 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay Cytotoxicity against human 697 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	[PMID: 29170024]
A-375	IC₅₀	7.5 μM Compound: (+)-JQ1	Antiproliferative activity against human A375 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human A375 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
A549	IC₅₀	1.67 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human A549 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human A549 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
A549	IC₅₀	13.1 μM Compound: (+)-JQ1	Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
A549	EC₅₀	17 μM Compound: (+)-JQ1	Cytotoxicity against human A549 cells assessed as viable cells incubated for 23 hrs by alamar blue assay Cytotoxicity against human A549 cells assessed as viable cells incubated for 23 hrs by alamar blue assay	[PMID: 35007061]
ASPC1	IC₅₀	3.39 μM Compound: JQ1	Antiproliferative activity against human ASPC1 cells assessed as cell growth inhibition incubated for 6 days by MTS assay Antiproliferative activity against human ASPC1 cells assessed as cell growth inhibition incubated for 6 days by MTS assay	[PMID: 35500243]
CAPAN-1	IC₅₀	0.45 μM Compound: (+)-JQ1	Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 7 days by MTT assay Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 7 days by MTT assay	[PMID: 35091172]
CAPAN-1	IC₅₀	0.58 μM Compound: (+)-JQ1	Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 5 days by MTT assay Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 5 days by MTT assay	[PMID: 35091172]
CAPAN-1	IC₅₀	2.44 μM Compound: (+)-JQ1	Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 4 days by MTT assay Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 4 days by MTT assay	[PMID: 35091172]
CAPAN-1	IC₅₀	2.44 μM Compound: JQ-1	Antiproliferative activity against human CAPAN-1 cells assessed as reduction in cell viability after 4 days by MTT assay Antiproliferative activity against human CAPAN-1 cells assessed as reduction in cell viability after 4 days by MTT assay	[PMID: 34813314]
CAPAN-1	IC₅₀	24.1 μM Compound: (+)-JQ1	Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 3 days by MTT assay Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 3 days by MTT assay	[PMID: 35091172]
CFPAC-1	IC₅₀	0.35 μM Compound: (+)-JQ1	Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 7 days by MTT assay Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 7 days by MTT assay	[PMID: 35091172]
CFPAC-1	IC₅₀	1.56 μM Compound: JQ-1	Antiproliferative activity against human CFPAC-1 cells assessed as reduction in cell viability after 4 days by MTT assay Antiproliferative activity against human CFPAC-1 cells assessed as reduction in cell viability after 4 days by MTT assay	[PMID: 34813314]
CFPAC-1	IC₅₀	1.56 μM Compound: (+)-JQ1	Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 5 days by MTT assay Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 5 days by MTT assay	[PMID: 35091172]
CFPAC-1	IC₅₀	1.86 μM Compound: (+)-JQ1	Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 4 days by MTT assay Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 4 days by MTT assay	[PMID: 35091172]
CFPAC-1	IC₅₀	13.9 μM Compound: (+)-JQ1	Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 3 days by MTT assay Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 3 days by MTT assay	[PMID: 35091172]
CT26	IC₅₀	28.67 μM Compound: 1; JQ1	Antiproliferative activity against human CT26 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Antiproliferative activity against human CT26 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 33862375]
CWR22R	IC₅₀	0.033 μM Compound: 1, JQ1	Antiproliferative activity against human 22Rv1 cells assessed as inhibition of cell growth incubated for 96 to 120 hrs by celltiter glo assay Antiproliferative activity against human 22Rv1 cells assessed as inhibition of cell growth incubated for 96 to 120 hrs by celltiter glo assay	[PMID: 34999525]
CWR22R	IC₅₀	0.071 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human 22Rv1 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human 22Rv1 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
CWR22R	IC₅₀	0.071 μM Compound: 1; (+)-JQ1	Antiproliferative activity against human 22Rv1 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay Antiproliferative activity against human 22Rv1 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay	[PMID: 29541371]
DU-145	IC₅₀	2.52 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human DU145 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human DU145 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
DU-145	IC₅₀	2.52 μM Compound: 1; (+)-JQ1	Antiproliferative activity against human DU145 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay Antiproliferative activity against human DU145 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay	[PMID: 29541371]
HCT-116	IC₅₀	2.03 μM Compound: (+)-JQ1	Antiproliferative activity against BRCA2-mutated human HCT-116 cells assessed as inhibition of cell growth measured after 7 days by MTT assay Antiproliferative activity against BRCA2-mutated human HCT-116 cells assessed as inhibition of cell growth measured after 7 days by MTT assay	[PMID: 35091172]
HCT-116	IC₅₀	4.212 μM Compound: 1; JQ1	Antiproliferation activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferation activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33214826]
HEK-293T	IC₅₀	107 nM Compound: JQ1	Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay	[PMID: 34710325]
HeLa	IC₅₀	> 100 μM Compound: 1, (+)-JQ1	Cytotoxicity against human HeLa cells after 24 hrs by WST-1 assay Cytotoxicity against human HeLa cells after 24 hrs by WST-1 assay	[PMID: 23517011]
HeLa	IC₅₀	3.76 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human HeLa cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human HeLa cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
HepG2	IC₅₀	11.3 μM Compound: (+)-JQ1	Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
HepG2	IC₅₀	18.39 μM Compound: 1; JQ1	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 33862375]
HFL1	IC₅₀	0.29 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against HFL1 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against HFL1 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
HL-60	GI₅₀	0.021 μM Compound: 15; (+)-JQ1	Growth inhibition of human HL60 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay Growth inhibition of human HL60 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay	[PMID: 33275431]
HL-60	IC₅₀	0.06 μM Compound: 1; (+)-JQ1	Antiproliferative activity against human HL60 cells after 72 hrs by CCK8 assay Antiproliferative activity against human HL60 cells after 72 hrs by CCK8 assay	[PMID: 26731490]
HL-60	IC₅₀	0.11 μM Compound: (+)-JQ1	Antiproliferative activity against BRD4-sensitive human HL60 cells after 72 hrs by CCK8 assay Antiproliferative activity against BRD4-sensitive human HL60 cells after 72 hrs by CCK8 assay	[PMID: 28314513]
HL-60	IC₅₀	0.16 μM Compound: 1; (+)-jQ1	Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK8 assay	[PMID: 32883643]
HL-60	EC₅₀	0.2 μM Compound: (+)-JQ1	Induction of ATRA-induced human HL60 cell differentiation pretreated for 1 hr followed by ATRA addition measured after 3 days by Wright-Giemsa staining based microscopic analysis Induction of ATRA-induced human HL60 cell differentiation pretreated for 1 hr followed by ATRA addition measured after 3 days by Wright-Giemsa staining based microscopic analysis	[PMID: 28549889]
HL-60	IC₅₀	0.87 μM Compound: 2; JQ1	Antiproliferative activity against human HL60 cells assessed as reduction in cell viability by MTT assay Antiproliferative activity against human HL60 cells assessed as reduction in cell viability by MTT assay	[PMID: 31857846]
HL-60	IC₅₀	2.91 μM Compound: (+)-JQ-1	Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK-8 assay	[PMID: 31079968]
HL-60	IC₅₀	3.46 μM Compound: (+)-JQ-1	Antiproliferative activity against human HL60 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HL60 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 32631570]
HL-60	IC₅₀	5.3 μM Compound: 3; (+)-JQ1	Cytotoxicity against human HL60 cells assessed as decrease in cell viability after 24 hrs by MTT assay Cytotoxicity against human HL60 cells assessed as decrease in cell viability after 24 hrs by MTT assay	[PMID: 27266999]
Hs-578T	IC₅₀	0.16 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human Hs578T cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human Hs578T cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
HT-29	IC₅₀	0.02 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human HT-29 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human HT-29 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
HT-29	IC₅₀	0.104 μM Compound: 1, (+)-JQ1	Growth inhibition of human HT-29 cells after 72 hrs by SRB assay Growth inhibition of human HT-29 cells after 72 hrs by SRB assay	[PMID: 25559428]
HT-29	IC₅₀	0.28 μM Compound: 1; (+)-JQ1	Antiproliferative activity against human HT-29 cells after 72 hrs by CCK8 assay Antiproliferative activity against human HT-29 cells after 72 hrs by CCK8 assay	[PMID: 26731490]
HT-29	IC₅₀	0.48 μM Compound: 1; (+)-jQ1	Antiproliferative activity against human HT29 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HT29 cells incubated for 72 hrs by MTT assay	[PMID: 32883643]
HT-29	IC₅₀	19.6 μM Compound: (+)-JQ1	Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
K562	IC₅₀	> 2000 nM Compound: 1, JQ-1	Cytotoxicity against human K562 cells harboring BCR-ABL fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay Cytotoxicity against human K562 cells harboring BCR-ABL fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay	[PMID: 26080064]
K562	IC₅₀	0.64 μM Compound: 2; (+-)JQ1	Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by Alamar blue assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by Alamar blue assay	[PMID: 27142751]
K562	IC₅₀	9.12 μM Compound: (+)-JQ1	Antiproliferative activity against BRD4-independent human K562 cells after 72 hrs by CCK8 assay Antiproliferative activity against BRD4-independent human K562 cells after 72 hrs by CCK8 assay	[PMID: 28314513]
L02	IC₅₀	54.2 μM Compound: (+)-JQ1	Cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 24 hrs by MTT assay Cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 24 hrs by MTT assay	[PMID: 30926312]
LNCaP	IC₅₀	0.16 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human LNCAP cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human LNCAP cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
LNCaP	IC₅₀	0.16 μM Compound: 1; (+)-JQ1	Antiproliferative activity against human LNCAP cells after 96 hrs by Cell-Titer glo reagent based luminescence assay Antiproliferative activity against human LNCAP cells after 96 hrs by Cell-Titer glo reagent based luminescence assay	[PMID: 29541371]
LNCaP C4-2B	IC₅₀	0.19 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human C4-2B cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human C4-2B cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
LNCaP C4-2B	IC₅₀	0.19 μM Compound: 1; (+)-JQ1	Antiproliferative activity against human C4-2B cells after 96 hrs by Cell-Titer glo reagent based luminescence assay Antiproliferative activity against human C4-2B cells after 96 hrs by Cell-Titer glo reagent based luminescence assay	[PMID: 29541371]
LOUCY	EC₅₀	0.09 μM Compound: 1; (+)-JQ1	Cytotoxicity against human Loucy cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay Cytotoxicity against human Loucy cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	[PMID: 29170024]
MCF7	GI₅₀	> 50 μM Compound: 15; (+)-JQ1	Growth inhibition of human MCF7 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay Growth inhibition of human MCF7 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay	[PMID: 33275431]
MCF7	IC₅₀	0.2 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human MCF7 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human MCF7 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
MCF7	IC₅₀	38 μM Compound: (+)-JQ1	Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
MCF7:CFR	IC₅₀	90 nM Compound: 1; JQ1	Growth inhibition of fulvestrant-resistant human MCF7:CFR cells measured after 5 days by Hoechst 33342 dye based imaging analysis Growth inhibition of fulvestrant-resistant human MCF7:CFR cells measured after 5 days by Hoechst 33342 dye based imaging analysis	[PMID: 32453591]
MDA-MB-231	IC₅₀	0.64 μM Compound: (+)-JQ1	Antiproliferative activity against BRCA-proficient human MDA-MB-231 cells assessed as inhibition of cell growth measured after 7 days by MTT assay Antiproliferative activity against BRCA-proficient human MDA-MB-231 cells assessed as inhibition of cell growth measured after 7 days by MTT assay	[PMID: 35091172]
MDA-MB-231	IC₅₀	0.64 μM Compound: JQ-1	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 7 days Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 7 days	[PMID: 34813314]
MDA-MB-231	IC₅₀	29.51 μM Compound: 1; JQ1	Antiproliferative activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay	[PMID: 34908415]
MDA-MB-468	IC₅₀	0.54 μM Compound: (+)-JQ1	Antiproliferative activity against BRCA-proficient human MDA-MB-468 cells assessed as inhibition of cell growth measured after 7 days by MTT assay Antiproliferative activity against BRCA-proficient human MDA-MB-468 cells assessed as inhibition of cell growth measured after 7 days by MTT assay	[PMID: 35091172]
MDA-MB-468	IC₅₀	30.19 μM Compound: 1; JQ1	Antiproliferative activity against human MDA-MB-468 cells incubated for 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells incubated for 24 hrs by MTT assay	[PMID: 34908415]
MM1.S	IC₅₀	0.019 μM Compound: 1; (+)-JQ1	Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay	[PMID: 28586718]
MM1.S	IC₅₀	0.02 μM Compound: 2; (+)-JQ1	Cytotoxicity against human MM1S cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MM1S cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 28535045]
MM1.S	IC₅₀	0.062 μM Compound: JQ1	Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 36563515]
MM1.S	IC₅₀	0.109 μM Compound: 1, (+)-JQ1	Growth inhibition of human MM1S cells after 72 hrs by SRB assay Growth inhibition of human MM1S cells after 72 hrs by SRB assay	[PMID: 25559428]
MM1.S	IC₅₀	29.8 nM Compound: (+)-JQ-1; 1	Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 or SRB assay Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 or SRB assay	[PMID: 31490070]
MM1.S	IC₅₀	33 nM Compound: JQ1	Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay	[PMID: 34710325]
MM1.S	IC₅₀	69.1 nM Compound: 1; (+)-JQ-1	Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay	[PMID: 29525435]
MOLM-13	IC₅₀	56 nM Compound: 1, JQ-1	Cytotoxicity against human MOLM13 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay Cytotoxicity against human MOLM13 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay	[PMID: 26080064]
MOLM-13	IC₅₀	56 nM Compound: 1; JQ-1	Growth inhibition of human MOLM13 cells after 4 days by WST-8 assay Growth inhibition of human MOLM13 cells after 4 days by WST-8 assay	[PMID: 28463487]
MV4-11	IC₅₀	0.012 μM Compound: 1; (+)-JQ1	Antiproliferative activity against human MV4-11 cells after 72 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells after 72 hrs by CCK8 assay	[PMID: 26731490]
MV4-11	IC₅₀	0.017 μM Compound: 1, JQ1	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 96 to 120 hrs by celltiter glo assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 96 to 120 hrs by celltiter glo assay	[PMID: 34999525]
MV4-11	IC₅₀	0.023 μM Compound: 1, (+)-JQ1	Growth inhibition of human MV4-11 cells after 72 hrs by SRB assay Growth inhibition of human MV4-11 cells after 72 hrs by SRB assay	[PMID: 25559428]
MV4-11	IC₅₀	0.042 μM Compound: JQ1	Antiproliferative activity against human MM4-11 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human MM4-11 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 36563515]
MV4-11	IC₅₀	0.06 μM Compound: Cpd X1; (+)-JQ1	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 31421967]
MV4-11	IC₅₀	0.08 μM Compound: (+)-JQ1	Antiproliferative activity against BRD4-sensitive human MV411 cells after 72 hrs by CCK8 assay Antiproliferative activity against BRD4-sensitive human MV411 cells after 72 hrs by CCK8 assay	[PMID: 28314513]
MV4-11	GI₅₀	0.08 μM Compound: (+)-JQ-1	Cytotoxicity against human MV4-11 cells after 24 hrs by CellTiter-Blue assay Cytotoxicity against human MV4-11 cells after 24 hrs by CellTiter-Blue assay	[PMID: 26191363]
MV4-11	IC₅₀	0.08082 μM Compound: 1; JQ1	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 48 hrs by CellTiter-Glo assay	[PMID: 31767403]
MV4-11	IC₅₀	0.157 μM Compound: (+)-JQ-1	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter-Glo assay	[PMID: 34731760]
MV4-11	IC₅₀	0.16 μM Compound: (+)-JQ-1	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 32631570]
MV4-11	IC₅₀	0.16 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human MV4-11 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human MV4-11 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
MV4-11	IC₅₀	0.24 μM Compound: 2; (+-)JQ1	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by Alamar blue assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by Alamar blue assay	[PMID: 27142751]
MV4-11	IC₅₀	0.242 μM Compound: 1, (+)-JQ1	Cytotoxicity against human MV4-11 cells after 72 hrs by MTS assay Cytotoxicity against human MV4-11 cells after 72 hrs by MTS assay	[PMID: 23517011]
MV4-11	IC₅₀	0.57 μM Compound: (+)-JQ-1	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CCK-8 assay	[PMID: 31079968]
MV4-11	IC₅₀	24 nM Compound: 1, JQ-1	Cytotoxicity against human MV4-11 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay Cytotoxicity against human MV4-11 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay	[PMID: 26080064]
MV4-11	IC₅₀	24 nM Compound: 1; JQ-1	Growth inhibition of human MV4-11 cells after 4 days by WST-8 assay Growth inhibition of human MV4-11 cells after 4 days by WST-8 assay	[PMID: 28463487]
MV4-11	IC₅₀	6.4 μM Compound: 3; (+)-JQ1	Cytotoxicity against human MV4-11 cells assessed as decrease in cell viability after 24 hrs by MTT assay Cytotoxicity against human MV4-11 cells assessed as decrease in cell viability after 24 hrs by MTT assay	[PMID: 27266999]
MX1	EC₅₀	0.144 μM Compound: 1; (+)-JQ1	Inhibition of BRD4 in human MX1 cells assessed as decrease in cell proliferation after 3 days by Celltiter-Glo assay Inhibition of BRD4 in human MX1 cells assessed as decrease in cell proliferation after 3 days by Celltiter-Glo assay	[PMID: 31303996]
MX1	EC₅₀	254 nM Compound: 1b; JQ1	Antiproliferative activity against human MX1 cells after 72 hrs by Cell Titer Glo assay Antiproliferative activity against human MX1 cells after 72 hrs by Cell Titer Glo assay	[PMID: 28949521]
NALM-6	EC₅₀	0.06 μM Compound: 1; (+)-JQ1	Cytotoxicity against human NALM6 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay Cytotoxicity against human NALM6 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay	[PMID: 29170024]
NCI-H1975	IC₅₀	1.23 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human NCI-H1975 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human NCI-H1975 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
NRK-49F	IC₅₀	21.1 μM Compound: (+)-JQ1	Antifibrotic activity against rat NRK-49F cells assessed as reduction in cell growth measured after 48 hrs by MTT assay Antifibrotic activity against rat NRK-49F cells assessed as reduction in cell growth measured after 48 hrs by MTT assay	[PMID: 30926312]
PC-3	IC₅₀	3.01 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human PC3 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human PC3 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
PC-3	IC₅₀	3.01 μM Compound: 1; (+)-JQ1	Antiproliferative activity against human PC3 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay Antiproliferative activity against human PC3 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay	[PMID: 29541371]
Raji	IC₅₀	0.069 μM Compound: 2, (+)-JQ1	Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs	[PMID: 24900758]
SK-MEL-5	GI₅₀	> 40 μM Compound: 15; (+)-JQ1	Growth inhibition of human SK-MEL-5 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay Growth inhibition of human SK-MEL-5 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay	[PMID: 33275431]
SW1990	IC₅₀	0.63 μM Compound: (+)-JQ1	Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 7 days by MTT assay Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 7 days by MTT assay	[PMID: 35091172]
SW1990	IC₅₀	1.11 μM Compound: (+)-JQ1	Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 5 days by MTT assay Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 5 days by MTT assay	[PMID: 35091172]
SW1990	IC₅₀	3.74 μM Compound: (+)-JQ1	Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 4 days by MTT assay Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 4 days by MTT assay	[PMID: 35091172]
SW1990	IC₅₀	3.74 μM Compound: JQ-1	Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability after 4 days by MTT assay Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability after 4 days by MTT assay	[PMID: 34813314]
SW1990	IC₅₀	31.6 μM Compound: (+)-JQ1	Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth after 3 days by MTT assay Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth after 3 days by MTT assay	[PMID: 35091172]
T-cell	IC₅₀	0.11 μM Compound: 6m; JQ1	Immunosuppressive activity in BALB/c mouse splenic T cells assessed as inhibition of PMA/CD28 induced cell proliferation after 24 hrs by [methyl-3H]thymidine incorporation assay Immunosuppressive activity in BALB/c mouse splenic T cells assessed as inhibition of PMA/CD28 induced cell proliferation after 24 hrs by [methyl-3H]thymidine incorporation assay	[PMID: 26869194]
THP-1	IC₅₀	0.33 μM Compound: (+)-JQ1	Antiproliferative activity against human THP-1 cells expressing BRD4 assessed as inhibition of cell growth measured after 3 days by MTT assay Antiproliferative activity against human THP-1 cells expressing BRD4 assessed as inhibition of cell growth measured after 3 days by MTT assay	[PMID: 35091172]
THP-1	IC₅₀	0.56 μM Compound: JQ-1	Antiinflammatory activity against human THP-1 cells assessed as inhibition of LPS-induced IL-6 production incubated for 18 hrs by ELISA Antiinflammatory activity against human THP-1 cells assessed as inhibition of LPS-induced IL-6 production incubated for 18 hrs by ELISA	[PMID: 35318165]
U-266	IC₅₀	3.45 μM Compound: 1; JQ1	Antiproliferative activity against human U-266 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Antiproliferative activity against human U-266 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 33862375]
U2OS	IC₅₀	> 100 μM Compound: 1, (+)-JQ1	Cytotoxicity against human U2OS cells after 24 hrs by WST-1 assay Cytotoxicity against human U2OS cells after 24 hrs by WST-1 assay	[PMID: 23517011]
U2OS	IC₅₀	1.62 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human U2OS cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human U2OS cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
U-937	IC₅₀	> 20 μM Compound: 3; (+)-JQ1	Cytotoxicity against human U937 cells assessed as decrease in cell viability after 24 hrs by MTT assay Cytotoxicity against human U937 cells assessed as decrease in cell viability after 24 hrs by MTT assay	[PMID: 27266999]
VCaP	IC₅₀	0.012 μM Compound: 1; (+)-JQ-1	Antiproliferative activity against human VCaP cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human VCaP cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
WI-38	IC₅₀	4.97 μM Compound: 1; (+)-jQ1	Antiproliferative activity against human WI-38 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human WI-38 cells incubated for 72 hrs by MTT assay	[PMID: 32883643]

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].

MedChemExpress (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].

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

Molecular Weight

456.99

Formula

C₂₃H₂₅ClN₄O₂S

CAS No.

1268524-70-4

Appearance

Solid

Color

White to yellow

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 20% HP-β-CD in Saline
Solubility: 10 mg/mL (21.88 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 10 mg/mL (21.88 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (287 KB) SDS (393 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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1882 mL	10.9412 mL	21.8823 mL	54.7058 mL
	5 mM	0.4376 mL	2.1882 mL	4.3765 mL	10.9412 mL
	10 mM	0.2188 mL	1.0941 mL	2.1882 mL	5.4706 mL
	15 mM	0.1459 mL	0.7294 mL	1.4588 mL	3.6471 mL
	20 mM	0.1094 mL	0.5471 mL	1.0941 mL	2.7353 mL
	25 mM	0.0875 mL	0.4376 mL	0.8753 mL	2.1882 mL
	30 mM	0.0729 mL	0.3647 mL	0.7294 mL	1.8235 mL
	40 mM	0.0547 mL	0.2735 mL	0.5471 mL	1.3676 mL
	50 mM	0.0438 mL	0.2188 mL	0.4376 mL	1.0941 mL
	60 mM	0.0365 mL	0.1824 mL	0.3647 mL	0.9118 mL
	80 mM	0.0274 mL	0.1368 mL	0.2735 mL	0.6838 mL

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

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

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