JQ-1 (carboxylic acid)

JQ-1 (carboxylic acid) 是一种细胞渗透性 BRD4 抑制剂,对 BRD4(1) 和 BRD4(2) 的 IC50 分别为 77 和 33 nM。它是一种 (+)-JQ1 衍生物,可作为合成 PROTACs 的前体。

CAS号

202592-23-2

分子式

C19H17ClN4O2S

主要靶点

Epigenetic Reader Domain

仅限科研使用

Cat No : CM01197

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Synonyms

JQ-1 carboxylic acid



产品信息

JQ-1 (carboxylic acid) is a cell-permeable BRD4 inhibitor with IC50s of 77 nM for BRD4(1) and 33 nM for BRD4(2)

CAS号 202592-23-2
分子式 C19H17ClN4O2S
主要靶点 Epigenetic Reader Domain
主要通路 表观遗传
分子量 400.88
纯度 99.39%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 JQ-1 carboxylic acid

靶点活性

BRD4(1):77 nM |BRD4(2):33 nM

体外活性

JQ-1 carboxylic acid is an inhibitor of bromodomain and extra terminal domain (BET) family proteins, blocking their interaction with acetylated histones[1],it has been used as a chemical probe to investigate the role of BET bromodomains in the transcriptional regulation of oncogenesis[2][3].

溶解度

DMSO:155 mg/mL (386.65 mM)

参考文献

1.Rosner M , Hengstschl?Ger M . Targeting Epigenetic Readers in Cancer[J]. New England Journal of Medicine, 2012, 367(18):1764-1765.
2.Dawson M A , Prinjha R K , Dittmann A , et al. Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia[J]. Nature, 2011, 478(7370):529-533.
3.Mertz J A , Conery A R , Bryant B M , et al. Targeting MYC dependence in cancer by inhibiting BET bromodomains[J]. Proceedings of the National Academy of Sciences of the United States of America, 2011, 108(40):16669-16674.

The molarity calculator equation

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

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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