BCI is a DUSP6 inhibitor. BCI has anti-inflammatory activity and reduces the production of reactive oxygen species (ROS). BCI can be used in inflammatory disease studies[1][2].At a concentration of 100 ng/mL for 24 h, BCI down-regulated DUSP6 expression in RAW264.7 macrophages. At a concentration of 1 nM for 24 h, BCI inhibited the expression of IL-1β and IL-6 in lipid LPS-activated macrophages. At a concentration of 4 nM for 24 h, BCI reduced ROS production and activated the Nrf2 pathway in LPS-activated macrophages[2].
BCI 细胞实验
Cell Line
Concentration
Treated Time
Description
References
STS26T MPNST cells
2-4 μM
72 h
Evaluate the effect of BCI on MPNST cell growth, results showed cells were less sensitive to BCI
Clin Cancer Res. 2019 Jul 1;25(13):4117-4127.
iHSC-1λ Schwann cells
2-4 μM
72 h
Evaluate the effect of BCI on Schwann cell growth, results showed cells were less sensitive to BCI
Clin Cancer Res. 2019 Jul 1;25(13):4117-4127.
S462.TY MPNST cells
2-4 μM
72 h
Evaluate the effect of BCI on MPNST cell growth, results showed BCI significantly inhibited cell growth
Clin Cancer Res. 2019 Jul 1;25(13):4117-4127.
ST8814 MPNST cells
2-4 μM
72 h
Evaluate the effect of BCI on MPNST cell growth, results showed BCI significantly inhibited cell growth
Clin Cancer Res. 2019 Jul 1;25(13):4117-4127.
HeLa cells
10 μM
15 min
BCI treatment restored p-ERK levels in Dusp6-Myc transfected cells, indicating that BCI directly inhibited Dusp6-Myc function
Nat Chem Biol. 2009 Sep;5(9):680-7.
Mouse bone marrow-derived macrophages (BMMs)
1 μM
6 days
To investigate the effect of (E/Z)-BCI on osteoclast differentiation, results showed that (E/Z)-BCI significantly accelerated osteoclastogenesis.
Cell Death Dis. 2021 Sep 2;12(9):825.
BaF3 cells
400 nM
1 week
To evaluate the effect of BCI on CSF3R mutant-induced CFU formation, results showed that BCI alone or in combination with ruxolitinib significantly suppressed CSF3R mutant-induced CFU formation.
Blood Adv. 2024 Jun 11;8(11):2765-2776.
SH-SY5Y neuroblastoma cells
5 μM
24 h
BCI enhances P2X7 receptor expression
Front Cell Dev Biol. 2022 Dec 15;10:1049566.
N2a neuroblastoma cells
5 μM
24 h
BCI enhances P2X7 receptor expression
Front Cell Dev Biol. 2022 Dec 15;10:1049566.
BCI 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Jak2V617F-induced MPN model
Oral
100 mg/kg
Daily, for 40 weeks
Evaluate the selective eradication effect of BCI on Jak2V617F clones
Leukemia. 2023 Aug;37(8):1686-1697.
Zebrafish
Ventricular resection model
Intraperitoneal injection
10 µM
Once daily until hearts were collected
BCI promotes heart regeneration by inhibiting Dusp6
Cell Res. 2014 Sep;24(9):1091-107
Nude mice
S462.TY cell line xenograft model
Intraperitoneal injection
10 mg/kg
Once daily, 5x/wk for 27 days
Evaluate the effect of BCI on MPNST xenograft model, results showed no significant difference in tumor volume but tumor tissue exhibited necrosis
Clin Cancer Res. 2019 Jul 1;25(13):4117-4127.
Zebrafish
Transgenic zebrafish embryos
Immersion
5 μM
From the 1000-cell stage
BCI treatment enhanced FGF signaling, leading to increased transcription of several FGF target genes
Nat Chem Biol. 2009 Sep;5(9):680-7.
C57BL/6J mice
Ovariectomy-induced osteoporosis model
Intraperitoneal injection
30 mg/kg
Twice a week for 6 weeks
To investigate the effect of (E/Z)-BCI on osteoporosis in vivo, results showed that (E/Z)-BCI significantly accelerated the bone loss process.
Cell Death Dis. 2021 Sep 2;12(9):825.
NSG mice
Orthotopic model of prostate cancer
Intraperitoneal injection
10 mg/kg
Five consecutive days per week, until experimental endpoint
BCI inhibits DUSP6 activity and prevents tumor formation induced by FBXO31 knockout
Cell Rep. 2021 Oct 19;37(3):109870
Mice
Conventionally-raised wild-type mice and Dusp6-deficient mice
Intraperitoneal injection
5 μg/g
Once a day during CR period
Investigate the role of DUSP6 inhibitor BCI in maintaining cold-adapted microbiota and promoting white adipose tissue browning after cold exposure
NPJ Biofilms Microbiomes. 2024 Mar 13;10(1):22
Mice
CSF3R-induced leukemia model
Intraperitoneal injection
10 mg/kg
Twice daily for 8 weeks
To evaluate the therapeutic effect of BCI alone or in combination with trametinib on CSF3R-induced leukemia, results showed that the combination of BCI and trametinib successfully cured the leukemia in mice.
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