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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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+ |
规格 | 价格 | 会员价 | 库存 | 数量 | |||
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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。 |
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] . |
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 |
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 |