KG-501

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Chemical Structure| 18228-17-6 同义名 : Naphtholas-ephosphate; 2-naphthol-AS-E-phosphate; Naphthol AS-E phosphate
CAS号 : 18228-17-6
货号 : A631283
分子式 : C17H13ClNO5P
纯度 : 99%+
分子量 : 377.72
MDL号 : MFCD00042718
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 5 mg/mL(13.24 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • bromodomain
描述 KG-501 is a CREB inhibitor, with an IC50 of 6.89 μM[1]. KG-501 disrupts phospho (Ser-133) CREB binding to KIX with a Ki of ~90 μM, using concentrations of CREB that are within the linear range of the binding assay. Treatment of HEK293T cells with KG-501 also blocks induction of endogenous CREB target genes (NR4A2, αCG, c-fos, and RGS2) by forskolin, indicating that KG-501 likely exerts a general effect on CREB activity[2]. In addition, KG-501 and CREB knockdown significantly decreased the levels of phosphorylated Akt, leading to a reduced number of oocytes with Foxo3a nuclear export. KG-501 also inhibited bpV (HOpic)-stimulated primordial follicle activation[3]. At 10 μM, KG-501 suppresses the expression of all of the IL-1β-induced CXC chemokine genes except CXCL8. For the protein level, KG-501 significantly suppresses IL-1β-induced CXCL5 protein secretion[4]. BAA (Bulleyaconitine) treatment induced phosphorylation of CREB (rather than NF-κB) and prodynorphin expression in cultured primary microglia, and antiallodynia in neuropathy, which were totally inhibited by the CREB inhibitor KG-501[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.65mL

0.53mL

0.26mL

13.24mL

2.65mL

1.32mL

26.47mL

5.29mL

2.65mL
参考文献

[1]Lee JW, Park HS, Park SA, Ryu SH, Meng W, Jürgensmeier JM, Kurie JM, Hong WK, Boyer JL, Herbst RS, Koo JS. A Novel Small-Molecule Inhibitor Targeting CREB-CBP Complex Possesses Anti-Cancer Effects along with Cell Cycle Regulation, Autophagy Suppression and Endoplasmic Reticulum Stress. PLoS One. 2015 Apr 21;10(4):e0122628

[2]Best JL, Amezcua CA, Mayr B, Flechner L, Murawsky CM, Emerson B, Zor T, Gardner KH, Montminy M. Identification of small-molecule antagonists that inhibit an activator: coactivator interaction. Proc Natl Acad Sci U S A. 2004 Dec 21;101(51):17622-7

[3]Li J, Zhang Y, Zheng N, Li B, Yang J, Zhang C, Xia G, Zhang M. CREB activity is required for mTORC1 signaling-induced primordial follicle activation in mice. Histochem Cell Biol. 2020 Sep;154(3):287-299

[4]Sun H, Chung WC, Ryu SH, Ju Z, Tran HT, Kim E, Kurie JM, Koo JS. Cyclic AMP-responsive element binding protein- and nuclear factor-kappaB-regulated CXC chemokine gene expression in lung carcinogenesis. Cancer Prev Res (Phila). 2008 Oct;1(5):316-28

[5]Li TF, Wu HY, Wang YR, Li XY, Wang YX. Molecular signaling underlying bulleyaconitine A (BAA)-induced microglial expression of prodynorphin. Sci Rep. 2017 Mar 22;7:45056