FM19G11是一种HIF-1α抑制剂,能够有效阻断缺氧诱导的信号通路。它不仅抑制HIF-1α的活性,还调节其他相关信号途径,如mTOR和PI3K/Akt/eNOS,在癌症研究中具有广泛应用前景。
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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+ |
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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 | FM19G11 is a hypoxia-inducible factor-1-alpha (HIF-1α) inhibitor, suppresses hypoxia-induced luciferase activity with an IC50 of 80 nM in HeLa cells. It also influences other signaling pathways, including mTOR and PI3K/Akt/eNOS, when the HIF-1α pathway is inactive under normoxic conditions[1].[2]. |
体内研究 | Through intramedullary injection over 1-8 weeks, FM19G11 improves locomotion in severe spinal cord injury (SCI)[3]. After 8 weeks of intramedullary injection, FM19G11 induces the expression of GAP43, an axon growth marker, and RIP, a marker for myelinated oligodendrocytes, at the injury site[3]. |
体外研究 | In HeLa cell lines, FM19G11 at concentrations ranging from 30-300 nM inhibits HIFα proteins. Under hypoxic conditions, FM19G11 at 500 nM promotes oligodendrocyte differentiation[1]. Administered at 300 nM for 3 days, FM19G11 significantly reduces the mRNA levels of O6-methylguanine DNA-methyltransferase (MGMT) in hypoxic GBM‐XD, hypoxic T98G, and normoxic T98G cells[2]. FM19G11, when combined with temozolomide (TMZ), significantly enhances the pro‐apoptotic effect of TMZ, although FM19G11 alone does not induce apoptosis[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.16mL 0.43mL 0.22mL |
10.79mL 2.16mL 1.08mL |
21.58mL 4.32mL 2.16mL |
CAS号 | 329932-55-0 |
分子式 | C23H17N3O8 |
分子量 | 463.396 |
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(226.59 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 |