(R)-(-)-JQ1 Enantiomer

The inactive stereoisomer of a BET bromodomain inhibitor

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库存: 现货

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数量
2mg

￥625.00

500.00

- +
5mg

￥1212.00

970.00

- +
10mg

￥2075.00

1660.00

- +
50mg

￥7075.00

5660.00

- +
100mg

￥12825.00

10260.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajci11886
CAS: 1268524-71-5
别名: (R)-(-)2-(4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-F][1,2,4]三唑并[4,3-A][1,4]二氮杂环庚烷-6-基)乙酸叔丁酯
分子式: C23H25ClN4O2S
分子量: 456.99
纯度: >98%
溶解度: DMSO : ≥ 100 mg/mL (218.82 mM)
储存: Store at -20°C
库存: 现货

Background

The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, play a key role in many cellular processes, including inflammatory gene expression, mitosis, and viral/host interaction by controlling the assembly of histone acetylation-dependent chromatin complexes. (±)-JQ1 displaces BET proteins from chromatin by competitively binding to the acetyl-lysine recognition pocket of BET bromodomains.^1,2 The (?)-JQ1 stereoisomer has no appreciable affinity to BET bromodomains, whereas enantiomerically pure (+)-JQ1 binds to BRD4 bromodomains 1 and 2 with K_d values of ~50 and 90 nM, respectively.¹

1.Filippakopoulos, P., Qi, J., Picaud, S., et al.Selective inhibition of BET bromodomainsNature468(7327)1067-1073(2010) 2.Dawson, M.A., Kouzarides, T., and Huntly, B.J.Targeting epigenetic readers in cancerN. Engl. J. Med.367(7)647-657(2012)