(+)-JQ1

目录号 M2167 所有产品仅供科研使用，严禁用于人或动物的治疗等任何其他用途，不为任何个人提供产品和服务

(+)-JQ1是一种BET bromodomain抑制剂，作用于BRD4(2)，IC50为33 nM，结合到BET家族的所有Bromodomain结构域，而不结合到BET家族以外的Bromodomain结构域，JQ1通过c-MYC介导的途径下调CD47的表达。

别名：JQ1

规格	价格	库存状态
Free Sample (0.5-1 mg)	¥ 0	中国库存现货
10mM*1mL in DMSO	¥ 583	中国库存现货
2mg	¥ 352	中国库存现货
5mg	¥ 583	中国库存现货
10mg	¥ 759	中国库存现货
50mg	¥ 1562	中国库存现货

其他规格数量报价？

质量标准及产品资料

纯度： 98.80%
COA
MSDS
H-NMR
HPLC

产品信息

生物活性

使用AbMole产品发表的文献

Nat Commun. 2023 Mar 14;14(1):1413.

BRD9-mediated chromatin remodeling suppresses osteoclastogenesis through negative feedback mechanism
J Exp Med. 2022 Nov 7;219(11):e20212405.

Transit-amplifying cells control R-spondins in the mouse crypt to modulate intestinal stem cell proliferation
JCI Insight. 2022 Sep 8;7(17):e151851.

Targeting ESR1 mutation-induced transcriptional addiction in breast cancer with BET inhibition
Cancer Cell. 2016 Aug 8;30(2):290-307.

Regulation of OGT by URI in Response to Glucose Confers c-MYC-Dependent Survival Mechanisms
Oncotarget. 2015 Nov 10;6(35):37410-25.

SMAC mimetic Debio 1143 synergizes with taxanes, topoisomerase inhibitors and bromodomain inhibitors to impede growth of lung adenocarcinoma cells

产品使用成果展示

	数据来源	Cancer Cell (2016). Figure 8. (+)-JQ1 (Abmole Bioscience, Shanghai, China)
	方法	Treatment started in 4-week-old mice that were euthanized and analyzed at 8 weeks of age.
	细胞系/动物模型
	浓度	50 mg/kg
	处理时间
	实验结果	Inhibition of BET bromodomain by JQ1, known to downregulate c-MYC levels in vivo (Delmore et al., 2011), significantly reduced dysplatic lesions in 8-week-old URI(WT)(+/KI)hep livers (Figures 8O–8Q), consistent with the role of c-MYC in liver tumor progression (Qu et al., 2014).

	数据来源	Oncotarget.(2015) . Figure 6. JQ1 (Abmole Bioscience)
	方法	in vivo
	细胞系/动物模型	H1975 and A549 lung adenocarcinoma in xenograft mouse models
	浓度	25 mg/kg i.p.
	处理时间	20 days
	实验结果	Limited effects of the combination of Debio 1143 and JQ1 treatment on tumor volume were observed in H1975 xenografts treated with 30mg/kg Debio 1143; 25mg/kg JQ1 (maximum %treated/control [%T/C] = 52.7%) (Figure 6A). At these drug concentrations, body weights were reduced early in treatment, indicative of toxicity, but body weights stabilized over time (Figure 6B).

	数据来源	Oncotarget.(2015) . Figure 5. JQ1 (Abmole Bioscience)
	方法	western blot
	细胞系/动物模型	A549, H1975, H2030 cells
	浓度	1000 nM
	处理时间	24 h
	实验结果	In H1975, H2030, and A549 cells, JQ1 also moderately reduces cIAP1 levels in H1975, A549, and H2030 cells. Protein levels of cIAP1 are undetectable in the Debio 1143/JQ1 combinations (Figure 5A). cIAP2 and XIAP levels were most completely suppressed following combination treatment with Debio 1143 and JQ1 in H1975 cells. Debio 1143 enhanced TNFα mRNA expression in H2030 cells, but not H1975 or A549 (Figure 5B), and JQ1 did not affect TNFα mRNA expression. these results indicate a functioning ripoptosome is formed in the two cell lines most sensitive to the combination of Debio 1143 and JQ1.

	数据来源	Oncotarget.(2015) . Figure 4. JQ1 (Abmole Bioscience)
	方法	western blot
	细胞系/动物模型	A549, H1975, H2030 cells
	浓度	1000 nM
	处理时间	24 h
	实验结果	The combination, but neither single agent, elevated IκBα, an NF-κB inhibitor (Figure 4A). Debio 1143, but not JQ1, induced nuclear localization of p52 in each cell line tested - H1975, A549, and H2030, with no augmentation by the combination (Figure 4B, 4C, and 4D).

	数据来源	Oncotarget.(2015) . Figure 3. JQ1 (Abmole Bioscience)
	方法	growth inhibition assays
	细胞系/动物模型	A549, H1975, H2030 cells
	浓度	0~100 µ M
	处理时间	24 h
	实验结果	Debio 1143 was also more effective in combination with the bromodomain inhibitor JQ1. Over a period of 24 hours, Debio 1143 alone induced moderate polyADP ribose polymerase (PARP) cleavage in H1975 and H2030 cells; cleaved PARP levels were greatly enhanced in the presence of JQ1 in H1975 and H2030 cells (Figure 3G).

	数据来源	Oncotarget.(2015) . Figure 2. JQ1 (Abmole Bioscience)
	方法	growth inhibition assays
	细胞系/动物模型	A549, H1650, H1975, H820, H2030 and H2228 cells
	浓度	0~10 µ M
	处理时间	24 h
	实验结果	A subset of lung adenocarcinoma cell lines was also sensitive to bromodomain inhibition with both iBET (Figure S2B) and JQ1 (Figure 2D).

实验参考

体外实验*
细胞系	MM.1S, RPMI-8226, KMS-20, L-363 Dox40 and AMO-1 cell lines
方法	Cell Viability Assays MM cell lines were seeded onto 384-well tissue culture treated plates at a density of 1,000 cells/well in a volume of 50 µL of media. After seeding cells were incubated for 1 hour and during the interim a stock plate of JQ1 was thawed at room temperature in a desiccated box. The addition of JQ1 to the assay plate was done with disposable 384-well pins (V&P Scientific, San Diego, CA) that delivered 100 nL of the drug diluted in DMSO to each well of the plate. After 72 hours of incubation cells were analyzed for cell viability by the addition of CellTiter Glo (Promega, Madison, WI) to the assay plates. After 30 min incubation at 37 oC the signal from the viable cells was analyzed on a Luminoskan luminometer (Labsystems Franklin, MA).
浓度	0~1µM
处理时间	72 h

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

体内实验*
动物模型	SCID-beige mice orthotopically xenografted after intravenous injection with MM.1S-luc+ cells
配制	JQ1 in 10% cyclodextrine (Sigma)
剂量	50 mg/kg daily
给药处理	intra-peritoneally for 5 days/week, 2 weeks

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

化学性质

分子量	456.99
分子式	C23H25ClN4O2S
CAS号	1268524-70-4
溶解性（25°C）	DMSO 45 mg/mL Ethanol 45 mg/mL
储存条件	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月
运输方式	冰袋运输，根据产品的不同，可能会有相应调整。

储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / 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

不同实验动物依据体表面积的等效剂量转换表（参考来源于公开文献）

	小鼠	大鼠	兔	豚鼠	仓鼠	狗
重量 (kg)	0.02	0.15	1.8	0.4	0.08	10
体表面积 (m²)	0.007	0.025	0.15	0.05	0.02	0.5
K_m 系数	3	6	12	8	5	20

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的K_m系数
	动物 A的K_m系数

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Li Z, et al. Nucleic Acids Res. The BET bromodomain inhibitor JQ1 activates HIV latency through antagonizing Brd4 inhibition of Tat-transactivation.

[2] Matzuk MM, et al. Cell. Small-molecule inhibition of BRDT for male contraception.

[3] Delmore JE, et al. Cell. BET bromodomain inhibition as a therapeutic strategy to target c-Myc.

[4] Filippakopoulos P, et al. Nature. Selective inhibition of BET bromodomains.

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