<生产厂家价格>

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。

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

Fungal recognition enhances mannose receptor shedding through dectin-1 engagement.

J. Biol. Chem. 286(10) , 7822-9, (2011)

The mannose receptor (MR) is an endocytic type I membrane molecule with a broad ligand specificity that is involved in both hemostasis and pathogen recognition. Membrane-anchored MR is cleaved by a me...

Development of a pluripotent stem cell derived neuronal model to identify chemically induced pathway perturbations in relation to neurotoxicity: effects of CREB pathway inhibition.

Toxicol. Appl. Pharmacol. 280(2) , 378-88, (2014)

According to the advocated paradigm shift in toxicology, acquisition of knowledge on the mechanisms underlying the toxicity of chemicals, such as perturbations of biological pathways, is of primary in...

Transcription factor cyclic adenosine monophosphate responsive element binding protein negatively regulates tumor necrosis factor alpha-induced protein 1 expression.

Mol. Med. Report. 12 , 7763-9, (2015)

Tumor necrosis factor alpha (TNFα)-induced protein 1 (TNFAIP1) was originally identified as a protein involved in DNA replication, DNA damage repair, apoptosis and the progression of certain diseases,...

更多文献