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KG-548 {[allProObj[0].p_purity_real_show]}

货号:A117262

KG-548是一种 ARNT/TACC3 干扰子,能够通过与 TACC3 竞争结合 ARNT 的 PAS-B 结构域来抑制 HIF-1α 活性,适用于缺氧条件下的肿瘤研究。ARNT 是芳基烃受体核转位蛋白 (HIF-β),在癌症研究中具有重要作用。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
KG-548 化学结构 CAS号:175205-09-1
KG-548 化学结构
CAS号:175205-09-1
KG-548 3D分子结构
CAS号:175205-09-1
KG-548 化学结构 CAS号:175205-09-1
KG-548 3D分子结构 CAS号:175205-09-1
规格 价格 会员价 库存 数量
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KG-548 纯度/质量文件 产品仅供科研

货号:A117262 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 HIF HIF1 PHD1 PHD2 PHD3 其他靶点 纯度
KC7F2 +

HIF-1α, IC50: 20 μM

+

HIF-1α, IC50: 20 μM

98%
Lificiguat 99%+
BAY 87-2243 99%+
PX-478·2HCl 98%+
2-Methoxyestradiol 98%
CAY10585 ++

HIF, IC50: 4.4 μM

BCRP 97%
DMOG 98%
FG 2216 ++

PHD2, IC50: 3.9 μM

99%+
MK-8617 ++++

PHD1, IC50: 1 nM

++++

PHD2, IC50: 1 nM

++++

PHD3, IC50: 14 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

KG-548 生物活性

描述 KG-548 is an ARNT/TACC3 binding blocker and HIF-1α inhibitor. KG-548 directly interferes with the formation of the ARNT/TACC3 complex by competing with TACC3 for binding to the PAS-B structural domain of ARNT. ARNT is an aryl hydrocarbon receptor nuclear transporter, also known as HIF-β[1][2].At concentrations of 0-250 μM for 16 hours to overnight, KG-548 significantly reduces the formation of the ARNT/CCC complex of both co-activators and also disrupts the ARNT2 PAS-B/TACC3 interaction. And at concentrations of 0-2 mM, KG-548 dose-dependently disassembled (320 μM) ARNT PAS-B/TACC3 complexes in vitro and in cell lysates with an IC50 value of 25 μM[1].KG-548 significantly inhibited lactate production from glycolysis in FaDu cells[2] .

KG-548 参考文献

[1]Guo Y, et al. Regulating the ARNT/TACC3 axis: multiple approaches to manipulating protein/protein interactions with small molecules. ACS Chem Biol. 2013 Mar 15;8(3):626-35.

[2]Kleszcz R, et al. The inhibition of c-MYC transcription factor modulates the expression of glycolytic and glutaminolytic enzymes in FaDu hypopharyngeal carcinoma cells. Adv Clin Exp Med. 2018 Jun;27(6):735-742.

KG-548 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.54mL

0.71mL

0.35mL

17.72mL

3.54mL

1.77mL

35.44mL

7.09mL

3.54mL

KG-548 技术信息

CAS号175205-09-1
分子式C9H4F6N4
分子量 282.145
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 105 mg/mL(372.15 mM),配合低频超声助溶,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

动物实验配方
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