Rapamycin inhibits endogenous mTOR activity in HEK293 cells with IC50 of ~0.1 nM, more potently than iRap and AP21967 with IC50 of ~5 nM and ~10 nM, respectively. In Saccharomyces cerevisiae, Rapamycin treatment induces a severe G1/S cell cycle arrest and inhibition of translation initiation to levels below 20% of control. Rapamycin significantly inhibits the cell viability of T98G and U87-MG in a dose-dependent manner with IC50 of 2 nM and 1 μM, respectively, while displaying little activity against U373-MG cells with IC50 of >25 μM despite the similar extent of the inhibition of mTOR signaling. Rapamycin (100 nM) induces G1 arrest and autophagy but not apoptosis in Rapamycin-sensitive U87-MG and T98G cells by inhibiting the function of mTOR.
Rapamycin/西罗莫司 细胞实验
Cell Line
Concentration
Treated Time
Description
References
MEFs
5 µMol
3 hours
To induce autophagy and analyze LC3B expression.
Adv Sci (Weinh). 2022 Jan;9(3):e2102568.
Yeast cells
1 µM
5 min
Disruption of mismatch repair
Nucleic Acids Res. 2021 Sep 20;49(16):9327-9341.
CD25+ cells
100 ng/ml
days 4, 7, 11 and 18
To facilitate ex vivo CD25+ cell expansion.
Gut. 2023 Jan;72(1):49-53.
Yeast cells
1 ng/ul
1 hour
Induce CICI formation
Nat Commun. 2022 Feb 9;13(1):757.
Huh7 cells
20 nM
24 hours
To monitor autophagic flux as a positive control and its effects.
Redox Biol. 2021 Oct;46:102081.
Yeast cells
200 nM
1.5 hours
To study the upregulation of RPACs and the effects on proteasome assembly under TORC1 inhibition.
To examine translational activity at the whole-transcriptome level by ribosome profiling.
Sci Adv. 2020 Aug 12;6(33):eabb8771.
Raw264.7 cells
10 µM
2 hours
To evaluate the role of mTOR in BSNP-induced trained immunity, assessing inflammatory cytokine expression and phagocytosis.
Theranostics. 2022 Jan 1;12(2):675-688.
DLD1 cells
100 ng/ml
2 hours
To drive chemically induced dimerisation of TEV, and, as a result, PKCε cleavage
Nat Commun. 2020 Mar 13;11(1):1396.
F98 astrocytoma cells
100 nM
24 hours
To investigate the cytoprotective effect of rapamycin against GO-induced apoptosis.
J Nanobiotechnology. 2020 Mar 18;18(1):52.
MDMs
10 nM
24 hours
To investigate the effect of metabolic reprogramming on cytokine production.
Nat Commun. 2020 May 8;11(1):2282.
HL60 and U937 cells
500 mg/mL
24 hours
To evaluate the cytokine profiles and elimination capacity of CAR-T cells; rapamycin-pretreated exhibited lower AML residues.
Clin Cancer Res. 2021 Nov 1;27(21):6026-6038.
MLE-12 cells
10 μg/ml
24 hours
To explore the effect of autophagy activation with rapamycin treatment on SWCNTs-induced senescence and FMT in MLE-12 cells.
J Nanobiotechnology. 2023 Feb 28;21(1):69.
Human Renal Proximal Tubular Cells
100 nM
24 hours
To investigate the effect of rapamycin on GLUT2 expression under hyperglycemic conditions.
Nat Commun. 2022 Apr 4;13(1):1783.
RPE cells
100 nM
24 hours
To determine optimal drug concentration and its time-dependent response; no significant difference was observed comparing treatments to no treatment controls.
Redox Biol. 2020 Jul;34:101552.
Myotubes cells
10 nM
24 hours
To investigate mTORC1 activity suppression and measure autophagic flux.
Nat Commun. 2020 Sep 9;11(1):4510.
Endothelial cells and smooth muscle cells
0.3 to 3000 ng/mL
24 hours, 48 hours, 72 hours
To compare anti-proliferative effects of SRM-NPs and PTX-NPs; SRM proved more effective under hypoxia.
Bioact Mater. 2020 Oct 1;6(3):880-889.
CD8+ T cells
20 nM
36 hours
Transient mTOR inhibition can restore ACD in aged CD8+ T cells, suggesting a potential therapeutic strategy to reinvigorate immune responses in elderly individuals.
Nat Commun. 2021 May 11;12(1):2715.
COS-7 cells
100 nM
50 min
The purpose was to evaluate the effect of rapamycin on mitochondrial deformation, resulting in a ~60% decrease in TMRE signal.
Nat Commun. 2022 Jul 29;13(1):4413.
HeLa
1 µM
80 min
To study the effects of rapamycin on immunostaining in HeLa cells expressing a specific construct.
Cell Res. 2022 Dec;32(12):1086-1104.
SCC-25 cells
200 nM
up to 18 hours
To induce autophagy and assess its effect on FN1 degradation, showing that increased autophagic activity correlates with reduced FN1 levels.
Int J Oral Sci. 2020 Dec 14;12(1):34.
C2C12 cells
100 nM
In the presence of rapamycin, S6 phosphorylation was drastically reduced, both in the presence or absence of TubA.
Nat Commun. 2022 Nov 19;13(1):7108.
MSCs
50 nM
Improved colony-forming capability, proliferation, and osteogenic differentiation of TNFα−/− MSCs
Bone Res. 2021 Jan 1;8(1):44.
HEK293T
333 nM
Disruption of FUS condensates and prevention of new condensate formation.
Nat Commun. 2021 Mar 22;12(1):1809.
Tsc2-deficient cells
20 nM
Had no additional effect on the proliferation of Tsc2-deficient cells, but decreased the expression of Tfeb by about 2-fold.
Nat Commun. 2021 Jul 12;12(1):4245.
Intestinal Intraepithelial Lymphocytes (IEL)
20 nM
To assess the impact of Rapamycin on IEL growth and granzyme B expression.
Nat Commun. 2021 Jul 13;12(1):4290.
MCF10AecoR cells
1 µM
4 hours
To study the effect of mTOR inhibitors on BRAF T401 phosphorylation, results showed rapamycin partially suppressed pT401 levels.
Cell Commun Signal. 2024 Sep 2;22(1):428.
Rapamycin/西罗莫司 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
OTULIN-deficient mouse model
Intraperitoneal injection
1 mg/kg
Twice weekly from postnatal day 8 until 8 weeks of age
To reduce liver pathology caused by OTULIN deficiency; rapamycin treatment reduced histological abnormalities and fibrosis.
Cell Death Differ. 2020 May;27(5):1457-1474
C57BL/6 mice
DMM surgery model for OA
Intra-articular injection
10 µM
Once weekly for 8 weeks
To evaluate the therapeutic effect on OA and reduce cartilage destruction.
J Nanobiotechnology. 2023 Oct 4;21(1):361.
Mice
Pik3c2b KO Mouse Model
Intraperitoneal injection
10 mg/kg
Single treatment before sacrifice
To normalize mTORC1 activity in KO adult brains.
Brain. 2022 Jul 29;145(7):2313-2331
Mice
Telomerase-deficient mice
Intraperitoneal injection
2 mg/kg
2 h post-injection
To test the inhibition of mTORC1 and understand its role in the survival of telomerase-deficient mice.
Nat Commun. 2020 Mar 3;11(1):1168
BALB/c nude mice
HepG2 cells or MHCC97H cells transplantation
Intraperitoneal injection
3 mg/kg
Every other day starting at day 4
Rescues increased cell size and mTORC1 activation induced by TET2 deficiency.
Cell Discov. 2023 Aug 8;9(1):84
NRG mice
Patient-derived xenografts (PDX)
Intraperitoneal injection
4 mg/kg
5 days/week
Combination treatment significantly prolonged survival of mice.
Leukemia. 2021 May;35(5):1267-1278.
Mice
DTG mice
Intraperitoneal injection
4 mg/kg
Daily for 5 consecutive days
Improved symptoms for human patients with extramammary PD.
Cell Res. 2020 Oct;30(10):854-872
SCID/NOD mice
Tumor-bearing mice
Intraperitoneal injection
6 mg/kg
Daily
Combination treatment to enhance efficacy against tumors.
Mol Cancer. 2022 Aug 30;21(1):171
Mice
Pancreatic growth model
Intraperitoneal injection
0.2 mg/(100 g body weight)
Daily injections for 7 days
To study the role of the mTOR signaling pathway in pancreatic growth, results showed that rapamycin inhibited camostat-induced pancreatic growth
J Physiol. 2006 Jun 15;573(Pt 3):775-86
Mice
Col6a1−⁄− mice
Intraperitoneal injection
2 mg/kg body weight
Every 24 h for 14 days
Investigated the effects of rapamycin on col6a1??? mice, finding that rapamycin treatment reduced ER stress, increased autophagy molecular signatures, and improved platelet counts.
Autophagy. 2023 Mar;19(3):984-999
Mice
Diabetic embryopathy model
Intraperitoneal injection
2 mg/kg
Daily from E5.5 to E8.5 or E10.5
Investigate the preventive effect of rapamycin on diabetes-induced neural tube defects
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