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> Rapamycin [53123-88-9]

Rapamycin [53123-88-9]

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Cat# HY-10219-10mg

Size : 10mg

Brand : MedChemExpress


Rapamycine (Sirolimus; AY 22989) est un inhibiteur puissant et spécifique de mTOR avec un IC50 de 0,1 nM dans les cellules HEK293. Rapamycine se lie au FKBP12 et agit spécifiquement comme un inhibiteur allostérique de mTORC1. Rapamycine est un activateur de l'autophagie, un immunosuppresseur.

Rapamycin (Sirolimus; AY 22989) ist ein potenter und spezifischer mTOR-Inhibitor mit einem IC50 von 0,1 nM in HEK293-Zellen. Rapamycin bindet an FKBP12 und wirkt spezifisch als allosterischer Inhibitor von mTORC1. Rapamycin ist ein Autophagie-Aktivator, ein Immunsuppressivum.

Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.

For research use only. We do not sell to patients.

Rapamycin Chemical Structure

Rapamycin Chemical Structure

CAS No. : 53123-88-9

This product is a controlled substance and not for sale in your territory.

Based on 861 publication(s) in Google Scholar

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    Rapamycin purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2023 Jul 5,453,131354.

    Rapamycin (50 nM; 24 h) efficiently inhibits the Cobalt-induced hyperphosphorylation of Tau in Ser262 and Thr181, when in H4 cells.

    Rapamycin purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2023 Jul 5,453,131354.

    Rapamycin (50 nM; 24 h) partially reverses the cobalt-induced increase in LC3B-II and p62 levels in H4 cells.

    Rapamycin purchased from MedChemExpress. Usage Cited in: PLoS Pathog. 2023 Mar 27;19(3):e1011295.  [Abstract]

    Rapamycin (100 nM; 24 h) increases PRRSV replication in Marc-145 cells.

    Rapamycin purchased from MedChemExpress. Usage Cited in: Cancer Cell Int. 2023 Apr 16;23(1):68.  [Abstract]

    Rapamycin (2.5 mM; 24 h) ignificantly reverses the PCK1-sh-induced decreased expression of LC3B-II in SW480-sh cells.

    Rapamycin purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2020 Jun 12;11(6):454.  [Abstract]

    Immunofluorescence staining of p62 is conducted in HSC-T6 cells. G-Rg3 pretreatment with 16 μM and Ra are conducted with 100 or 200 nM.

    Rapamycin purchased from MedChemExpress. Usage Cited in: Nature. 2018 Jun;558(7711):540-546.  [Abstract]

    Western blot and quantification of P-AKT (Ser473) and P-S6RP in the liver, heart and muscle, respectively, of PIK3CAWT and PIK3CACAGG-CreER mice treated with vehicle or Rapamycin directly after Cre induction.

    Rapamycin purchased from MedChemExpress. Usage Cited in: Acta Biomater. 2018 Nov;81:278-292.  [Abstract]

    Evident LC3 turnover and increased level of Atg5 are found upon Rapamycin treatment, which indicate significant autophagy activation.

    Rapamycin purchased from MedChemExpress. Usage Cited in: Int J Cancer. 2018 Aug 15;143(4):931-943.  [Abstract]

    H1975 cells are pretreated with Rapamycin (100 nM) for 1 h and then cells are exposed to IFN-γ (100 U/mL). Phosphorylation of AKT, S6, 4E-BP1 are analyzed by western blotting.

    Rapamycin purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Mar 7;8(1):4108.  [Abstract]

    L02 cells exposed to PA (200 μM) with different concentrations of Rapamycin (Rapa) or Chloroquine (CQ) for 24 h. Palmitate (PA) induced higher protein expression of LC3 II/I and p62 compared with control as indicated by western blot.

    Rapamycin purchased from MedChemExpress. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):144-155.  [Abstract]

    Raw264.7 macrophages treated without or with Rapamycin (1 μΜ) or Chloroquine (20 μΜ) for 48 h. Western blot shows the protein expression levels of Atg5, Beclin1, LC3, and p62/SQSMT1.

    Rapamycin purchased from MedChemExpress. Usage Cited in: Pharmacol Biochem Behav. 2019 Feb;177:1-11.  [Abstract]

    Effect of treatment with Rapamycin, trehalose, or their combination on tyrosine hydroxylase (TH) expression in the striatum in MPTP-induced mouse model of Parkinson’s disease.

    Rapamycin purchased from MedChemExpress. Usage Cited in: Pharmacol Biochem Behav. 2019 Feb;177:1-11.  [Abstract]

    Effect of treatment with Rapamycin, trehalose, or their combination on autophagy activity measured by quantified immunoreactivity of LC3-II in the s. nigra. MPTP is administered at the dose of 20 mg/kg (i.p., daily) for 4 days to induce PD-like pathology.

    Rapamycin purchased from MedChemExpress. Usage Cited in: Biotechnol Appl Biochem. 2018 Sep;65(5):665-671.  [Abstract]

    The mTOR inhibitor Rapamycin augments the autophagy induced by GEM. (A, B) Beclin-1 and LC3B expression is analyzed by western blot after treatment of the cells with GEM (5 μM) and Rapamycin (0, 1, and 2.5 μM) for 48 (A) or 72 (B) h.

    Rapamycin purchased from MedChemExpress. Usage Cited in: PeerJ. 2018 Nov 21;6:e5988.  [Abstract]

    C6/36 cells are treated with 3-MA, Rapa or CQ for 36 h, 6 h and 36 h, respectively and then subjected to MDC staining. Mock and DMSO treated C6/36 cells are used as controls.

    Rapamycin purchased from MedChemExpress. Usage Cited in: PeerJ. 2018 Nov 21;6:e5988.  [Abstract]

    C6/36 cells are treated with 3-MA, Rapa or CQ for 36 h, 6 h and 36 h, respectively. For Rapa plus CQ treatment, C6/36 cells are treated with CQ for 30 h then treated with Rapa for 6 h. Mock and DMSO treated C6/36 cells are used as controls. After the treatment, the levels of AaAtg8-I and AaAtg8-II are analysed by immunoblotting using antibody against AaAtg8.

    Rapamycin purchased from MedChemExpress. Usage Cited in: Int J Ophthalmol. 2018 May 18;11(5):712-718.  [Abstract]

    Western blotting shows that Rapamycin treatment downregulates p-mTOR protein levels in infected and uninfected corneal tissues compared to the vehicle group.

    Rapamycin purchased from MedChemExpress. Usage Cited in: Evid Based Complement Alternat Med. 2018 Jun 26;2018:6049498.  [Abstract]

    Western blot analysis of AKT, p-Akt, mTOR, p-mTOR, FOXO1 and p-FOXO1 expression in U-87 MG cells after treatment with LY294002 (20 μM), Rapamycin (50 nM) or NAC (5 mM) with or without Xihuang pill (XHP).

    Rapamycin purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2018;48(6):2318-2336.  [Abstract]

    Cells are treated with Rapamycin (Rp; 10 μM)+Eicosapentaenoic acid (EPA; 40 μM) with or without Chloroquine (CQ; 5 μM) for 48 h. Cell extracts are prepared and subjected to western blot analysis.

    Rapamycin purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2018;48(6):2318-2336.  [Abstract]

    Cells are pretreated with 5 mM 3-MA or 2 μM for 1 h and then exposed to 40 μM EPA and 10 μM Rp for 48 h. Cell extracts are prepared and subjected to western blot analysis.

    Rapamycin purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 Jun 8;8:15617.  [Abstract]

    Immunoblot analysis of KRAS protein levels in parental (P) and resistant derivatives (R1 and R2) following 4 h treatment with the corresponding inhibitors Rapamycin, AZD2014, MLN0128, BEZ235 and 4EGI-1. Images are cropped for clarity from the same exposure of the same membrane.

    Rapamycin purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2017 Sep 1;127(9):3339-3352.  [Abstract]

    Phosphorylation of SMAD1/5/8 and SMAD2/3 in FOP-iMSCs. Serum-starved FOP-iMSCs are pretreated with 10 nM Rapamycin (Rapa), 1 μM DMH1, or 1 μM SB-431542 for 1 hour.

    Rapamycin purchased from MedChemExpress. Usage Cited in: PLoS One. 2017 Nov 29;12(11):e0188748.  [Abstract]

    FTY720 reverses activation of autophagy induced by mTOR inhibitor, rapamycin. The impact of FTY720 and Rapamycin on the expression of Beclin1 and LC3 is evaluated by western blotting. Results are representative of 4 independent experiments.

    Rapamycin purchased from MedChemExpress. Usage Cited in: PLoS One. 2017 Jun 21;12(6):e0179772.  [Abstract]

    RAW264.7 cells transfected with miR-144-3p control or miR-144-3p mimic in full medium with or without 50μg/mL Rapamycin or 0.1% DMSO. 50 μg of total cell extracts are analyzed by Western blotting with a mouse anti-SQSTM1/p62 antibody. The p62 levels are detected by Western-blot (upper). Quantitative analysis of the p62 band normalized to β-actin is shown (lower).

    Rapamycin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2016 Dec 15;122:42-61.  [Abstract]

    Inhibition of SREBPs processing by AHI is dependent on LKB-1/AMPK/mTOR pathway. (A) HepG2 cells are incubated with or without MHY1485 or Rapamycin for 1 h, the cells are switched to medium D in the presence of vehicle, or AHI. (B) HepG2 cells are incubated with or without Compound C for 1 h, the cells are switched to medium D in the presence of vehicle, or AHI.

    Rapamycin purchased from MedChemExpress. Usage Cited in: Sci Bull. 2015 Dec;60(24):2120-2128.

    CNE-2Z cells are treated with AZD8055 or Rapamycin with or without 1 T SMF for 3 d before they are harvested for Western blot.

    View All mTOR Isoform Specific Products:

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    mTOR mTORC1 mTORC2

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    Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam
    Description

    Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1[1]. Rapamycin is an autophagy activator, an immunosuppressant[2].

    IC50 & Target[1][2]

    mTOR

    0.1 nM (IC50, in HEK293 cells )

    Microbial Metabolite

     

    Autophagy

     

    In Vitro

    Rapamycin (12.5-100 nM; 24 hours) treatment exerts modest inhibitory effect on lung cancer cell proliferation in a dose-dependent manner in all cell lines (A549, SPC-A-1, 95D and NCI-H446 cells) tested, achieving about 30-40% reduction in cell proliferation at 100 nM vs. ~10% reduction at 12.5 nM[3].
    Lung cancer cell line 95D cells are exposed to Rapamycin (10 nM, 20 nM) and RP-56976 (1 nM, 10 nM) alone or in combination (Rapamycin 20 nM+ RP-56976 10 nM). After 24 hours exposure to Rapamycin or RP-56976 alone does not significantly alter the level of expression or phosphorylation of ERK1/2, whereas cells treated with the combination of Rapamycin with RP-56976 exhibit a marked reduction in the phosphorylation levels of ERK1/2[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Rapamycin Related Antibodies

    Cell Viability Assay[3]

    Cell Line: Lung cancer cell lines A549, SPC-A-1, 95D and NCI-H446
    Concentration: 12.5 nM, 25 nM, 50 nM, 100 nM
    Incubation Time: 24 hours
    Result: Treatment exerted modest inhibitory effect on lung cancer cell proliferation in a dose-dependent manner in all cell lines.

    Western Blot Analysis[3]

    Cell Line: 95D cells
    Concentration: 10 nM and 20 nM
    Incubation Time: 24 hours
    Result: Combination treatment with RP-56976 decreased phosphorylation of ERK.
    In Vivo

    Rapamycin (2.0 mg/kg; intraperitoneal injection; every other day; 28 days) alone has a moderate inhibitory effect. However, the combination of Metformin and Rapamycin exerts a significantly increased inhibition of tumor growth compared with the control group, the Rapamycin monotherapy group and the Metformin monotherapy group[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: 24 male nu/nu mice aged 4-5 week old (15-20 g)[4]
    Dosage: 2.0 mg/kg
    Administration: Intraperitoneal injection; every other day; 28 days
    Result: Had a moderate inhibitory effect in monotherapy group. The combination with Metformin exerted a significantly increased inhibition of tumor growth.
    Clinical Trial
    Molecular Weight

    914.17

    Formula

    C51H79NO13
    CAS No.

    53123-88-9
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C([C@@]1(O)[C@@H](CC[C@@H](C[C@@H](/C(C)=C/C=C/C=C/[C@H](C[C@@H](C)C([C@@H]([C@@H](/C(C)=C/[C@H]2C)O)OC)=O)C)OC)O1)C)C(N3CCCC[C@H]3C(O[C@@H](CC2=O)[C@@H](C[C@H]4C[C@H]([C@H](O)CC4)OC)C)=O)=O
    Structure Classification
    • Antibiotics
    • Disease Research
    • Anti-inflammation/Immunoregulatory
    • Antibiotics
    • Macrolide Antibiotics
    Initial Source
    • Microorganisms

    bacterium Streptomyces hygroscopicus
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (136.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 50 mg/mL (54.69 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.0939 mL 5.4694 mL 10.9389 mL
    5 mM 0.2188 mL 1.0939 mL 2.1878 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (2.73 mM); Suspended solution

      This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% EtOH    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (2.73 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

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    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    % 
    +
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.94%

    COA (257 KB) HNMR (241 KB) LCMS (121 KB)

    Handling Instructions (2659 KB)
    References

    • [1]. Edwards SR, et al. The rapamycin-binding domain of the protein kinase mammalian target of rapamycin is a destabilizing domain. J Biol Chem, 2007, 282(18), 13395-13401.  [Content Brief]

      [2]. Rangaraju S, et al. Rapamycin activates autophagy and improves myelination in explant cultures from neuropathicmice. J Neurosci. 2010 Aug 25;30(34):11388-97.  [Content Brief]

      [3]. Niu H, et al. Rapamycin potentiates cytotoxicity by RP-56976 possibly through downregulation of Survivin in lung cancer cells. J Exp Clin Cancer Res. 2011 Mar 10;30:28.  [Content Brief]

      [4]. Zhang JW, et al. Metformin synergizes with rapamycin to inhibit the growth of pancreatic cancer in vitro and in vivo. Oncol Lett. 2018 Feb;15(2):1811-1816.  [Content Brief]

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 1.0939 mL 5.4694 mL 10.9389 mL 27.3472 mL
    5 mM 0.2188 mL 1.0939 mL 2.1878 mL 5.4694 mL
    10 mM 0.1094 mL 0.5469 mL 1.0939 mL 2.7347 mL
    15 mM 0.0729 mL 0.3646 mL 0.7293 mL 1.8231 mL
    20 mM 0.0547 mL 0.2735 mL 0.5469 mL 1.3674 mL
    25 mM 0.0438 mL 0.2188 mL 0.4376 mL 1.0939 mL
    30 mM 0.0365 mL 0.1823 mL 0.3646 mL 0.9116 mL
    40 mM 0.0273 mL 0.1367 mL 0.2735 mL 0.6837 mL
    50 mM 0.0219 mL 0.1094 mL 0.2188 mL 0.5469 mL
    DMSO 60 mM 0.0182 mL 0.0912 mL 0.1823 mL 0.4558 mL
    80 mM 0.0137 mL 0.0684 mL 0.1367 mL 0.3418 mL
    100 mM 0.0109 mL 0.0547 mL 0.1094 mL 0.2735 mL
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    Rapamycin Related Classifications

    Help & FAQs

    Keywords:

    Rapamycin53123-88-9Sirolimus AY-22989AY22989AY 22989AY-22989mTORFKBPFungalAutophagyEndogenous MetaboliteAntibioticBacterialMammalian target of RapamycinFK506-binding proteinHEK293FKBP12mTORC1autophagyimmunosuppressantInhibitorinhibitorinhibit

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