(+)-JQ1

Catalog No.S7110 Batch:S711013

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Technical Data

Formula

C23H25ClN4O2S
Molecular Weight 456.99 CAS No. 1268524-70-4
Solubility (25°C)* In vitro DMSO 91 mg/mL (199.12 mM)
Ethanol 91 mg/mL (199.12 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description (+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. (+)-JQ1 suppresses cell proliferation via inducing autophagy. (+)-JQ1 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.
Targets
BRD4 (2) [1]
(Cell-free assay)		 BRD4 (1) [1]
(Cell-free assay)
33 nM 77 nM
In vitro (+)-JQ1 enantiomer binds directly into the Kac binding site of BET bromodomains. (+)-JQ1 (500 nM) binds BRD4 competitively with chromatin resulting in differentiation and growth arrest of NMC cells. (+)-JQ1 (500 nM) attenuates rapid proliferation of NMC 797 and Per403 cell lines as demonstrated by reduced Ki67 staining. (+)-JQ1 (500 nM) potently decreases expression of both BRD4 target genes in NMC 797 cells. (+)-JQ1 inhibits cellular viability with IC50 of 4 nM in NMC 11060 cells. [1] (+)-JQ1 results in robust inhibition of MYC expression in MM cell lines. (+)-JQ1 inhibits proliferating of KMS-34 and LR5 with IC50 of 68 nM and 98 nM, respectively. (+)-JQ1 (500 nM)-treated MM.1S cells results in a pronounced decrease in the proportion of cells in S-phase, with a concomitant increase in cells arrested in G0/G1. (+)-JQ1 (500 nM) results in pronounced cellular senescence by beta-galactosidase staining. (+)-JQ1 (800 nM) exposure leads to a significant reduction in cell viability among the majority of CD138+ patient-derived MM samples tested. [2] (+)-JQ1 inhibits growth of LP-1 cells with GI50 of 98 nM. (+)-JQ1 (625 nM) results in an increase in the percentage of LP-1 cells in G0/G1. (+)-JQ1 (500 nM) suppresses the expression of MYC, BRD4 and CDK9 in LP-1 cells. [3] (+)-JQ1 (1 μM) activates HIV transcription in latently infected Jurkat T cells. (+)-JQ1 (50 μM) stimulates predominantly Tat-dependent HIV transcription in both Jurkat and HeLa cells. (+)-JQ1 (5 μM) induces Brd4 dissociation enables Tat to recruit SEC to HIV promoter and induce Pol II CTD phosphorylation and viral transcription in J-Lat A2 cells. JQ1 enables Tat to increase CDK9 T-loop phosphorylation and partially dissociates P-TEFb from 7SK snRNP in Jurkat T cells. [4]
In vivo (+)-JQ1 (50 mg/kg) inhibits tumors growth in mice with NMC 797 xenografts. (+)-JQ1 (50 mg/kg) results in effacement of NUT nuclear speckles in mice with NMC 797 xenografts, consistent with competitive binding to nuclear chromatin. (+)-JQ1 (50 mg/kg) induces strong (grade 31) keratin expression in NMC 797 xenografts. (+)-JQ1 (50 mg/kg) promotes differentiation, tumor regression and prolonged survival in mice models of NMC xenografts. [1] (+)-JQ1 (50 mg/kg) results in a significant prolongation in overall survival of SCID-beige mice orthotopically xenografted after intravenous injection with MM.1S-luc+ cells compared to vehicle-treated animals. [2] (+)-JQ1 (50 mg/kg i.p.) leads to a highly significant increase in survival of mice bearing Raji xenografts. [3]
Features (+)-JQ1 is more effective than (-)-JQ1.

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    MC 11060 cells

  • Concentrations

    ~500 nM

  • Incubation Time

    48 hours

  • Method

    Cells are seeded into white, 384-well microtiter plates at 500 cells per well in a total volume of 50 μL media. The 797, TT and TE10 cells are grown in DMEM containing 1% penicillin/streptomycin and 10% FBS. The Per403 cells are grown in DMEM containing 1 % penicillin/streptomycin and 20% FBS. Patient-derived NMC 11060 cells are grown in RPMI with 10% FBS and 1% penicillin/streptomycin. (+)-JQ1 is delivered to microtiter assay plates by robotic pin transfer. Following a 48 hours incubation at 37℃, cells are lysed and wells are assessed for total ATP content using a commercial proliferation assay. Replicate measurements are analyzed with respect to dose and estimates of IC50 are calculated by logistic regression (GraphPad Prism).
Animal Study:

[1]
  • Animal Models

    Mice bearing NMC 797 xenografts

  • Dosages

    50 mg/kg

  • Administration

    intraperitoneal injection

Customer Product Validation

Data from [Cancer Res, 2014, 74(23), 7090-102]

Data from [Cancer Res, 2014, 74(23), 7090-102]

Data from [Data independently produced by , , Sci Rep, 2016, 6:23770.]

Data from [Data independently produced by , , Oncotarget, 2016, 6(7):5134-46.]

Selleck's (+)-JQ1 has been cited by 425 publications

Mechanism for controlled assembly of transcriptional condensates by Aire [ Nat Immunol, 2024, 25(9):1580-1592] PubMed: 39169234
Dual Inhibition of CDK4/6 and XPO1 Induces Senescence With Acquired Vulnerability to CRBN-Based PROTAC Drugs [ Gastroenterology, 2024, S0016-5085(24)00062-3] PubMed: 38262581
C5aR1 inhibition reprograms tumor associated macrophages and reverses PARP inhibitor resistance in breast cancer [ Nat Commun, 2024, 15(1):4485] PubMed: 38802355
Orthogonal proteogenomic analysis identifies the druggable PA2G4-MYC axis in 3q26 AML [ Nat Commun, 2024, 15(1):4739] PubMed: 38834613
LSD1 inhibition improves efficacy of adoptive T cell therapy by enhancing CD8+ T cell responsiveness [ Nat Commun, 2024, 15(1):7366] PubMed: 39191730
A SWI/SNF-dependent transcriptional regulation mediated by POU2AF2/C11orf53 at enhancer [ Nat Commun, 2024, 15(1):2067] PubMed: 38453939
The MYCN oncoprotein is an RNA-binding accessory factor of the nuclear exosome targeting complex [ Mol Cell, 2024, S1097-2765(24)00285-5] PubMed: 38703770
ARGLU1 enhances promoter-proximal pausing of RNA polymerase II and stimulates DNA damage repair [ Nucleic Acids Res, 2024, gkae208] PubMed: 38520408
A novel MYC-ZNF706-SLC7A11 regulatory circuit contributes to cancer progression and redox balance in human hepatocellular carcinoma [ Cell Death Differ, 2024, 10.1038/s41418-024-01324-3] PubMed: 38862581
Mechanism of co-operation of mutant IL-7Rα and mutant NRAS in acute lymphoblastic leukemia: role of MYC [ Haematologica, 2024, 109(6):1726-1740] PubMed: 38031763

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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