(+)-JQ-1 [1268524-70-4] 500 mg

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HY-13030_500mg

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(+)-JQ1

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Description

1268524-70-4

(+)-JQ1, 500 mg

Catalog No.S7110
For research use only.

Bulk (+)-JQ1 BET bromodomain inhibitor

The IC50 is 77 nM/33 nM for BRD4(1/2) in cell-free assays that are binding to all bromodomains of the BET family. They are not binding 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.

Properties:
Purity:	>98%
Molecular Formula:	C23H25ClN4O2S
Molecular weight:	456.99

	Research Use Only
UNSPSC:	12352200

AGTC (+)-JQ1

(+)-JQ1 | C23H25ClN4O2S | CAS No. 1268524-70-4

Potent and selective BET bromodomain inhibitor; cell permeable
Chemical Name: (6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid 1,1-dimethylethyl ester
Purity: ≥98% (HPLC)

Biological Activity for (+)-JQ1

(+)-JQ1 is a potent, high affinity, selective BET bromodomain inhibitor (IC50 values are 17.7, 32.6, 76.9 and 12942 nM for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP respectively; Kd values are 49, 59.5, 82, 90.1, 128 and 190 nM for BRD4 (N), BRD3 (N), BRD3 (C), BRD4 (C), BRD2 (N) and BRDT (N) respectively).
(+)-JQ1 induces squamous differentiation in NUT midline carcinoma (NMC) cell lines and inhibits tumor growth in NMC xenograft models in vivo. (+)-JQ1 inhibits proliferation and induces autophagy in bladder cancer cells in vitro and in vivo. It also suppresses MYC gene expression and inhibits proliferation of lymphoma and leukemia cell lines. In human pulmonary microvasular endothelial cells (HPMEC), NF-κB activation, IL-6 and IL-8 expression and proliferation are inhibited by (+)-JQ1.
The compound also inhibits transcription of ACE2 and TMPRSS2 genes in mouse lung tissue and prevents infection by SARS-CoV-2. In germ cells from male mice, (+)-JQ1 exhibits reversible contraceptive effects. (+)-JQ1 inhibits the BRD4-JUN-CCL2-TNF-α axis in pancreatic cancer cells and improves survival by reducing macrophage recruitment.

Inactive Analog also available from AGTC

Carboxylic acid-functionalized

click-activated (alkyne) versions for PROTAC development also available.

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the (+)-JQ1 probe summary on the SGC website.

External Portal Information for (+)-JQ1

What is the use of (+)-JQ1 compound Libraries for (+)-JQ1?

(+)-JQ1 in Epigenetics Library

Technical Data for (+)-JQ1

M. Wt 456.99
Formula C23H25ClN4O2S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1268524-70-4
PubChem ID 46907787
InChI Key DNVXATUJJDPFDM-KRWDZBQOSA-N
Smiles O=C(OC(C)(C)C)C[C@@H]1N=C(C4=CC=C(Cl)C=C4)C3=C(SC(C)=C3C)N2C1=NN=C2C
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

How soluble is (+)-JQ1?

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 45.7 100
ethanol 45.7 100
Preparing Stock Solutions for (+)-JQ1
The following data is based on the product molecular weight 456.99. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.19 mL 10.94 mL 21.88 mL
5 mM 0.44 mL 2.19 mL 4.38 mL
10 mM 0.22 mL 1.09 mL 2.19 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

Product Datasheets for (+)-JQ1
Certificate of Analysis / Product Datasheet

Safety Datasheet

References for (+)-JQ1 that support the biological activity of the product.

Filippakopoulos et al (2010) Selective inhibition of BET bromodomains. Nature 468 1067 PMID: 20871596
Herrmann et al (2012) Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia AML. Oncotarget 3 1588 PMID: 23249862
Matzuk et al (2012) Small-molecule inhibition of BRDT for male contraception. Cell 150 673 PMID: 22901802
Li et al (2019) BET inhibitor JQ1 suppresses cell proliferation via inducing autophagy and activating LKB1/AMPK in bladder cancer cells. Cancer Med. 8 4792 PMID: 31250978
Mumby et al (2017) Bromodomain and extra-terminal protein mimic JQ1 decreases inflammation in human vascular endothelial cells: Implications for pulmonary arterial hypertension. Respirology 22 157 PMID: 27539364
Qiao et al (2020) Targeting transcriptional regulation of SARS-CoV-2 entry factors ACE2 and TMPRSS2. Proc.Natl.Acad.Sci.U.S.A. 118 e2021450118 PMID: 33310900
Mertz et al (2011) Targeting MYC dependence in cancer by inhibiting BET bromodomains. Proc.Natl.Acad.Sci.U.S.A. 108 16669 PMID: 21949397
Tu et al (2021) TNF-a-producing macrophages determine subtype identity and prognosis via AP1 enhancer reprogramming in pancreatic cancer. Nat.Cancer 2 1185 PMID: 35122059
If you know of a relevant reference for (+)-JQ1, please let us know.
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Keywords: (+)-JQ1, (+)-JQ1 supplier, BET, bromodomains, inhibitors, inhibits, potent, selective, high, affinity, NUT, midline, carcinomas, antitumor, male, contraceptive, BRD2, BRD3, BRD4, BRDT, sgc, autophagy, induces, activators, activates, induction, anti-inflammatory, coronavirus, SARS-CoV-2, Bromodomains, Coronavirus, 4499, Tocris Bioscience

Scientific information:

Scientific info:

(+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2). IC50 Value: 77 nM(for BRD4(1)), 33 nM( for BRD4(2)) Target: BRD4 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. (+)-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. (+)-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. 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. (+)-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. (+)-JQ1 (50 mg/kg i.p.) leads to a highly significant increase in survival of mice bearing Raji xenografts.

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