Halofuginone is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/mL in mammal.
Halofuginone/常山酮 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Calu-3 cells
3 µM
marked resistance to SARS-CoV-2 infection
Nat Commun. 2021 Jun 23;12(1):3907.
Caco-2 cells
3 µM
18 h
marked reduction in endogenous TMPRSS2 protein expression
Nat Commun. 2021 Jun 23;12(1):3907.
Beas-2B cells
10 µM
18 h
reduce TMPRSS2-HiBiT abundance
Nat Commun. 2021 Jun 23;12(1):3907.
murine T cells
3.6 ± 0.4 nM
24 h
Selectively inhibited TH17 cell differentiation without affecting TH1, TH2, or iTreg cell differentiation
Science. 2009 Jun 5;324(5932):1334-8.
WM852, 501mel and 888mel human melanoma cell lines
200nM
24 h
Halofuginone significantly inhibited TGF-β-induced activity of the (CAGA)9 promoter in all the melanoma lines analyzed.
Cancer Res. 2012 Dec 1;72(23):6247-56.
Human 1205Lu melanoma cells
50-300nM
24, 48 and 72 h
Halofuginone 200 and 300nM treatments for 48 and 72 h significantly induced cell death.
Cancer Res. 2012 Dec 1;72(23):6247-56.
Human 1205Lu melanoma cells
200nM
4 h
Halofuginone pretreatment for 4 h followed by TGF-β treatment for 15 to 60 min significantly increased expression of Smad7 mRNA.
Cancer Res. 2012 Dec 1;72(23):6247-56.
Human 1205Lu melanoma cells
200nM
4 and 12 h
Halofuginone pretreatment for 4 and 12 h followed by 30 mins of TGF-β treatment decreased the levels of phosphoSmad2 and phosphoSmad3 levels, while total Smad2/3 levels remained unchanged.
To evaluate the effect of HF on gene expression in endothelial cells, results showed that HF increased VEGF gene expression and protein secretion, but had no significant effect on the gene expression of ANGPT-1, HIF-1α, TIMP2 and CXCL10, while ANGPT-2 expression was increased.
J Exp Clin Cancer Res. 2015 Jun 23;34(1):65.
NB4 cells
50, 100 or 200 ng/mL
6 h
To evaluate the effect of HF on gene expression in leukemic cells, results showed that HF down-regulated the expression of several pro-angiogenic factors, including HIF-1α, HGF, ANGPT-1 and ANGPT-2, while up-regulating the anti-angiogenic factors TIMP2 and CXCL10.
J Exp Clin Cancer Res. 2015 Jun 23;34(1):65.
human pancreatic stellate cells
50 nM and 100 nM
48 h
inhibition of α-SMA expression, reduction of fibrosis-related genes (e.g., type-I collagen and hyaluronan synthase-2), and inhibition of cell proliferation
Cancer Res. 2019 Jan 15;79(2):372-386.
murine pancreatic stellate cells
50 nM and 100 nM
48 h
inhibition of α-SMA expression, reduction of fibrosis-related genes (e.g., type-I collagen and hyaluronan synthase-2), and inhibition of cell proliferation
Cancer Res. 2019 Jan 15;79(2):372-386.
293T cells
50 nM
24 h
Halofuginone treatment significantly decreased the expression of NRF2-Δ100aa and NRF2-C but had no obvious effect on NRF2-N expression.
Redox Biol. 2022 Feb;49:102224.
NCTC 1469 cells
0–200 nM
24 h
Halofuginone treatment decreased the expression of NRF2, HO-1, and NQO-1.
Redox Biol. 2022 Feb;49:102224.
HepG2 cells
0–200 nM
24 h
Halofuginone treatment decreased the expression of NRF2, HO-1, and NQO-1, and this reduction was achieved via the proteasome pathway.
Redox Biol. 2022 Feb;49:102224.
breast cancer MCF-7 cells
100 nM
4, 8, 24 h
Induced both the AAR and the autophagy pathways time-dependently
Cell Commun Signal. 2019 May 2;17(1):39.
ovarian cancer OAW-42 cells
100 nM
4, 8, 24 h
Induced both the AAR and the autophagy pathways time-dependently
Cell Commun Signal. 2019 May 2;17(1):39.
thyroid cancer WRO cells
100 nM
4, 8, 24 h
Induced both the AAR and the autophagy pathways time-dependently
Halofuginone attenuates OA progression by inhibition of Th17-induced osteoclastogenesis, TGF-β-dependent Smad2/3 phosphorylation and angiogenesis
Ann Rheum Dis. 2016 Sep;75(9):1714-21
Nude mice
1205Lu melanoma bone metastasis model
Intraperitoneal (i.p.) injection
1 or 5µg/mouse
Daily until the end of the experiment
Preventive treatment with halofuginone significantly reduced osteolytic lesion area.
Cancer Res. 2012 Dec 1;72(23):6247-56.
NOD/SCID mice
Acute Promyelocytic Leukemia transplanted model
Intraperitoneal injection
150 μg/kg
Daily for 21 days
To evaluate the antileukemic effects of HF in vivo, results showed that HF treatment significantly reduced WBC counts, decreased accumulation of immature cells in the BM and spleen, and reduced the number of VEGF+ cells and VEGF gene expression.
J Exp Clin Cancer Res. 2015 Jun 23;34(1):65.
Mice
KrasG12D/+;p53R172H/+;Pdx-1-Cre (KPC) genetically engineered mouse model
Intraperitoneal injection
0.75 mg/kg
3 times/week, total of 5 doses
Reduced tumor volume growth, increased necrotic areas, improved drug distribution, and promoted anti-tumor immune cell infiltration
Cancer Res. 2019 Jan 15;79(2):372-386.
C57BL/6 mice
Regular chow-fed mice
Intraperitoneal injection
3 mg/kg
3 days
Halofuginone treatment decreased the protein expression of NRF2, HO-1, and NQO-1 in the liver.
Redox Biol. 2022 Feb;49:102224.
BALB/c nude mice
HCT116 xenograft model
Intraperitoneal injection
0.1 mg/kg
Once daily for 2 weeks
Retards tumor growth under both standard chow diet and caloric restriction conditions
United States, California
... 展开 >>
University of California, Davis Medical Center
Sacramento, California, United States, 95817
United States, Maryland
Kennedy Krieger Institute, Johns Hopkins School of Medicine
Baltimore, Maryland, United States, 21205
United States, Missouri
Washington University School of Medicine
Saint Louis, Missouri, United States, 63110
United States, Ohio
Cincinnati Children's Hospital Medical Center
Cincinnati, Ohio, United States, 45229
Nationwide Children's Hospital
Columbus, Ohio, United States, 43205 收起 <<
United States, California
... 展开 >>
University of California, Davis Medical Center
Sacramento, California, United States, 95817
United States, Maryland
Kennedy Krieger Institute, Johns Hopkins School of Medicine
Baltimore, Maryland, United States, 21205
United States, Missouri
Washington University School of Medicine
Saint Louis, Missouri, United States, 63110
United States, Ohio
Cincinnati Children's Hospital Medical Center
Cincinnati, Ohio, United States, 45229
Nationwide Children's Hospital
Columbus, Ohio, United States, 43205 收起 <<
United States, California
... 展开 >>
University of California, Davis Medical Center
Sacramento, California, United States, 95817
United States, Maryland
Kennedy Krieger Institute, Johns Hopkins School of Medicine
Baltimore, Maryland, United States, 21205
United States, Missouri
Washington University School of Medicine
Saint Louis, Missouri, United States, 63110
United States, Ohio
Cincinnati Children's Hospital Medical Center
Cincinnati, Ohio, United States, 45229
Nationwide Children's Hospital
Columbus, Ohio, United States, 43205 收起 <<
United States, California
... 展开 >>
University of California, Davis Medical Center
Sacramento, California, United States, 95817
United States, Maryland
Kennedy Krieger Institute, Johns Hopkins School of Medicine
Baltimore, Maryland, United States, 21205
United States, Missouri
Washington University School of Medicine
Saint Louis, Missouri, United States, 63110
United States, Ohio
Cincinnati Children's Hospital Medical Center
Cincinnati, Ohio, United States, 45229
Nationwide Children's Hospital
Columbus, Ohio, United States, 43205 收起 <<
United States, California
... 展开 >>
University of California, Davis Medical Center
Sacramento, California, United States, 95817
United States, Maryland
Kennedy Krieger Institute, Johns Hopkins School of Medicine
Baltimore, Maryland, United States, 21205
United States, Missouri
Washington University School of Medicine
Saint Louis, Missouri, United States, 63110
United States, Ohio
Cincinnati Children's Hospital Medical Center
Cincinnati, Ohio, United States, 45229
Nationwide Children's Hospital
Columbus, Ohio, United States, 43205 收起 <<
United States, California
... 展开 >>
University of California, Davis Medical Center
Sacramento, California, United States, 95817
United States, Maryland
Kennedy Krieger Institute, Johns Hopkins School of Medicine
Baltimore, Maryland, United States, 21205
United States, Missouri
Washington University School of Medicine
Saint Louis, Missouri, United States, 63110
United States, Ohio
Cincinnati Children's Hospital Medical Center
Cincinnati, Ohio, United States, 45229
Nationwide Children's Hospital
Columbus, Ohio, United States, 43205 收起 <<
Unspecified Adult Solid Tumor,... 展开 >> Protocol Specific 收起 <<
Phase 1
Completed
-
Belgium
... 展开 >> U.Z. Gasthuisberg
Leuven, Belgium, B-3000
Netherlands
University Hospital - Rotterdam Dijkzigt
Rotterdam, Netherlands, 3000 CA
Daniel Den Hoed Cancer Center at Erasmus Medical Center
Rotterdam, Netherlands, 3008 AE 收起 <<
搜索
