GN44028 free base · Synonyms: GN-44028 · GN 44028

GN44028 is a potent and orally active hypoxia inducible factor-1α inhibitor.

For research use only. Not for human or veterinary use.

Target HIF/HIF Prolyl-Hydroxylase

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

GN44028 structure

CAS No.: 1421448-26-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 520.00	BP-01887-250mg	In stock	Get quote
500 mg	USD 880.00	BP-01887-500mg	In stock	Get quote
1 g	USD 1,380.00	BP-01887-1g	In stock	Get quote
5 g	Inquire	BP-01887-5g	Inquire	Inquire

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Description

GN44028 is a potent and orally active hypoxia inducible factor (HIF)-1α inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization. GN44028 can be used in the research of cancers.

Biological activity

In Vitro GN44028 (compound 2I, 0-30 μM approximately) has anti-proliferative activities against HCT116, HepG2 and HeLa cells. GN44028 (0.001-1 μM, 4 h) inhibits the hypoxia-induced VEGF mRNA expression in HeLa cells. GN44028 (20 nM, 10 days) abrogates the TGF‐β‐induced colony formation in HCT116 cells. In Vivo GN44028 (10 mg/kg, oral gavage) extends the survival rate of animals in mice bearing a mixed orthotopic tumor with PN12 and ME23 cells. GN44028 (5 mg/kg, tail vein injection, twice a week) suppresses tumor growth in a subcutaneous colorectal cancer model.

Identifiers

SMILES: C1(NC2=CC=C(OCCO3)C3=C2)=NNC4=C1CC5=CC=CC=C45
InChIKey: CGZKSZVSWAAUHE-UHFFFAOYSA-N

Specifications

MW (average): 305.3306
Formula: C₁₈H₁₅N₃O₂
CAS No.: 1421448-26-1
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month

Solubility

Soluble in DMSO : 50 mg/mL

Documents

References

[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.

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