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色酚AS-E磷酸盐

色酚AS-E磷酸盐用途

KG-501 是 CREB 的抑制剂，其 IC₅₀ 值为 6.89 μM。

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色酚AS-E磷酸盐名称

[ CAS 号 ]:
18228-17-6

[ 中文名 ]:
磷酸萘酚AS-E

[ 英文名 ]:
KG-501

[中文别名 ]:

[英文别名 ]:

naphthol as-e phosphate
KG-501

色酚AS-E磷酸盐生物活性

[ 描述 ]:

KG-501 是 CREB 的抑制剂,其 IC50 值为 6.89 μM。

[ 相关类别 ]:

信号通路 >> 表观遗传学 >> 表观遗传读者域

研究领域 >> 炎症/免疫

[ 靶点 ]

IC50: 6.89 μM (CREB)[1].

[体外研究]

KG-501直接靶向CBP的KIX结构域,导致CREB-CBP复合物被破坏,抑制CREB靶基因诱导,并抑制IL-1β介导的NSCLC血管生成活性[1]。使用在结合测定的线性范围内的CREB浓度,KG-501破坏磷酸(Ser-133)CREB与KIX结合,Ki为~90μM。用KG-501处理HEK293T细胞也阻断了毛喉素诱导内源性CREB靶基因(NR4A2,αCG,c-fos和RGS2),表明KG-501可能对CREB活性产生一般影响[2]。 KG-501还可以抑制NF-κB转录活性,因为NF-κB也使用CBP作为辅因子来调节基因表达。由IL-1β加10μMKG-501处理的A549细胞的CM诱导的HUVEC迁移显着低于单独用IL-1β处理的A549细胞CM诱导的HUVEC迁移。在10μM时,KG-501抑制除CXCL8外的所有IL-1β诱导的CXC趋化因子基因的表达。对于蛋白质水平,KG-501显着抑制IL-1β诱导的CXCL5蛋白分泌。在H1734细胞系中也观察到KG-501的类似作用[3]。

[参考文献]

[1]. Lee JW, et al. 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 et al. 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]. Sun H, et al. 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.

[相关活性小分子]

(+)-JQ1 | GSK126 | Tazemetostat (EPZ-6438) | 比拉瑞塞 | A-485 | 姜黄素 | ARV-771 | ARV-825 | (4S)-6-(4-氯苯基)-N-乙基-8-甲氧基-1-甲基-4H-[1,2,4]三唑并[4,3-A][1,4]苯并二氮杂卓-4-乙酰胺 | BI 2536 | 1-异丙基-N-[(6-甲基-2-氧代-4-丙基-1,2-二氢-3-吡啶基)甲基]-6-[2-(4-甲基-1-哌嗪基)-4-吡啶基]-1H-吲唑-4-甲酰胺 | C646 | 3-去氮腺嘌呤A | 7-(3,5-二甲基异噁唑-4-基)-8-甲氧基-1-((R)-1-(吡啶-2-基)乙基)-1H-咪唑并[4,5-C]喹啉-2(3H)-酮 | 化合物3i(666-15)

色酚AS-E磷酸盐物理化学性质

[ 密度 ]:
1.567g/cm3

[ 分子式 ]:
C₁₇H₁₃ClNO₅P

[ 分子量 ]:
377.71600

[ 精确质量 ]:
377.02200

[ PSA ]:
105.67000

[ LogP ]:
4.29000

[ 外观性状 ]:
粉末

[ 折射率 ]:
1.723

[ 储存条件 ]:
-20℃

色酚AS-E磷酸盐MSDS

详细MSDS(安全技术说明书)

色酚AS-E磷酸盐安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

色酚AS-E磷酸盐文献

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