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Catalog No.
Product Name
Application
Product Information
Citations
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dual pan-PI3K/mTOR inhibitor
PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/34/16/1 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ and 4.7 nM for mTOR. Antitumor activity. -
mTOR inhibitor
mTOR inhibitor-1 is a novel mTOR pathway inhibitor which can suppress cells proliferation and inducing autophagy. -
PI3K/mTOR inhibitor
PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual PI3K/mTOR inhibitor with IC50s of 20/376/204/46 nM and 186 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ and mTOR, respectively. Antitumor activity. -
mTOR inhibitor
42-(2-Tetrazolyl)rapamycin is a prodrug compound of a rapamycin analog extracted from patent US 20080171763 A1, Example 1. Rapamycin is a specific mTOR inhibitor. -
PI3K/Akt/mTOR inhibitor
PI3K/Akt/mTOR-IN-2 is an inhibitor of the PI3K/AKT/mTOR signaling pathway with demonstrated anticancer activity. It selectively inhibits the proliferation of MDA-MB-231 cells with an IC50 of 2.29 μM and induces cell cycle arrest and apoptosis, making it a promising candidate for cancer research. -
Hsp90/HSV inhibitor
AT-533 is a potent inhibitor of heat shock protein 90 (Hsp90) and herpes simplex virus (HSV), exhibiting strong antitumor and antiviral activities. It suppresses tumor growth and angiogenesis by disrupting the HIF-1α/VEGF/VEGFR-2 signaling axis, a critical pathway in tumor vascularization and progression. Additionally, AT-533 inhibits key downstream signaling cascades, including Akt/mTOR/p70S6K, ERK1/2, and FAK pathways. In endothelial cells, specifically human umbilical vein endothelial cells (HUVECs), AT-533 effectively inhibits tube formation, cell migration, and invasion, highlighting its anti-angiogenic properties. These combined effects position AT-533 as a promising candidate for cancer therapy and angiogenesis-related disease research. -
PI3K/Akt/mTOR Inhibitor
Veratramine is a selective inhibitor of the PI3K/Akt/mTOR signaling pathway and serves as a modulator of SIGMAR1. This compound facilitates autophagic apoptosis in tumor cells, effectively induces G0/G1 cell cycle arrest, and diminishes epithelial-mesenchymal transition (EMT) markers, thereby reducing tumor migration. Additionally, Veratramine exhibits neuroprotective effects by inhibiting SIGMAR1 interactions with NMDAR and the phosphorylation of NMDAR Ser896, resulting in reduced neurological damage in neuropathy models. Its diverse biological activities make it suitable for research on liver cancer, osteosarcoma, and diabetic peripheral neuropathy. -
mTORC1 Inhibitor
RMC-4745 is a selective dual-site inhibitor of mTORC1 with a 35-fold higher affinity for mTORC1 compared to mTORC2. It effectively inhibits the proliferation of MCF-7 breast cancer cells and induces apoptosis by upregulating Caspase-3/7 activity. Notably, RMC-4745 does not lead to the upregulation of HER3 due to its selective inhibition of mTORC2. This compound is valuable for research focused on breast cancer and the mechanisms underlying mTOR signaling. -
mTOR Inhibitor
Ovalitenone is a flavonoid compound known to inhibit the mTOR signaling pathway. This compound demonstrates significant anti-cancer activity, as it effectively reduces anchorage-independent growth and suppresses the migration and invasion of cancer cells without inducing cytotoxicity in lung cancer cell lines H460 and A549. Ovalitenone modulates epithelial-mesenchymal transition (EMT) by decreasing N-cadherin, snail, and slug levels while promoting E-cadherin expression. Additionally, it inhibits signaling pathways associated with focal adhesion kinase (FAK), ATP-dependent tyrosine kinase (AKT), and cell division cycle 42 (Cdc42), making it a valuable reagent for cancer research applications. -
PI3K/AKT/mTOR Inhibitor
PI3K/Akt/mTOR-IN-3 is a potent inhibitor targeting the PI3K/AKT/mTOR signaling pathway. It demonstrates significant biological activity, exhibiting IC50 values of 0.77 μM, 1.23 μM, and 4.57 μM in MCF-7, HeLa, and HepG2 cells, respectively. Additionally, this compound effectively inhibits the migration of MCF-7 and HeLa cells at a concentration of 4 μM, while also inducing apoptosis and causing cell cycle arrest in the S phase. This makes PI3K/Akt/mTOR-IN-3 a valuable tool for research in cancer biology and therapeutic development. -
mTOR/PI3/AKT Inhibitor
Royleanone, a diterpenoid isolated from plants, inhibits the proliferation of cancer cells by inducing cell cycle arrest and mitochondria-mediated apoptosis, also inhibits cell migration potential, inhibits mTOR/PI3/AKT signaling pathway in LNCaP prostate cancer cells. -
PI3K/Akt/mTOR Inhibitor、MAPK Inhibitor、NF-κB Inhibitor
Calebin A is a potent inhibitor of the PI3K/Akt/mTOR pathway, as well as MAPK and NF-κB signaling pathways. It exhibits significant anti-tumor activity through epigenetic regulation and can suppress apoptosis while inhibiting autophagy. Additionally, Calebin A modulates adipogenesis, enhances thermogenic processes, and supports gut microbiota. This compound is suitable for research in various domains, including osteoarthritis, Alzheimer's disease, type 2 diabetes, malignant peripheral nerve sheath tumors, and colorectal cancer. -
AKT/mTOR/p70S6K Inhibitor
22-(4′-py)-JA is a semisynthetic derivative of junamycin A, primarily targeting the AKT/mTOR/p70S6K signaling pathway. This compound exhibits significant antimetastatic activity by inhibiting tumor cell invasion and tube formation in human umbilical vein endothelial cells (HUVEC). Furthermore, 22-(4′-py)-JA downregulates key factors including metalloproteinases (MMP-2 and MMP-9), hypoxia-inducible factor 1α (HIF-1α), and vascular endothelial growth factor (VEGF). Its potent anticancer properties make it a valuable tool for research, particularly in non-small cell lung cancer (NSCLC) studies. -
Dual PI3K/mTOR Inhibitor
DHW-221 is a potent dual inhibitor of PI3K and mTOR, demonstrating low nanomolar potency across all four Class I PI3K isoforms (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM) and mTOR (IC50 = 3.9 nM). This compound exhibits significant antitumor activity by disrupting the PI3K/Akt/mTOR signaling pathway, promoting mitochondrial apoptosis and paraptosis via endoplasmic reticulum stress and MAPK signaling, while also hindering cell cycle progression, migration, invasion, and angiogenesis. DHW-221 serves as a valuable tool in research related to non-small cell lung cancer (NSCLC), colon cancer, and breast cancer. -
PIM/PI3K/AKT/mTOR Inhibitor
IBL-302 is an orally available dual inhibitor targeting PIM and the PI3K/AKT/mTOR pathways. It exhibits significant antitumor activity against breast cancer and neuroblastoma, showing in vivo efficacy in nude mouse xenograft models by overcoming trastuzumab resistance. Additionally, IBL-302 enhances the cytotoxic effects of commonly used chemotherapeutic agents, including cisplatin, doxorubicin, and etoposide, making it a valuable compound for cancer research applications. -
Akt/mTOR Inhibitor
MKC-1 is an orally active and potent inhibitor targeting the Akt/mTOR signaling pathway. This compound exhibits broad antitumor activity by arresting cellular mitosis and inducing apoptosis. MKC-1 interacts with various cellular proteins, including tubulin and members of the importin β family, making it valuable for research in cancer cell cycle regulation and therapeutic mechanisms. -
AKT/mTOR Inhibitor
Dehydrovomifoliol is a dual inhibitor of the AKT/mTOR signaling pathway. It effectively reduces lipid accumulation and lipogenesis, making it a valuable reagent in the study of nonalcoholic fatty liver disease (NAFLD). The compound's targeted inhibition of AKT and mTOR provides insights into metabolic regulation and potential therapeutic strategies for liver-related disorders. -
PI3K/Akt/mTOR signaling pathway Inhibitor, TLR4 signaling Inhibitor
25(R,S)-Ruscogenin is a potent inhibitor of the PI3K/Akt/mTOR and TLR4 signaling pathways. This compound effectively suppresses hepatocellular carcinoma (HCC) metastasis by decreasing the expression of matrix metalloproteinases (MMP-2 and MMP-9), uPA, VEGF, and HIF-1α. Additionally, 25(R,S)-Ruscogenin mitigates LPS-induced apoptosis in pulmonary endothelial cells, highlighting its potential for applications in cancer research and inflammatory disease studies. -
PI3K/AKT/mTOR Inhibitor
Notoginsenoside Ft1 is a potent PI3K/AKT/mTOR inhibitor with significant bioactive properties. This compound induces apoptosis and lysosomal cell death in various cancer cell types by modulating key signaling pathways, such as p38 MAPK and ERK1/2, while promoting angiogenesis. Additionally, Notoginsenoside Ft1 enhances CD8+ T cell populations and exerts vasodilatory effects through glucocorticoid and estrogen receptor beta activation in endothelial cells. By acting as a TGR5 agonist and FXR antagonist, it may provide protective effects against renal injury and contribute to the management of obesity and insulin resistance through the modulation of intracellular calcium and cAMP levels. -
mTOR/HDAC Inhibitor
mTOR/HDAC-IN-1 is a dual inhibitor targeting mTOR and HDAC, exhibiting IC50 values of 0.49 nM and 0.91 nM for mTOR and HDAC1, respectively. This compound demonstrates significant anti-cancer activity, making it a valuable tool for research in cancer therapeutics and signaling pathways. Its selective inhibition profile offers potential for elucidating the roles of mTOR and HDAC in tumorigenesis and for developing novel cancer treatment strategies. -
mTORC1/2 Inhibitor
(+)–Usnic acid is a potent mTORC1/2 inhibitor derived from lichens, acting by binding to the ATP-binding pocket of mTOR. It effectively inhibits the phosphorylation of downstream effectors such as Akt (Ser473), 4EBP1, and S6K, thereby promoting autophagy and exhibiting both anti-cancer and anti-inflammatory properties. Additionally, (+)-Usnic acid demonstrates antimicrobial activity against several planktonic gram-positive bacteria, including Staphylococcus aureus, Enterococcus faecalis, and Enterococcus faecium, making it a valuable tool for various biological research applications. -
mTOR Inhibitor
2,6-Dihydroxyacetophenone primarily functions as an mTOR inhibitor. This polyphenolic derivative exhibits significant antioxidant activity and effectively inhibits cell growth and proliferation in colorectal cancer (CRC) cells by inducing apoptosis and arresting the cell cycle at the G0/G1 phase, while also suppressing cell migration. Additionally, 2,6-Dihydroxyacetophenone inhibits xanthine oxidase with an IC50 of 1.24 mM and enhances uric acid metabolism in hyperuricemic models. It further reduces plasma cholesterol levels in hypercholesterolemic rats and mitigates lipid accumulation in mice subjected to a high-fat diet. This compound is valuable for research into CRC, hyperuricemia, and hypercholesterolemia. -
PI3K/mTOR Inhibitor
FD274 is a potent dual inhibitor of PI3K and mTOR, exhibiting IC50 values of 0.65 nM for PI3Kα, 1.57 nM for PI3Kβ, 0.65 nM for PI3Kγ, 0.42 nM for PI3Kδ, and 2.03 nM for mTOR. This compound demonstrates significant anti-proliferative effects on acute myeloid leukemia (AML) cell lines, specifically HL-60 and MOLM-16, inducing G1 phase cell cycle arrest and promoting apoptosis. In vivo studies reveal dose-dependent inhibition of tumor growth in HL-60 xenograft models, making FD274 a valuable tool for research into acute myeloid leukemia therapies. -
PI3Kα/mTOR Inhibitor
PWT-33597 free base is a dual inhibitor targeting PI3Kα and mTOR, effectively disrupting downstream signaling pathways associated with cell growth and metabolism. This compound induces apoptosis in tumor cells and demonstrates significant inhibitory effects on tumor proliferation. PWT-33597 free base is applicable in research focused on various tumors, including renal cell carcinoma, making it a valuable tool for cancer studies. -
HSP90/mTOR Inhibitor
HSP90/mTOR-IN-1 is a potent inhibitor targeting both Hsp90 and mTOR, exhibiting IC50 values of 69 nM and 29 nM, respectively. This compound effectively suppresses the proliferation of SW780 cells by over-activating the PI3K/AKT/mTOR signaling pathway. In addition to inducing apoptosis and autophagy through selective inhibition, HSP90/mTOR-IN-1 demonstrates significant in vivo anti-tumor activity. It serves as a valuable reagent for research applications focused on bladder cancer. -
PI3Kα/mTOR Inhibitor
PWT-33597 is a potent dual inhibitor of PI3Kα and mTOR, effectively disrupting downstream signaling pathways associated with cell growth and survival. This reagent induces apoptosis in tumor cells and demonstrates significant anti-tumor activity. PWT-33597 is a valuable tool for research into various malignancies, including renal cell carcinoma, providing insights into tumor biology and therapeutic strategies. -
mTOR Inhibitor
MT-44 is a potent and selective inhibitor of the mechanistic target of rapamycin (mTOR), exhibiting an IC50 of 49.4 nM. It effectively inhibits cancer cell proliferation, migration, and invasion, while inducing apoptosis and increasing reactive oxygen species (ROS) production. MT-44 also causes G2/M phase cell cycle arrest and activates the cGAS/STING signaling pathway. This compound is valuable for cancer research, particularly in the study of triple-negative breast cancer. -
mTOR/HDAC6 Inhibitor
mTOR/HDAC6-IN-1 is a potent dual inhibitor targeting mTOR and HDAC6, exhibiting IC50 values of 133.7 nM and 56 nM, respectively. This compound is known to induce significant autophagy and apoptosis while suppressing cell migration. It holds potential for research applications in triple-negative breast cancer (TNBC) studies, offering insights into the interplay between these critical pathways in cancer progression. -
mTOR/TEX264 Inhibitor
SI-W052 is a selective small-molecule inhibitor targeting mTOR and TEX264, with oral bioavailability and brain penetrance. It activates autophagy by inhibiting mTOR phosphorylation, while enhancing TEX264 expression to promote endoplasmic reticulum turnover. Additionally, SI-W052 suppresses LPS-induced release of inflammatory factors such as TNF-α and IL-6, making it a promising candidate for research into neuroinflammation associated with Alzheimer’s disease. -
Tyrosinase Inhibitor; Melanosome Inhibitor; mTORC1 Signaling Inhibitor
Decanoic acid is a tyrosinase inhibitor that also targets melanosomes and mTORC1 signaling pathways. It effectively reduces tyrosinase activity and inhibits melanosome maturation, while also suppressing c-Met phosphorylation and inducing apoptosis in hepatocellular carcinoma cells. This compound's ability to influence oncogenic protein expression makes it a valuable tool for research in melanoma, hepatocellular carcinoma, and epilepsy. Additionally, its brain-penetrant properties and non-competitive inhibition of AMPA receptors highlight its potential in neurological studies. -
PI3k/Akt/mTOR Inhibitor
D-87503 is a potent inhibitor of the PI3K/Akt/mTOR signaling pathway, exhibiting IC50 values of 62 nM for PI3K and 0.76 μM for Erk2. This compound effectively attenuates the activity of downstream substrates, including Akt and Rsk1, making it a valuable tool for studying cellular processes regulated by this pathway. D-87503 has applications in cancer research and investigates the role of PI3K signaling in various physiological conditions. -
AKT/mTOR Inhibitor
19-epi-Scholaricine is a potent AKT/mTOR inhibitor, classified as an orally active indole alkaloid. This compound downregulates profibrotic and apoptotic proteins, such as HRAS, HSP90AA1, and KDR, while upregulating the cell cycle regulator CDK2. Furthermore, 19-epi-Scholaricine inhibits ROS production and reduces inflammatory mediator release, leading to decreased podocyte apoptosis, renal inflammation, and oxidative stress. It is a valuable tool for research into chronic glomerulonephritis and membranous nephropathy. -
mTOR Inhibitor
Rapamycin-d3 is a deuterium-labeled analog of Rapamycin, a highly potent and selective inhibitor of the mechanistic target of rapamycin (mTOR), exhibiting an IC50 of 0.1 nM in HEK293 cells. It functions by binding to FKBP12, leading to allosteric inhibition of mTORC1. This compound is notable for its roles in autophagy activation and immunosuppression, making it valuable for various research applications including cancer biology, metabolic disorders, and studies of cellular growth and proliferation. -
PI3K/mTOR Inhibitor
Dactolisib hydrochloride is a potent dual inhibitor of class I phosphoinositide 3-kinases (PI3K) and the mammalian target of rapamycin (mTOR), specifically targeting p110α, p110γ, p110δ, and p110β with IC50 values of 4 nM, 5 nM, 7 nM, 75 nM, and 20.7 nM, respectively. This compound effectively inhibits both mTORC1 and mTORC2, making it a valuable tool for studying the PI3K/mTOR signaling pathway. Its applications include cancer research, drug development, and exploring therapeutic strategies for various diseases associated with dysregulated PI3K/mTOR signaling. -
mTOR Inhibitor
CC214-2 is a selective mTOR kinase inhibitor that targets both mTORC1 and mTORC2 pathways, affecting pS6 and pAktS473 signaling. This compound induces autophagy, making it a promising candidate for host-directed therapy in tuberculosis, demonstrating synergistic bactericidal effects that can shorten treatment duration. Additionally, CC214-2 has shown efficacy in inhibiting Rapamycin-resistant signaling and suppressing glioblastoma growth in vitro and in vivo, positioning it as a valuable tool in cancer research and infectious disease studies. -
mTOR Inhibitor
T133 is a potent ATP-competitive inhibitor of the mechanistic target of rapamycin (mTOR) with an IC50 of 0.34 nM and a Ki of 0.17 nM. It effectively suppresses the phosphorylation of downstream targets, including AKT, S6K1, and 4EBP1, leading to the inhibition of cancer cell proliferation and migration, induction of apoptosis, cell cycle arrest, and promotion of autophagy. T133 demonstrates significant antitumor efficacy in xenograft mouse models and serves as a valuable tool in cancer research, particularly for studies involving gastric and lung cancers. -
AMPK Activator/mTOR Inhibitor
OSU-53 is an orally active AMPK activator and a direct mTOR inhibitor, exhibiting an EC50 of 0.3 μM. This compound induces autophagy by facilitating the conversion of LC3 I to LC3 II and plays a crucial role in modulating energy homeostasis by downregulating fatty acid biosynthesis while enhancing oxidative metabolism through upregulation of PGC1α and NRF-1. OSU-53 demonstrates antitumor activity across various cancer models, including breast and thyroid cancers, making it a valuable tool for cancer research and metabolic studies. -
mTOR Inhibitor
4-FPBUA is a semisynthetic analog of usnic acid that functions as an inhibitor of mTOR. It enhances cellular autophagy and supports blood-brain barrier (BBB) integrity, facilitating the transport of Amyloid β (Aβ) across monolayer cell systems. This compound is of particular interest in Alzheimer's disease research due to its potential to reverse BBB disruption and promote neuroprotection. -
mTOR Inhibitor
3HOI-BA-01 is a potent mTOR inhibitor that plays a critical role in modulating cellular processes. It has been shown to reduce infarct size and induce autophagy in murine models of myocardial ischemia/reperfusion injury. This compound is valuable for research applications focused on cardiac health, autophagy pathways, and cellular stress responses. -
mTORC1 Inhibitor
ICSN3250 hydrochloride is a potent mTORC1 inhibitor that acts by binding to the FRB domain of mTOR, effectively displacing phosphatidic acid and reversing mTORC1 activation. This compound exhibits significant cytotoxicity in cancer cells at nanomolar concentrations via a caspase-independent cell death mechanism. By selectively inhibiting the mTORC1 pathway, ICSN3250 hydrochloride promotes autophagy and induces G0-G1 cell cycle arrest in cancer cells, making it a valuable tool for cancer research. -
mTORC1 Inhibitor
ICSN3250 is a selective mTORC1 inhibitor that operates by directly binding to the FRB domain of mTOR, effectively displacing phosphatidic acid and reversing mTORC1 activation. This compound demonstrates significant cytotoxicity in cancer cells at nanomolar concentrations via a caspase-independent cell death mechanism. Additionally, ICSN3250 specifically inhibits the mTORC1 pathway, promoting autophagy and inducing G0-G1 cell-cycle arrest. It is suitable for research applications focused on cancer biology and therapeutic exploration. -
mTOR Inhibitor
RapaLink-1 is a third-generation bivalent inhibitor targeting the mechanistic target of rapamycin (mTOR). By combining Rapamycin with MLN0128 through an inert linker, RapaLink-1 demonstrates superior efficacy in inhibiting both wild-type and mutant forms of mTOR compared to other inhibitors. This compound effectively crosses the blood-brain barrier, promoting durable mTORC1 inhibition via FKBP12 binding. Additionally, RapaLink-1 exhibits anticancer properties and may play an antithrombotic role in antiphospholipid syndrome by enhancing autophagy. -
mTOR Inhibitor/Autophagy Inducer
mTOR inhibitor-8 is a potent inhibitor of the mechanistic target of rapamycin (mTOR), functioning through the interaction with FKBP12. This compound effectively suppresses mTOR activity and induces autophagy in A549 human lung cancer cells. It is a valuable tool for studying mTOR signaling pathways and the role of autophagy in cancer research. -
mTOR/p70s6K Inhibitor
Zederone is a sesquiterpene that acts as an inhibitor of the mTOR/p70S6K signaling pathway. It effectively reduces ovarian cancer cell proliferation and exhibits selective inhibition of various CYP450 enzymes, notably with IC50 values of 2.9 μM for CYP2B6 and 9.2 μM for CYP2C9. Additionally, Zederone demonstrates antibacterial properties against multi-drug resistant strains of Staphylococcus aureus and has been shown to improve cognitive function while modulating gut bacterial dysbiosis. However, caution is warranted due to its hepatotoxicity, evidenced by an LD50 of approximately 223 mg/kg in mice. -
DNA-PK/mTOR Inhibitor
CC-115 hydrochloride is a potent dual inhibitor of DNA-PK and mTOR, exhibiting IC50 values of 13 nM and 21 nM, respectively. It effectively disrupts signaling pathways associated with both mTORC1 and mTORC2. This compound is valuable for research focused on cancer therapeutics and the modulation of DNA damage response mechanisms.
