Catalog No.
Product Name
Application
Product Information
Citations
-
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 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. -
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/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. -
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. -
mTOR Inhibitor/AMPK Activator
AMPK/mTOR modulator-1 is a Ginsenoside derivative functioning as both an mTOR inhibitor and AMPK activator. It activates AMPK signaling with a Kd of 4.759 μM, promoting M1-like tumor-associated macrophage polarization while inhibiting M2-like polarization. This compound enhances glycolysis and demonstrates significant anti-inflammatory activity alongside inhibition of tumor progression. AMPK/mTOR modulator-1 is ideal for research focused on colorectal cancer and related metabolic disorders. -
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. -
mTOR Inhibitor
Aschantin is a bisepoxylignan that acts as a potent mTOR kinase inhibitor. This compound demonstrates significant biological activities, including antiplasmodial effects, calcium channel antagonism, and the inhibition of platelet activating factor. Additionally, Aschantin serves as an inhibitor of Cytochrome P450 and UGT enzymes, making it a valuable tool for chemoprevention research and various biochemical studies. -
mTORC1 Inhibitor
Sulindac sulfone is an mTORC1 pathway inhibitor and an active metabolite of Sulindac. It has been shown to effectively inhibit the growth of colon cancer cells and induce cell cycle arrest, making it a valuable tool in cancer research. This compound is primarily utilized to study the role of mTORC1 in tumorigenesis and to explore potential therapeutic strategies against colorectal cancer. -
mTOR
Dioctanoylphosphatidic acid sodium acts as a modulator of the mammalian target of rapamycin (mTOR) signaling pathway. This compound enhances phagocyte respiratory burst, serves as a precursor for diacylglycerol and lysophosphatidic acid, and improves the viability of gallbladder carcinoma cells when used in conjunction with histone deacetylase inhibitors (HDACIs). Its unique biosynthetic origins from glycerophospholipid highlight its relevance in cellular signaling research and cancer studies. -
mTORC1/glucose transporter Inhibitor
NV-5440 is an inhibitor of the mechanistic target of rapamycin complex 1 (mTORC1) and glucose transporters GLUT-1, GLUT-2, GLUT-3, and GLUT-4. This compound effectively inhibits glucose uptake in cells, providing valuable insights into glucose metabolism and its regulation. NV-5440 is useful for research applications involving cancer metabolism, diabetes, and other metabolic disorders where mTORC1 signaling and glucose transport play significant roles. -
FLNA Modulator
Simufilam hydrochloride is an orally active modulator of filamin A (FLNA) that targets neuronal signaling pathways. This compound restores NMDAR signaling and Arc expression while inhibiting dysregulated mTOR activity. Additionally, it enhances insulin sensitivity and mitigates Aβ42-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam hydrochloride is applicable in research related to Alzheimer's disease, particularly in understanding the underlying mechanisms of neurodegeneration. -
FLNA Modulator
Simufilam is an orally active modulator of filamin A (FLNA) that restores NMDA receptor (NMDAR) signaling and Arc expression. It effectively inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, which results in improved insulin sensitivity and a reduction in Aβ42-induced neuroinflammation and tau protein hyperphosphorylation. This compound is particularly valuable for research applications focused on Alzheimer's disease and related neurodegenerative disorders. -
mTORC1/S6K1 Inhibitor
Coronarin A is a natural compound that functions as an inhibitor of mTORC1 and S6K1, enhancing IRS1 activity. This compound exhibits anti-inflammatory properties and is relevant for research into type 2 diabetes mellitus. Its modulation of key signaling pathways makes Coronarin A a valuable tool for studying metabolic disorders and inflammation-related conditions. -
Nrf2/AMPK/mTOR Activator
Hydroxycitric acid is an orally active compound that serves as a multifunctional activator of Nrf2, AMPK, and mTOR pathways. It enhances the expression of antioxidant enzymes, such as superoxide dismutase, and increases glutathione levels, thereby mitigating oxidative stress and ferroptosis, particularly in renal tubular epithelial cells. Additionally, hydroxycitric acid induces cell cycle arrest in cancer cells and promotes DNA fragmentation through modulation of the AMPK and mTORC1/S6K signaling pathways. This compound is valuable for research in oxidative stress, cancer biology, and metabolic regulation. -
mTORC2 Inhibitor
JR-AB2-011 is a selective inhibitor of the mTORC2 complex, exhibiting an IC50 value of 0.36 μM. This compound disrupts the association between Rictor and mTOR (Ki: 0.19 μM), leading to reduced phosphorylation of Akt and decreased MMP2 activity. Consequently, JR-AB2-011 inhibits the migratory and invasive capabilities of tumor cells while also triggering non-apoptotic cell death. It serves as a valuable tool for research into cancer treatment and the regulation of cellular signaling pathways. -
mTORC1 Inhibitor
RMC-5552 is a potent and selective inhibitor of the mTORC1 pathway. It effectively inhibits the phosphorylation of S6K and 4EBP1 with IC50 values of 0.14 nM and 0.48 nM, respectively. RMC-5552 demonstrates significantly lower inhibition of AKT (IC50 of 19 nM), conferring a selectivity ratio for mTORC1 over mTORC2 of nearly 40-fold. This compound exhibits anti-cancer activity, making it a valuable tool for cancer research and therapeutic development targeting mTOR signaling. -
Rheb/mTORC1 Inhibitor
Rheb inhibitor NR1 is a selective Rheb/mTORC1 inhibitor with an IC50 of 2.1 µM in the Rheb-IVK assay. This compound directly binds to the switch II domain of Rheb, effectively inhibiting the activation of the mechanistic target of rapamycin complex 1 (mTORC1). Rheb inhibitor NR1 attenuates phosphorylation of T389pS6K1 while enhancing phosphorylation of S473pAKT in a dose-dependent manner, with no effect on mTORC2 activity. It serves as a valuable tool for investigating the mTOR signaling pathway and its implications in various diseases. -
PIP4K2C-mTOR Activator
C24-Ceramide is a competitive binding agonist of PIP4K2C, a key regulator of the mTOR signaling pathway. This compound facilitates cellular processes such as enhanced keratinocyte proliferation and migration, thereby promoting skin wound healing. Moreover, C24-Ceramide has been implicated in the proliferation and metastasis of gallbladder cancer cells, indicating its potential as a therapeutic target. Additionally, C24-Ceramide levels in serum may serve as a diagnostic marker for gallbladder cancer. -
mTORC1 Activator
Mefluleucine hydrochloride is a selective and orally active activator of mTORC1, functioning primarily through its interaction with Sestrin2. This leucine analog plays a critical role in neurobiology and has been utilized in research studies focused on antidepressant mechanisms. Its distinct properties make it a valuable tool for investigating mTORC1 signaling pathways and their implications in mood disorders. -
mTORC1-Selective Inhibitor
RMC-6272 is a bi-steric inhibitor selectively targeting mTORC1. It demonstrates potent inhibition of mTORC1 with over 10-fold selectivity compared to mTORC2, outperforming Rapamycin in its ability to inhibit mTORC1 and induce cell death in TSC2 null tumors. This compound is valuable for research applications focusing on cancer biology and therapeutic strategies targeting the mTOR signaling pathway. -
Dual PI3K/mTOR Inhibitor
PKI-179 is a highly effective dual inhibitor of PI3K and mTOR, exhibiting IC50 values of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ, and mTOR, respectively. It demonstrates significant activity against E545K and H1047R mutant isoforms, with IC50 values of 14 nM and 11 nM. PKI-179 is utilized in cancer research due to its proven anti-tumor efficacy in vivo, making it a valuable tool for investigating the PI3K/mTOR signaling pathway in various cancer models. -
mTOR Inhibitor
PQR626 is a selective mTOR inhibitor that demonstrates potent activity with an IC50 of 5 nM and a Ki of 3.6 nM. This orally active compound is designed for effective brain penetration, making it suitable for investigating neurological disorders. Research applications include studying the role of mTOR in neurodegenerative diseases and evaluating potential therapeutic strategies targeting this pathway. -
mTORC1/mTORC2 Inhibitor
MTI-31 is a potent inhibitor of mTORC1 and mTORC2, demonstrating high selectivity for mTOR with a Kd of 0.20 nM and over 5,000-fold selectivity against PIK3CA, PIK3CB, and PIK3G. It exhibits an IC50 of 39 nM in the LANCE assay for mTOR substrate phosphorylation in the presence of 100 μM ATP. This compound is valuable for research into breast cancer and other diseases involving aberrant mTOR signaling pathways. -
PI3K/mTOR Inhibitor
PI3K/mTOR Inhibitor-4 is a potent orally active pan-class I PI3K/mTOR inhibitor. It demonstrates enzymatic inhibition across PI3Kα, PI3Kγ, PI3Kδ, and mTOR with IC50 values of 0.63 nM, 22 nM, 9.2 nM, and 13.85 nM, respectively. This reagent is primarily utilized in cancer research to investigate the role of the PI3K/mTOR signaling pathway in tumorigenesis and therapeutic responses. -
mTOR Inhibitor
WYE-23 is a selective mTOR inhibitor with a reported IC50 of 0.45 nM against mTOR and 661 nM against PI3Kα. This compound exhibits significant antitumor activity, making it a valuable reagent for cancer research. It is particularly useful for studies investigating the role of mTOR signaling in tumorigenesis and therapeutic interventions targeting this pathway. -
PI3K/mTOR Inhibitor
PI3K/mTOR Inhibitor-11 is a potent oral inhibitor of the PI3K/mTOR signaling pathway, exhibiting IC50 values of 3.5 nM, 4.6 nM, and 21.3 nM for PI3Kα, PI3Kδ, and mTOR, respectively. This compound effectively impairs the phosphorylation of AKT and S6 proteins, thereby modulating critical cellular processes. PI3K/mTOR Inhibitor-11 is valuable for cancer research, offering insights into therapeutic strategies targeting aberrant signaling in tumors. -
mTORC1 Inhibitor
RMC-4627 is a selective inhibitor of the mechanistic target of rapamycin complex 1 (mTORC1), a key regulator of cell growth and proliferation. This compound has been shown to activate 4EBP1, leading to the downregulation of protein synthesis and subsequently inhibiting tumor growth. RMC-4627 is valuable for research applications focused on cancer biology and the elucidation of mTOR signaling pathways. -
TMBIM6 Antagonist
TMBIM6 antagonist-1 selectively inhibits TMBIM6, disrupting its interaction with mTORC2, and thereby decreasing mTORC2 activity. This compound also modulates TMBIM6-mediated calcium leakage, which is relevant for investigating calcium signaling pathways. TMBIM6 antagonist-1 serves as a valuable tool for research on cellular signaling and the role of TMBIM6 in various biological processes. -
mTOR Complex 1 Inhibitor
WRX606 is a selective inhibitor of the mTOR complex 1 (mTORC1), which effectively disrupts the phosphorylation of key mTORC1 substrates, including S6 kinase 1 (S6K1) and eukaryotic translation initiation factor 4E binding protein (4E-BP1), with IC50 values of 10 nM and 0.27 μM, respectively. This compound demonstrates significant antitumor activity by suppressing tumor growth in mouse models without promoting metastasis. WRX606 is a valuable tool for research focused on exploring therapeutic strategies against cancer through mTORC1 inhibition. -
mTOR Inhibitor
mTOR inhibitor WYE-28 selectively targets the mammalian target of rapamycin (mTOR), exhibiting an IC50 of 0.08 nM. Additionally, it inhibits PI3Kα with an IC50 of 6 nM, demonstrating its potential for broader applications in cancer therapy and metabolic research. WYE-28 has a metabolic half-life (T1/2) of 13 minutes in nude mouse microsomes, making it a valuable reagent for studying mTOR signaling pathways and their implications in disease models. -
mTOR Inhibitor
(32-Carbonyl)-RMC-5552 is a potent inhibitor of the mechanistic target of rapamycin (mTOR), effectively blocking mTORC1 and mTORC2 signaling pathways. This compound impedes the phosphorylation of key substrates including p-P70S6K-(T389), p-4E-BP1-(T37/36), and p-AKT1/2/3-(S473), with pIC50 values greater than 9 for the first two and between 8 and 9 for the latter. (32-Carbonyl)-RMC-5552 is valuable for studies investigating mTOR-related cellular processes and the development of therapies targeting mTOR in various diseases. -
mTORC1/2 Inhibitor
AZD3147 is a potent, orally bioavailable dual inhibitor of mTORC1 and mTORC2, exhibiting an IC50 value of 1.5 nM. This compound selectively targets both complexes, while also having a specific inhibitory effect on PI3K. AZD3147 is primarily utilized in research related to cancer therapeutics and metabolic disorders, where modulation of the mTOR signaling pathway is of significant interest. -
mTOR Inhibitor
WYE-687 dihydrochloride is an ATP-competitive inhibitor of the mechanistic target of rapamycin (mTOR), demonstrating an IC50 of 7 nM. This compound effectively inhibits the activation of both mTORC1 and mTORC2, making it a valuable tool for studying mTOR signaling pathways. Additionally, WYE-687 modulates PI3Kα and PI3Kγ activity with IC50 values of 81 nM and 3.11 μM, respectively, supporting its role in cancer and metabolic research. -
PI3K/mTOR Inhibitor
DS-7423 is a potent dual inhibitor of PI3K and mTOR, exhibiting IC50 values of 15.6 nM for PI3Kα and 34.9 nM for mTOR. This compound demonstrates significant anti-tumor activity, making it a valuable tool for research into cancer biology and potential therapeutic strategies. Its ability to inhibit key signaling pathways involved in cell growth and survival positions DS-7423 as a promising candidate for further exploration in oncology studies. -
PI3K/mTOR Inhibitor
PI3K-IN-37 is a potent inhibitor of the PI3K family, specifically targeting PI3K α, β, and δ isoforms with IC50 values of 6, 8, and 4 nM, respectively. Additionally, PI3K-IN-37 demonstrates strong inhibition of mTOR with an IC50 of 4 nM. This compound is valuable for research applications involving cancer biology, metabolic disorders, and signaling pathways related to cell growth and survival. -
PI3Kα/mTOR Kinase Inhibitor
PI3K-IN-22 is a potent dual inhibitor of the PI3Kα and mTOR kinases, with IC50 values of 0.9 nM and 0.6 nM, respectively. This compound exhibits substantial biological activity, making it valuable for investigating the roles of these pathways in cancer research. PI3K-IN-22 can facilitate the study of tumor growth and response to therapy, contributing to the understanding of oncogenic signaling and potential treatment strategies. -
Dual PI3K/mTOR Inhibitor
PKI-179 hydrochloride is a potent dual inhibitor of the PI3K and mTOR signaling pathways, demonstrating IC50 values of 8 nM for PI3K-α, 24 nM for PI3K-β, 74 nM for PI3K-γ, 77 nM for PI3K-δ, and 0.42 nM for mTOR. This compound is effective against mutant variants E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride has been shown to exhibit significant anti-tumor activity in vivo, making it a valuable tool for cancer research and therapeutic development targeting PI3K/mTOR pathways. -
PI3K/mTOR Inhibitor
SN32976 is a potent and selective inhibitor of class I phosphoinositide 3-kinases (PI3K) and mTOR, exhibiting IC50 values of 15.1 nM for PI3Kα, 461 nM for PI3Kβ, 110 nM for PI3Kγ, 134 nM for PI3Kδ, and 194 nM for mTOR. This compound demonstrates significant selectivity against a wide panel of 442 kinases. SN32976 is primarily utilized in cancer research, showcasing notable anticancer activity that makes it a valuable tool for studying PI3K/mTOR pathway modulation. -
mTOR Inhibitor
MHY-1685 is a novel inhibitor of the mammalian target of rapamycin (mTOR), a key regulator of cell growth and metabolism. This compound demonstrates significant potential in promoting human cardiac stem cell (hCSC)-based myocardial regeneration. Its efficacy in modulating the mTOR pathway makes MHY-1685 a valuable tool for researchers investigating cardiac repair mechanisms and therapies. -
PI3K/mTOR Inhibitor
PI3K/mTOR Inhibitor-13 sodium is a dual inhibitor targeting phosphoinositide 3-kinase (PI3K) and mTOR kinase, demonstrating oral bioavailability. This compound exhibits significant biological activity in the modulation of cellular growth and metabolism, making it a valuable tool in research related to sexual dysfunction, solid tumors, and idiopathic pulmonary fibrosis (IPF). Its dual inhibition profile presents opportunities for therapeutic exploration in various disease contexts. -
PI3K/mTOR inhibitor
PI3K-IN-18 is a potent inhibitor of the PI3K/mTOR signaling pathway, selectively targeting PI3K-α and mTOR with IC50 values of 41 nM and 49 nM, respectively. This compound exhibits significant biological activity by disrupting key signaling processes involved in cell growth and proliferation. PI3K-IN-18 is valuable for research applications focused on cancer biology, metabolism, and therapeutic strategies targeting the PI3K/mTOR axis. -
mTORC1/2 Inhibitor
Dihydroevocarpine is a selective inhibitor of mTORC1 and mTORC2, exhibiting potent cytotoxic effects in acute myeloid leukemia cells. By effectively suppressing mTORC1/2 activity, it disrupts critical signaling pathways involved in cell proliferation and survival. This compound is valuable for research focused on cancer biology and the development of targeted therapies for hematological malignancies.
