GSK J5

A negative control compound for GSK-J4

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库存: 现货

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数量
1mg

￥462.00

370.00

- +
5mg

￥1712.00

1370.00

- +
10mg

￥2987.00

2390.00

- +
50mg

￥12425.00

9940.00

- +

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货号: ajci18478
CAS: 1394854-51-3
别名: N-[2-(3-吡啶基)-6-(1,2,4,5-四氢-3H-3-苯并氮杂卓-3-基)-4-嘧啶基]-BETA-丙氨酸乙酯
分子式: C24H27N5O2
分子量: 417.5
纯度: >98%
溶解度: 20mg/mL in ethanol, 30mg/mL in DMSO or in DMF
储存: Store at RT
库存: 现货

Background

The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.[1],[2]. GSK-J4 is a cell-permeable prodrug which is modified by intracellular esterases to give GSK-J1, an inhibitor of JMJD3. GSK-J5 is a pyridine regio-isomer of GSK-J4. Like GSK-J4, this isomer is cell-permeable and hydrolyzed to a free base.3 However, the free base is a weak inhibitor of JMJD3 (IC50 > 100 μM), making it an ideal inactive control molecule for elucidating the functional role of JMJD3 inhibition.[3]
Reference:
[1]. Agger, K., Cloos, P.A.C., Christensen, J., et al. UTX and JMJD3 are histone H3K27 demethylases involved in HOX gene regulation and development. Nat.Lett. 449(7163), 731-734 (2011).
[2]. Hübner, M.R., and Spector, D.L. Role of H3K27 demethylases Jmjd3 and UTX in transcriptional regulation. Cold Spring Harb.Symp.Quant.Biol. 75, 43-49 (2010).
[3]. Kruidenier, L., Chung, C.W., Cheng, Z., et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature 488, 404-408 (2012).