1. PI3K/Akt/mTOR
    Autophagy
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    Immunology/Inflammation
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  2. mTOR
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    Fungal
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    Endogenous Metabolite
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  3. Rapamycin

Rapamycin (Synonyms: Sirolimus; AY-22989)

目录号: HY-10219 纯度: 99.94%
产品使用指南

Rapamycin (Sirolimus) 是一种有效且特异性的 mTOR 抑制剂,作用于 HEK293 细胞,抑制 mTORIC50 为 0.1 nM。Rapamycin 与 FKBP12 结合且抑制 mTORC1。Rapamycin 还是一种自噬 (autophagy) 激活剂,免疫抑制剂。

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Rapamycin Chemical Structure

Rapamycin Chemical Structure

CAS No. : 53123-88-9

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Customer Review

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的科研文献

    Rapamycin purchased from MCE. 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.

    Rapamycin purchased from MCE. Usage Cited in: Biochem Pharmacol. 2016 Dec 15;122:42-61.

    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 MCE. Usage Cited in: PLoS One. 2017 Jun 21;12(6):e0179772.

    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 MCE. Usage Cited in: Nat Commun. 2017 Jun 8;8:15617.

    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 MCE. Usage Cited in: J Clin Invest. 2017 Sep 1;127(9):3339-3352.

    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 MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2018 Feb 1;50(2):144-155.

    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 MCE. Usage Cited in: Sci Rep. 2018 Mar 7;8(1):4108.

    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 MCE. Usage Cited in: Cell Physiol Biochem. 2018;48(6):2318-2336.

    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 MCE. Usage Cited in: Cell Physiol Biochem. 2018;48(6):2318-2336.

    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 MCE. Usage Cited in: PLoS One. 2017 Nov 29;12(11):e0188748.

    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 MCE. Usage Cited in: Int J Cancer. 2018 Aug 15;143(4):931-943.

    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 MCE. Usage Cited in: Biotechnol Appl Biochem. 2018 Sep;65(5):665-671.

    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 MCE. Usage Cited in: Evid Based Complement Alternat Med. 2018 Jun 26;2018:6049498.

    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 MCE. Usage Cited in: Int J Ophthalmol. 2018 May 18;11(5):712-718.

    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 MCE. Usage Cited in: Nature. 2018 Jun;558(7711):540-546.

    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 MCE. Usage Cited in: Acta Biomater. 2018 Nov;81:278-292.

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

    Rapamycin purchased from MCE. Usage Cited in: PeerJ. 2018 Nov 21;6:e5988.

    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 MCE. Usage Cited in: PeerJ. 2018 Nov 21;6:e5988.

    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 MCE. Usage Cited in: Pharmacol Biochem Behav. 2019 Feb;177:1-11.

    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 MCE. Usage Cited in: Pharmacol Biochem Behav. 2019 Feb;177:1-11.

    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 MCE. Usage Cited in: Cell Death Dis. 2020 Jun 12;11(6):454.

    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.

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    • 参考文献

    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

    mTOR

    0.1 nM (IC50, in HEK293 cells )

    Human Endogenous 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].

    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].

    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

    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

    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)

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

    H2O : < 0.1 mg/mL (insoluble)

    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
    10 mM 0.1094 mL 0.5469 mL 1.0939 mL
    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。 -80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

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

      此方案可获得 ≥ 2.5 mg/mL (2.73 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
    • 2.

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

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

      此方案可获得 2.5 mg/mL (2.73 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

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

      此方案可获得 ≥ 2.5 mg/mL (2.73 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    • 4.

      请依序添加每种溶剂: 10% EtOH    40% PEG300    5% Tween-80    45% saline

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

      此方案可获得 ≥ 2.5 mg/mL (2.73 mM,饱和度未知) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
    • 5.

      请依序添加每种溶剂: 10% EtOH    90% (20% SBE-β-CD in saline)

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

      此方案可获得 2.5 mg/mL (2.73 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 6.

      请依序添加每种溶剂: 10% EtOH    90% corn oil

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

      此方案可获得 ≥ 2.5 mg/mL (2.73 mM,饱和度未知) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 MCE 网站选购。
    References

    Purity: 99.94%

    • 摩尔计算器

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    C1   V1   C2   V2

    Keywords:

    RapamycinSirolimusAY-22989AY22989AY 22989mTORFKBPFungalAutophagyEndogenous MetaboliteAntibioticMammalian target of RapamycinFK506-binding proteinHEK293FKBP12mTORC1autophagyimmunosuppressantInhibitorinhibitorinhibit

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    产品名称:
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