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mTOR inhibiteurs/activateurs (mTOR Inhibitors/Activators)

Mammalian target of rapamycin (mTOR), also known as FKBP12-rapamycin-associated protein (FRAP), is a 280 kDa serine/threonine kinase which plays a key role in regulating critical cellular processes such as growth, proliferation, cytoskeletal organization, transcription, protein synthesis and ribosomal biogenesis by integrating three major inputs-nutrients (amino acids), growth factors (insulin), and cellular energy status.  [show the full text]

Autre PI3K/Akt/mTOR Inhibiteurs

PI3K Akt GSK-3 DNA-PK ATM/ATR PDK AMPK PTEN MELK PI4K

Produits sélectifs disoformes

N° de cat. Nom du produit Informations Citations dutilisation du produit Validations de produit
S1039 Rapamycin (Sirolimus) Rapamycin은 HEK293 세포에서 IC50가 약 0.1 nM인 특이적 mTOR 억제제입니다. 이 화합물은 FKBP12에 결합하여 mTORC1의 알로스테릭 억제제로 특이적으로 작용합니다. 이는 Autophagy 활성제이자 면역억제제입니다.
Nature, 2025, 10.1038/s41586-025-09018-7
Signal Transduct Target Ther, 2025, 10(1):271
Cell Metab, 2025, S1550-4131(25)00294-3
Verified customer review of Rapamycin (Sirolimus)
S1120 RAD001 (Everolimus) 에베로리무스는 무세포 분석에서 IC50 1.6-2.4 nM의 FKBP12 mTOR 억제제입니다. 에베로리무스는 세포 apoptosis 및 autophagy를 유도하고 종양 세포 증식을 억제합니다.
Cancer Cell, 2025, 43(4):776-796.e14
Nat Commun, 2025, 16(1):8189
Cell Rep Med, 2025, 6(11):102425
Verified customer review of RAD001 (Everolimus)
S2827 Torin 1 Torin 1은 무세포 분석에서 IC50이 2 nM/10 nM인 강력한 mTORC1/2 억제제이며, PI3K보다 mTOR에 대해 1000배 선택성을 보입니다.
Cell Mol Immunol, 2025, NONE
Nat Struct Mol Biol, 2025, 10.1038/s41594-025-01581-x
Nat Commun, 2025, 16(1):3292
Verified customer review of Torin 1
S2817 Torin 2 Torin 2는 p53 / - MEF 세포주에서 IC50 0.25nM의 강력하고 선택적인 mTOR 억제제이며, PI3K보다 800배 높은 mTOR 선택성과 개선된 약동학적 특성을 가집니다. 이 화합물은 PC3 세포주에서 각각 EC50 28nM/35nM/118nM으로 ATM/ATR/DNA-PK를 억제합니다. 세포 생존력을 감소시키고 Autophagy와 Apoptosis를 유도합니다.
J Med Virol, 2025, 97(8):e70534
J Gen Virol, 2025, 106(3)002086
bioRxiv, 2025, 2025.09.24.678136
Verified customer review of Torin 2
S2638 NU7441 (KU-57788) NU7441 (KU-57788)은 IC50 14 nM의 매우 강력하고 선택적인 DNA-PK 억제제입니다. 또한 무세포 분석에서 IC50 1.7 μM 및 5 μM로 mTOR 및 PI3K를 억제하고, Cas9 매개 DNA 절단 후 NHEJ 빈도를 줄이는 동시에 HDR 속도를 증가시킵니다.
Nat Cell Biol, 2025, 27(1):59-72
Trends Biotechnol, 2025, S0167-7799(25)00314-2
Nat Commun, 2025, 16(1):997
Verified customer review of NU7441 (KU-57788)
S9736 ME-344 ME-344는 NV-128의 합성 대사산물로, 미토콘드리아 산화적 인산화(OXPHOS) 복합체 I의 강력한 억제제이며, ATP 생성 및 산소 소비를 방해합니다. 또한 AKT/mTOR 경로를 하향 조절하여 mTOR를 억제하고, IC50 값이 70–260 nM인 백혈병 세포주에서 세포 성장 및 생존력을 억제함으로써 항암 활성을 나타냅니다.
S8163 Paxalisib (GDC-0084) Paxalisib (GDC-0084, RG7666)는 PI3K 및 mTOR의 뇌 침투 억제제로, PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ 및 mTOR에 대한 Kiapp 값은 각각 2 nM, 46 nM, 3 nM, 10 nM 및 70 nM입니다.
Cell Death Dis, 2025, 16(1):210
Cell Death Discov, 2023, 9(1):172
Mol Cancer Res, 2022, 20(6):996-1008
S1555 AZD8055 AZD8055는 MDA-MB-468 세포에서 PI3K 동형 및 ATM/DNA-PK에 대해 우수한 선택성(약 1,000배)을 가진 IC50 0.8 nM의 새로운 ATP 경쟁적 mTOR 억제제입니다. 이 화합물은 카스파제 의존성 아폽토시스를 유도하고 자가포식도 유도합니다. 1단계.
Signal Transduct Target Ther, 2025, 10(1):92
Plant Commun, 2025, 6(7):101389
J Cereb Blood Flow Metab, 2025, 0271678X251321641
Verified customer review of AZD8055
S1022 Ridaforolimus (Deforolimus, MK-8669) Ridaforolimus (Deforolimus, MK-8669, AP23573)는 HT-1080 세포주에서 IC50이 0.2 nM인 선택적 mTOR 억제제입니다. 프로드럭으로 분류되지는 않지만, mTOR 억제 및 FKBP12 결합은 라파마이신과 유사합니다. 3상 연구 중.
JCI Insight, 2025, e186456
Front Oncol, 2025, 15:1486671
Nat Commun, 2024, 15(1):3636
Verified customer review of Ridaforolimus (Deforolimus, MK-8669)
S2811 Sapanisertib (MLN0128, INK-128) Sapanisertib (MLN0128, INK 128, TAK-228)는 세포 자유 분석에서 IC50이 1 nM인 강력하고 선택적인 mTOR 억제제입니다. 클래스 I PI3K 동형에 대해 200배 이상 덜 강력하며, mTORC1/2 차단에 우수하고 전이 촉진 유전자(라파마이신 대비)에 민감합니다. 1상.
Mol Oncol, 2025, 19(1):151-172
Sci Adv, 2025, 11(6):eadq3802
Nat Aging, 2025, 5(7):1340-1357
Verified customer review of Sapanisertib (MLN0128, INK-128)

Mammalian target of Rapamycin (mTOR), also known as FKBP12-rapamycin-associated protein (FRAP), is a 280 kDa serine/threonine kinase [1-3]. mTOR kinase activity could be promoted by various extra- and intracellular stimulus like trophic factors, mitogens, hormones, amino acids and cellular stress [4-8]. In response to increased availability of stimuli, mTOR modulates numerous of important cellular processes, e.g. protein translation and autophagy, by phosphorylating its downstream molecules [9]. mTOR is the nuclear catalytic subunit of two complexes: mTORC1 and mTORC2 [1]. mTORC1 is comprised of mTOR, Raptor, mLST8, and PRAS40 (a mTOR inhibitor). This complex presented classic features of mTOR as a nutrient or energy sensor and protein synthesis conditioner [5, 10]. Low level of nutrient levels, growth factor and cellular stress inhibits the activity of mTORC1 [9, 10]. p70-S6 Kinase 1 (S6K1) and the eukaryotic initiation factor 4E (eIF4E) binding protein 1 (4E-BP1) are the best investigated targets of mTORC1 [5]. The activated mTORC1 showed a negative feedback inhibition on PI3K signaling [11]. mTORC1 could be specifically suppressed by rapamycin, as well as its allosteric ramifications. mTORC2 contains mTOR, Rictor, mLST8, and mSIN1 [12, 13]. Different from mTORC1, activated mTORC2 could induce the phosphorylation of Akt at serine 473  and serving as a positive feedback on PI3K signaling cascade [14]. Although mTORC2 was identified as a rapamycin-insensitive complex previously [14], an inhibition effect of rapamycin on free mTOR was observed in some cell lines [15]. Recent studies revealed that disordered activity of mTOR is related to some malignant and resistant cancer. The specific inhibitors, such as rapamycin and Temsirolimus(CCI-779), have been developed and trialed as novel anti-cancer agents [16, 17].