FOXM1 is a transcription factor from the Forkhead box (FOX) family that is critical for the differentiation of goblet cells from airway progenitor cells. RCM-1 is a FOXM1 inhibitor which inhibits goblet cell metaplasia and IL-13 signaling, and RCM-1 is used to treat patients with asthma and other chronic airway diseases. RCM-1 inhibited GFP-FOXM1 with an EC50 of 0.72 μM in U2OS cells. Furthermore, RCM-1 inhibited the expression of FOXM1 target genes Plk1 and Cdc25B, a functional readout of FOXM1 transcriptional activity. In addition to GFP-FOXM1, RCM-1 decreased the abundance of endogenous FOXM1 in primary human airway epithelial cells cultured on an air-liquid interface without altering that of other transcription factors. In vivo, RCM-1 treatment decreased the abundance of endogenous FOXM1 in wild-type BALB/c mice. RCM-1 protected lungs from HDM-induced airway hyperreactivity and preserved lung function in BALB/c mice. Moreover, RCM-1 decreased goblet cell metaplasia and airway resistance and improved lung function in IL-13-treated mice[2].
RCM-1 细胞实验
Cell Line
Concentration
Treated Time
Description
References
mouse pancreatic adenocarcinoma KPC-2 cells
mouse pancreatic adenocarcinoma KPC-2 cells
To assess the effect of RCM-1 on cancer cell proliferation, results showed that RCM-1 significantly inhibited the growth of KPC-2 cells
Mol Cancer Ther. 2019 Jul;18(7):1217-1229.
mouse prostate adenocarcinoma MyC-CaP cells
mouse prostate adenocarcinoma MyC-CaP cells
To assess the effect of RCM-1 on cancer cell proliferation, results showed that RCM-1 significantly inhibited the growth of MyC-CaP cells
Mol Cancer Ther. 2019 Jul;18(7):1217-1229.
mouse breast carcinoma 4T1 cells
mouse breast carcinoma 4T1 cells
To assess the effect of RCM-1 on cancer cell proliferation, results showed that RCM-1 significantly inhibited the growth of 4T1 cells
Mol Cancer Ther. 2019 Jul;18(7):1217-1229.
human lung adenocarcinoma H2122 cells
human lung adenocarcinoma H2122 cells
To assess the effect of RCM-1 on cancer cell proliferation, results showed that RCM-1 significantly inhibited the growth of H2122 cells
Mol Cancer Ther. 2019 Jul;18(7):1217-1229.
mouse melanoma B16-F10 cells
mouse melanoma B16-F10 cells
To assess the effect of RCM-1 on cancer cell proliferation, results showed that RCM-1 significantly inhibited the growth of B16-F10 cells
Mol Cancer Ther. 2019 Jul;18(7):1217-1229.
mouse rhabdomyosarcoma Rd76–9 cells
mouse rhabdomyosarcoma Rd76–9 cells
To assess the effect of RCM-1 on cancer cell proliferation, results showed that RCM-1 significantly inhibited the growth of Rd76–9 cells
Mol Cancer Ther. 2019 Jul;18(7):1217-1229.
BGC823 cells
BGC823 cells
RCM-1 enhances the interaction between RNF112 and FOXM1
JCI Insight. 2023 Jun 8;8(11):e166698.
MGC803 cells
MGC803 cells
RCM-1 enhances the interaction between RNF112 and FOXM1
JCI Insight. 2023 Jun 8;8(11):e166698.
human induced pluripotent stem cell–derived cardiomyocytes (hiPSC-CMs)
human induced pluripotent stem cell–derived cardiomyocytes (hiPSC-CMs)
FOXM1 inhibition promoted maturational characteristics such as increased contractility, oxygen consumption, and voltage peak maximum upstroke velocity.
J Am Heart Assoc. 2024 Jul 2;13(13):e033155.
RCM-1 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Rhabdomyosarcoma Rd76–9 model
Intraperitoneally (IP)
20 mg/kg
Once daily for 7 days
To evaluate the inhibitory effect of RCM-1 on tumor growth, results showed that RCM-1 significantly reduced tumor volume, decreased FOXM1 expression, reduced tumor cell proliferation and increased apoptosis
Mol Cancer Ther. 2019 Jul;18(7):1217-1229.
Nude mice
Xenograft tumor model
Intraperitoneal injection
20 mg/kg
Every 3 days until the sacrifice day
RCM-1 inhibits gastric cancer proliferation partially dependent on RNF112
JCI Insight. 2023 Jun 8;8(11):e166698.
C57BL/6 mice
Diabetic encephalopathy model
Oral gavage
0.75 g/kg, 1.5 g/kg, 3 g/kg
Once daily for 15 weeks
To evaluate the effects of RCM-1 on cognitive function and neuronal injury in diabetic encephalopathy model mice. Results showed that RCM-1 significantly improved cognitive function, alleviated hippocampal neuronal injury, and upregulated the expression of Nav1.1 and Nav1.2.
Front Pharmacol. 2025 Mar 14;16:1542015
Mice
Hymenolepis nana infection model
Intraperitoneal injection
1.7 mg/kg
Seven consecutive days
RCM-1 inhibited the immune responses induced by H. nana and its excretory-secretory products (ESP), affecting the host's ability to eliminate H. nana
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