RK-33 demonstrates the ability to inhibit a variety of cancer cell types, with IC50 values ranging between 3-6 µM. However, the PC3 cell line exhibits a much lower sensitivity to RK-33, with an IC50 exceeding 12 µM. Treatment with RK-33 leads to a notable increase in the G1 phase population in DU145 and LNCaP cell lines. In contrast, 22Rv1 cells show only a slight increase in the G1 phase upon RK-33 treatment, along with a significant decrease in the G2 phase population. Additionally, RK-33 induces a moderate elevation in the G1 phase in 22Rv1 cells[1].
RK-33 细胞实验
Cell Line
Concentration
Treated Time
Description
References
U2OS human osteosarcoma cells
6 µM
1 hour
To evaluate the effect of RK-33 on SG assembly, the results showed that RK-33 significantly inhibited the assembly of G3BP1-positive SGs.
Biochem Pharmacol. 2020 Dec;182:114280.
RD cells
1 µM
1 hour
To study the effect of RK-33 on HCoV-OC43 infection, results showed that RK-33 significantly reduced viral titers.
Front Microbiol. 2022 Aug 25;13:959577.
Vero cells
0.01, 0.04, 0.16, 0.63, 1.25, 2.5, 10, 20, 50 µM
22 hours
To test the inhibitory effect of RK-33 on various viruses, results showed that RK-33 effectively inhibited the replication of DENV-2, ZIKV, WNV, RSV, and hPIV-3.
Cells. 2020 Jan 9;9(1):170.
MDA-MB-435 cells
4.5 µM
24 hours
To evaluate changes in the protein landscape after RK-33 treatment, changes in mitochondrial translation, cell division, and cell cycle-related proteins were observed.
Transl Oncol. 2018 Jun;11(3):755-763.
MCF7 cells
1.5 µM, 3 µM, 4.5 µM
24 hours
To evaluate the effect of RK-33 on the cell cycle using the FUCCI system, a delay in all cell cycle phases was observed.
Transl Oncol. 2018 Jun;11(3):755-763.
Calu-3 cells
5 µM
24 hours
To study the effect of RK-33 on SARS-CoV-2 infection, results showed that RK-33 significantly reduced viral load and downregulated most SARS-CoV-2 gene expressions.
Front Microbiol. 2022 Aug 25;13:959577.
SW1990 SP cells
4.32 µM (IC50)
48 hours
To evaluate the effect of RK-33 on cancer stem cell markers, results showed that RK-33 significantly downregulated the expression of CD44v6, NANOG, SOX9, and β-CATENIN.
Gastroenterology. 2020 Nov;159(5):1898-1915.e6.
Capan1 SP cells
5.53 µM (IC50)
48 hours
To evaluate the effect of RK-33 on cancer stem cell markers, results showed that RK-33 significantly downregulated the expression of CD44v6, NANOG, SOX9, and β-CATENIN.
Gastroenterology. 2020 Nov;159(5):1898-1915.e6.
9–26 NP fibroblasts
9.23 µM (IC50)
48 hours
To evaluate the effect of RK-33 on normal fibroblasts, results showed that RK-33 had lower toxicity to normal cells.
Gastroenterology. 2020 Nov;159(5):1898-1915.e6.
Human lung fibroblasts
1 or 10 µM
48 hours
RK-33 inhibited TGF-β1-induced upregulation of NEU3
JCI Insight. 2023 Apr 10;8(7):e167566.
A549 cells (high DDX3 expression)
1 µM and 2 µM
72 hours
To evaluate the cytotoxicity of RK-33 on lung cancer cells, results showed that cells with high DDX3 expression were more sensitive to RK-33
EMBO Mol Med. 2015 May;7(5):648-69.
H3255 cells (low DDX3 expression)
1 µM and 2 µM
72 hours
To evaluate the cytotoxicity of RK-33 on lung cancer cells, results showed that cells with high DDX3 expression were more sensitive to RK-33
EMBO Mol Med. 2015 May;7(5):648-69.
MCF10A
7.4 µM (IC50)
72 hours
To evaluate the cytotoxicity of RK-33 on normal breast cells MCF10A, results showed that MCF10A was less sensitive to RK-33
Oncogene. 2018 Jan 4;37(1):63-74.
MCF7
2.8–4.5 µM (IC50)
72 hours
To evaluate the cytotoxicity of RK-33 on breast cancer cells MCF7, results showed that MCF7 was more sensitive to RK-33
Oncogene. 2018 Jan 4;37(1):63-74.
MDA-MB-231
2.8–4.5 µM (IC50)
72 hours
To evaluate the cytotoxicity of RK-33 on breast cancer cells MDA-MB-231, results showed that MDA-MB-231 was more sensitive to RK-33
Oncogene. 2018 Jan 4;37(1):63-74.
MDA-MB-435
2.8–4.5 µM (IC50)
72 hours
To evaluate the cytotoxicity of RK-33 on breast cancer cells MDA-MB-435, results showed that MDA-MB-435 was more sensitive to RK-33
Oncogene. 2018 Jan 4;37(1):63-74.
Rat primary cortical neurons
1 µM
72 hours
To validate the neuroprotective effects of RK-33 against the combined neurotoxicity of HIV Tat and cocaine, results showed RK-33 significantly reduced neuronal death
J Neuroimmune Pharmacol. 2020 Jun;15(2):209-223.
Marc-145 cells
8.495 µM
72 hours
RK-33 inhibits DDX3X expression and reduces PRRSV replication.
Vet Res. 2024 Aug 18;55(1):103.
DAOY cells
2.5 µM
72 hours
RK-33 inhibited the growth and promoted cell death in DAOY cells with an IC50 value of 2.5 μM.
Transl Oncol. 2019 Jan;12(1):96-105.
UW228 cells
3.5 µM
72 hours
RK-33 inhibited the growth and promoted cell death in UW228 cells with an IC50 value of 3.5 μM.
Transl Oncol. 2019 Jan;12(1):96-105.
A549, H1299, H23, and H460 cells
4.4–8.4 µM (IC50)
To evaluate the cytotoxicity of RK-33 on lung cancer cells, results showed that cells with high DDX3 expression were more sensitive to RK-33
EMBO Mol Med. 2015 May;7(5):648-69.
H3255 cells
> 25 µM (IC50)
To evaluate the cytotoxicity of RK-33 on lung cancer cells, results showed that cells with high DDX3 expression were more sensitive to RK-33
EMBO Mol Med. 2015 May;7(5):648-69.
DU145
3 µM (IC50)
RK-33 inhibited proliferation and induced G1 phase cell-cycle arrest in DU145 cells.
Cancer Res. 2016 Nov 1;76(21):6340-6350.
LNCaP
6 µM (IC50)
RK-33 inhibited proliferation and induced G1 phase cell-cycle arrest in LNCaP cells.
Cancer Res. 2016 Nov 1;76(21):6340-6350.
22Rv1
3–6 µM (IC50)
RK-33 inhibited proliferation and induced G1 phase cell-cycle arrest in 22Rv1 cells.
Cancer Res. 2016 Nov 1;76(21):6340-6350.
PC3
12 µM (IC50)
RK-33 had minimal effects on PC3 cells, with no significant changes in cell cycle.
Cancer Res. 2016 Nov 1;76(21):6340-6350.
RK-33 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Twist1/KrasG12D autochthonous lung tumor model
Intraperitoneal injection
20 mg/kg
Twice a week for 7 weeks
To evaluate the effect of RK-33 in combination with radiation, results showed that RK-33 significantly enhanced radiation-induced tumor regression
EMBO Mol Med. 2015 May;7(5):648-69.
C57BL/6 mice
Bleomycin-induced pulmonary fibrosis model
Intraperitoneal injection
20 mg/kg
Every 2 days for 11 days
RK-33 potentiated survival, reduced lung inflammation and fibrosis, and decreased tissue levels of DDX3, TGF-β1, and NEU3
JCI Insight. 2023 Apr 10;8(7):e167566.
SCID mice
DU145-Luc xenograft model
Intraperitoneal injection
50 mg/kg
Thrice weekly for two weeks
The combination of RK-33 and radiation significantly reduced tumor growth and induced more apoptosis.
Cancer Res. 2016 Nov 1;76(21):6340-6350.
Nude mice
Medulloblastoma xenograft model
Intraperitoneal injection
50 mg/kg
Every alternate day for two weeks
The combination of RK-33 and 5 Gy radiation caused tumor regression in a mouse xenograft model of medulloblastoma.
Transl Oncol. 2019 Jan;12(1):96-105.
RK-33 动物研究
Animal study
The combination of RK-33 and radiation in mice leads to increased cell death, characterized by pyknotic or condensed nuclei, mixed with fibrin and interstitial edema, in tumors compared to those treated with control or single treatments. This combined treatment approach shows superiority in diminishing tumor proliferation[1]. In mice that received RK-33-PLGA treatment, RK-33 was present in the plasma at a concentration of 34 μg/mL and in the liver at 28 μg/g, while no RK-33 was detected in the lungs[2].
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