货号:A1340294 同义名: 1,4-dihydrophenonthrolin-4-one-3-Carboxylic acid
1,4-DPCA是一种有效的脯氨酰-4-羟化酶抑制剂,IC50 为 2.4 μM,能够抑制 HIF-1α 的降解,从而稳定 HIF-1α 蛋白,同时抑制 FIH,IC50 为 60 μM,适用于缺氧相关疾病及纤维化的研究。
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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 | 1,4-DPCA is a potent inhibitor of prolyl-4-hydroxylase with an IC50 of 2.4 µM in human foreskin fibroblasts. 1,4-DPCA can inhibit the α isoenzyme of prolyl-4-hydroxylase and stabilize HIF-1α protein. 1,4-DPCA also inhibits factors that inhibit HIF with an IC50 of 60 µM[1][2].In mouse B6 cells, 1,4-DPCA specifically increases the expression of several target genes, including the pro-angiogenic targets Vegfa and Hmox1, and the proglycolytic targets Ldh-a, Pgk1, Pdk1, and Glut1, after 24 hours of treatment[1].1,4-DPCA significantly reduced cell colony size in T4-2 (10 μM) and ZR-75-1 cells (20 μM). T4-2 cells treated with 1,4-DPCA formed polarised spheroids in three-dimensional cultures. 1,4-DPCA treatment significantly reduced invasive branching in DA-MB-157 (20 μM) and MDA-MB-231 (10 μM) cells[3]. |
Animal study | 1,4-DPCA inhibited the growth of connective tissue resulting from PLGA discs implanted in the abdominal cavity of mice 28 days after implantation. It was found that 1,4-DPCA was effective in inhibiting collagen deposition on the internal and external surfaces of the discs, as well as limiting connective tissue growth, but not to the same extent as glucocorticoids[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
4.16mL 0.83mL 0.42mL |
20.81mL 4.16mL 2.08mL |
41.63mL 8.33mL 4.16mL |
CAS号 | 331830-20-7 |
分子式 | C13H8N2O3 |
分子量 | 240.214 |
别名 | 1,4-dihydrophenonthrolin-4-one-3-Carboxylic acid |
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: 12 mg/mL(49.96 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 |