产品说明书

GN44028

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Chemical Structure| 1421448-26-1 同义名 : -
CAS号 : 1421448-26-1
货号 : A1172999
分子式 : C18H15N3O2
纯度 : 99%+
分子量 : 305.331
MDL号 : MFCD30182340
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
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：
生物活性
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].
实验方案
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
参考文献

[1]Minegishi H, et al. Discovery of Indenopyrazoles as a New Class of Hypoxia Inducible Factor (HIF)-1 Inhibitors. ACS Med Chem Lett. 2013 Jan 27;4(2):297-301.

[2]Changfu Liu, et al. Tumor-associated macrophage-derived transforming growth factor-β promotes colorectal cancer progression through HIF1-TRIB3 signaling. Cancer Sci. 2021 Oct;112(10):4198-4207.

[3]Xiaoqing Fan, et al. Heterogeneity of subsets in glioblastoma mediated by Smad3 palmitoylation. Oncogenesis. 2021 Oct 27;10(10):72.