ARN-3236 是一种选择性且口服可利用的盐诱导激酶 2 (SIK2) 抑制剂,对 SIK2 的 IC50 值小于 1 nM,对 SIK1 和 SIK3 的 IC50 值分别为 21.63 nM 和 6.63 nM。ARN-3236 具有抗肿瘤活性。 GN44028 是一种高效的口服活性 HIF-1α 抑制剂,其 IC50 值为 14 nM。
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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 | GN44028 is a potent, orally active HIF-1α inhibitor with an IC50 value of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity, but not HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerisation[1][3].At concentrations less than 30 µM, GN44028 has antiproliferative activity against HCT116, HepG2 and HeLa cells. At a concentration of less than 1 µM for 4 hours, GN44028 inhibited hypoxia-induced VEGF mRNA expression in HeLa cells[1].At a concentration of 20 nM for 10 days, GN44028 inhibited TGF-β-induced colony formation in HCT116 cells[2]. |
Animal study | Administered orally at a dose of 10 mg/kg, GN44028 prolongs the survival of mice bearing mixed orthotopic tumours of PN12 and ME23 cells[3].At a dose of 5 mg/kg, administered by tail vein injection twice weekly, GN44028 inhibited tumour growth in a subcutaneous colorectal cancer model (HCT116)[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.28mL 0.66mL 0.33mL |
16.38mL 3.28mL 1.64mL |
32.75mL 6.55mL 3.28mL |
CAS号 | 1421448-26-1 |
分子式 | C18H15N3O2 |
分子量 | 305.331 |
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 Keep in dark place,Sealed in dry,2-8°C |
溶解度 |
DMSO: 50 mg/mL(163.76 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 |