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(+)-JQ-1

Catalog No. T2110 CAS 1268524-70-4

Synonyms: JQ1

(+)-JQ-1 (JQ1) is a BET bromine domain inhibitor that inhibits BRD4 (1/2) (IC50=77/33 nM) with specificity and reversibility. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.

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(+)-JQ-1, CAS 1268524-70-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 30.00
2 mg	In stock	$ 37.00
5 mg	In stock	$ 55.00
10 mg	In stock	$ 72.00
25 mg	In stock	$ 97.00
50 mg	In stock	$ 147.00
100 mg	In stock	$ 198.00
200 mg	In stock	$ 297.00
500 mg	In stock	$ 539.00
1 mL * 10 mM (in DMSO)	In stock	$ 61.00

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Purity: 99.97%

Purity: 98.36%

Purity: 98.15%

Purity: 98.00%

Purity: 98%

Purity: 97.57%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	(+)-JQ-1 (JQ1) is a BET bromine domain inhibitor that inhibits BRD4 (1/2) (IC50=77/33 nM) with specificity and reversibility. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.
Targets&IC50	BRD4(1):77 nM(cell free), BRD4(2):33 nM(cell free)
In vitro	METHODS: The BRD4-NUT-dependent cell line NMC 797 was treated with (+)-JQ-1 (250 nM) for 48 h. The cell cycle was detected using Flow Cytometry. RESULTS: (+)-JQ-1 induced G1 cell cycle arrest. [1] METHODS: Human multiple myeloma cells KMS11, LR5, OPM1 and INA-6 were treated with (+)-JQ-1 (500 nM) for 24 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: (+)-JQ-1 inhibited c-Myc protein expression in expanded Myc-dependent MM cell lines. [2]
In vivo	METHODS: To detect anti-tumor activity in vivo, (+)-JQ-1 (50 mg/kg, 5% DMSO in 5% dextrose) was administered intraperitoneally to NCr nude mice bearing NMC xenograft tumors once daily for eighteen days. RESULTS: Significant tumor regression and improved overall survival were observed after (+)-JQ-1 treatment. [1] METHODS: To detect anti-tumor activity in vivo, (+)-JQ-1 (50 mg/kg) was intraperitoneally injected into nude mice carrying human gastric cancer tumor HGC27 once daily for two weeks. RESULTS: (+)-JQ-1 prevented the growth of gastric cancer tumors and inhibited tumor metastasis. [3]
Cell Research	Cells were plated at 5,000 cells per well of 96-well plates containing titrations of the compounds as indicated. After incubation, the cells were washed once with PBS and resuspended in 175 μL of ice-cold 70% ethanol and fixed for a minimum of 16 h at 4 °C. The cells were pelleted and washed 1× with PBS and stained for 30 min at room temperature (RT) with 120 μL of staining solution [propidium iodide (20 μg/mL), RNase A (25 μg/mL), 0.1% Triton X-100 in PBS]. Cell number and cell cycle data were obtained by using a flow cytometer using the Express Pro module. DNA content histograms were analyzed by using ModFit LT 3.2 Software. To calculate the number of viable cells in each well, the concentration of events measured using the Guava was multiplied by the volume of cells in the well, then by the fraction of cells in G1+S+G2/M. GI50 values for each cell line were calculated as the concentration of compound giving a 50% reduction in cell number relative to the DMSO control [4].
Animal Research	(Harlan) inoculated s.c. with 3 × 10^6 cells per mouse resuspended in 10% Matrigel. Two weeks later (average tumor volume 150 mm3), mice were assigned into two groups: 15 mice were treated with vehicle control (5:95 DMSO:10% 2-Hydroxypropyl-β-cyclodextrin), and 15 mice were treated with 30 mg/kg (+)-JQ1 by i.p. injection twice a day for 28 d. Body weight and tumor volume were measured daily. Tumor volume was calculated from caliper measurements by using the following formula: W × H × L × 0.52. Mice were killed when tumor volume reached 2,000 mm3, when body weight decreased >20% of initial weight, or when the mice were in poor health as established in the IACUC protocol. Survival was plotted and analyzed in GraphPad Prism software, and statistical significance was calculated by using log-rank (Mantel-Cox) and Gehan–Breslow–Wilcoxon tests. MV4-11 xenografts were established in nude mice injected with 10 × 10^6 cells per mouse. JQ1 was dosed i.p. and formulated as described above. Mice were divided into 4 groups of 10 animals: vehicle control once a day; 50 mg/kg (+)-JQ1 once a day; 30 mg/kg (+)-JQ1 twice a day; and cytarabine 100 mg/kg daily (5 d on, 2 d off). Treatment of mice with cytarabine at 100 mg/kg resulted in significant weight loss at day 8 and, therefore, the dose needed to be decreased to 75 mg/kg [4].

Synonyms	JQ1
Molecular Weight	456.99
Formula	C23H25ClN4O2S
CAS No.	1268524-70-4

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 45.7 mg/mL (100 mM)

DMSO: 29.41 mg/mL (64.36 mM), Sonification is recommended.

References and Literature

1. Filippakopoulos P, et al. Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73. 2. Delmore JE, et al. BET bromodomain inhibition as a therapeutic strategy to target c-Myc. Cell. 2011 Sep 16;146(6):904-17. 3. Zhou S, et al. BET protein inhibitor JQ1 downregulates chromatin accessibility and suppresses metastasis of gastric cancer via inactivating RUNX2/NID1 signaling. Oncogenesis. 2020 Mar 10;9(3):33. 4. Mertz JA, et al. Targeting MYC dependence in cancer by inhibiting BET bromodomains. Proc Natl Acad Sci U S A. 2011 Oct 4;108(40):16669-74. 5. Wang M, Zhao L, Tong D, et al. BET bromodomain inhibitor JQ1 promotes immunogenic cell death in tongue squamous cell carcinoma[J]. International Immunopharmacology. 2019, 76: 105921.

Citations

1. Ding L, Chen X, Zhang W, et al.Canagliflozin primes antitumor immunity by triggering PD-L1 degradation in endocytic recycling.The Journal of Clinical Investigation.2023, 133(1). 2. Ma J, Hu W, Liu Y, et al.CD226 maintains regulatory T cell phenotype stability and metabolism by the mTOR/Myc pathway under inflammatory conditions.Cell Reports.2023, 42(10). 3. Wu T Y, Chen X C, Tang G X, et al.Development and Characterization of Benzoselenazole Derivatives as Potent and Selective c-MYC Transcription Inhibitors.Journal of Medicinal Chemistry.2023 4. Zhang G M, Huang S S, Ye L X, et al. Reciprocal positive regulation between BRD4 and YAP in GNAQ-mutant uveal melanoma cells confers sensitivity to BET inhibitors. Pharmacological Research. 2022: 106464. 5. Ding D, Zheng R, Tian Y, et al. Retinoblastoma protein as an intrinsic BRD4 inhibitor modulates small molecule BET inhibitor sensitivity in cancer. Nature Communications. 2022, 13(1): 1-15. 6. Zhao F, Huang Y, Zhang Y, et al. SQLE inhibition suppresses the development of pancreatic ductal adenocarcinoma and enhances its sensitivity to chemotherapeutic agents in vitro. Molecular Biology Reports. 2022: 1-9 7. Wang M, Zhao L, Tong D, et al. BET bromodomain inhibitor JQ1 promotes immunogenic cell death in tongue squamous cell carcinoma. International Immunopharmacology. 2019, 76: 105921

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Highly Selective Inhibitor Library NO PAINS Compound Library Anti-COVID-19 Compound Library Reprogramming Compound Library Preclinical Compound Library Epigenetics Compound Library PPI Inhibitor Library Target-Focused Phenotypic Screening Library Histone Modification Compound Library

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Keywords

(+)-JQ-1 1268524-70-4 Autophagy Chromatin/Epigenetic PROTAC Epigenetic Reader Domain Ligands for Target Protein for PROTAC JQ 1 Inhibitor (+)JQ1 JQ-1 (+) JQ 1 inhibit JQ1 Target Protein-binding Moiety inhibitor

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