Catalog No.
Product Name
Application
Product Information
Citations
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MELK Inhibitor
MELK-8a is a highly potent and selective inhibitor of maternal embryonic leucine zipper kinase (MELK), demonstrating an IC50 of 2 nM. This compound also inhibits Flt3 (ITD), Haspin, and PDGFRα with IC50 values of 0.18, 0.19, and 0.42 μM, respectively. MELK-8a's primary application lies in cancer research, where MELK is crucial for regulating cell mitosis in specific cancer cell types. This makes MELK-8a a valuable tool for exploring therapeutic strategies targeting MELK-associated pathways in cancer. -
Fyn/GSK-3β Inhibitor
Fyn-IN-1 is a selective inhibitor of Fyn and GSK-3β, demonstrating IC50 values of 0.044 μM and 0.61 μM, respectively. This compound effectively downregulates the expression of the pro-inflammatory enzyme iNOS, making it a valuable tool in studying neuroinflammatory processes. Fyn-IN-1 is particularly relevant for research focused on neurodegenerative diseases, providing insights into potential therapeutic interventions. -
DYRK1A/GSK3β Inhibitor
GNF4877 is a potent dual inhibitor of DYRK1A and GSK3β, demonstrating IC50 values of 6 nM and 16 nM, respectively. This inhibition results in the blockade of nuclear export of nuclear factor of activated T-cells (NFATc) and promotes β-cell proliferation, with an EC50 of 0.66 μM in mouse β (R7T1) cells. GNF4877 serves as a valuable tool in research related to diabetes and T-cell signaling pathways. -
GSK-3β/FYN Inhibitor
ARN25068 is a sub-micromolar inhibitor targeting the protein kinases GSK-3β, FYN, and DYRK1A. It plays a significant role in modulating tau hyperphosphorylation, which is implicated in neurodegenerative diseases. This compound is valuable for research applications focused on neurobiology and pathology related to tau protein and related neurodegenerative processes. -
GSK3 Inhibitor
GSK3-IN-10 is a potent inhibitor of glycogen synthase kinase 3 (GSK3) isoforms α and β, demonstrating IC50 values of 1.0 nM and 2.0 nM, respectively. This compound effectively inhibits the activation of β-catenin, thereby promoting neuronal survival and providing a protective effect against endoplasmic reticulum stress. GSK3-IN-10 is valuable for research applications focused on neuroprotection and cellular stress response mechanisms. -
AChE/GSK-3β Inhibitor
AChE/GSK-3β-IN-1 is a dual inhibitor targeting acetylcholinesterase (AChE) and glycogen synthase kinase 3 beta (GSK-3β), demonstrating potent inhibition with IC50 values of 1.2 nM for hAChE, 149.8 nM for hBChE, and 22.4 nM for hGSK-3β. This compound effectively penetrates the blood-brain barrier and displays high selectivity for the CMGC kinase family, particularly binding to the ATP site of DYRK1A. Additionally, AChE/GSK-3β-IN-1 has been shown to inhibit reactive oxygen species (ROS) expression, thereby reducing oxidative stress. It is a valuable tool for research into Alzheimer's disease and related neurodegenerative conditions. -
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. -
MELK Inhibitor
JNJ-47117096 is a selective inhibitor of the maternal embryonic leucine zipper kinase (MELK), exhibiting an IC50 of 23 nM. Additionally, it demonstrates significant inhibition of Flt3, with an IC50 of 18 nM. This compound is valuable for research applications focused on cancer biology, particularly in studies investigating cell proliferation and survival pathways associated with MELK and Flt3. -
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. -
PI3Kα Inhibitor
PI3Kα-IN-14 is a selective inhibitor of the phosphoinositide 3-kinase alpha (PI3Kα) isoform, demonstrating a potent IC50 value of 0.14 nM. This compound effectively reduces mitochondrial membrane potential, leading to cell cycle arrest in the G1 phase and initiating apoptosis in U87-MG glioma cells. PI3Kα-IN-14 exhibits significant anti-proliferative effects across a range of tumor-derived cell lines, including PC-3 (IC50 of 0.28 μM), HCT-116 (IC50 of 0.57 μM), and U87-MG (IC50 of 1.37 μM), making it a valuable tool in cancer research and therapeutic studies targeting PI3K signaling pathways. -
AMPK Activator
Thalidezine is a selective activator of AMP-activated protein kinase (AMPK), a crucial regulator of cellular energy homeostasis. It has been shown to promote autophagic cell death in anti-apoptotic cancer cells by modulating energy metabolism. Thalidezine serves as a valuable tool for investigating the mechanisms of apoptosis and potential therapeutic interventions in cancer research. -
PI3K Inhibitor
TYM-3-98 is a selective inhibitor of PI3Kδ, demonstrating an IC50 of 7.1 nM. This compound effectively inhibits the proliferation of B-lymphoma cells and disrupts the PI3K/AKT/mTOR signaling pathway, leading to the induction of apoptosis. Additionally, TYM-3-98 shows favorable pharmacokinetic properties and exhibits antitumor efficacy in mouse and rat models, while exhibiting minimal toxicity. -
PI3Kα Inhibtor
PI3Kα-IN-8 is a selective inhibitor of PI3Kα, exhibiting an IC50 of 0.012 μM. This compound increases intracellular levels of reactive oxygen species, reduces mitochondrial membrane potential, and effectively induces apoptosis. It is valuable in research applications focused on cancer biology and therapeutics targeting the PI3K signaling pathway. -
PI3K/VEGFR2 Inhibitor
PI3K/VEGFR2-IN-1 is a highly effective dual inhibitor of PI3K and VEGFR2, exhibiting IC50 values of 2.21 μM and 68 μM, respectively. This compound has been shown to induce apoptosis in various cancer cell lines. It is suitable for research applications focused on cancer biology and therapy development targeting the PI3K/VEGFR2 signaling pathways. -
PI3K Inhibitor
PIK-C98 is a potent and selective inhibitor of phosphoinositide 3-kinases (PI3K), exhibiting IC50 values of 0.59, 1.64, 3.65, and 0.74 μM for the α, β, δ, and γ isoforms, respectively. This compound effectively inhibits all class I PI3Ks while leaving AKT and mTOR activity unaffected. PIK-C98 operates by disrupting the ATP-binding sites of PI3Ks, forming hydrogen bonds and arene-H interactions with target amino acid residues. Its capacity to induce apoptosis via PI3K inhibition makes PIK-C98 a valuable tool for research into multiple myeloma and other related conditions. -
PI3K Inhibitor
Ramentaceone (7-Methyljuglon) is a naphthoquinone that selectively inhibits phosphoinositide 3-kinase (PI3K) activity. This compound effectively reduces PI3K protein expression and decreases Akt protein phosphorylation in breast cancer cells, thereby inducing apoptosis. Ramentaceone's mechanism of action makes it a valuable tool for research in cancer biology and therapeutic development targeting the PI3K/Akt signaling pathway. -
PI3K/EGFR Inhibitor
MTX-216 is a dual ATP-competitive inhibitor targeting PI3K and EGFR. It effectively cosuppresses Ki-67 and phosphorylation of ribosomal S6, leading to apoptosis in NF1LOF cells. Additionally, MTX-216 inhibits SYK kinase activity with an IC50 of 281 nM. This compound is primarily utilized in research related to melanoma. -
AMPK/SIRT3/PGC-1α Modulator
MitoPBN is an AMPK/SIRT3/PGC-1α modulator that enhances mitochondrial function by acting as a reactive oxygen species scavenger. This compound promotes mitochondrial biogenesis through increased AMPK phosphorylation, restoration of SIRT3 expression, and upregulation of PGC-1α. MitoPBN is effective in regulating glucose metabolism, as it decreases blood glucose levels by inhibiting hepatic gluconeogenesis and enhancing glucose uptake, while also improving ATP production and maintaining mitochondrial membrane potential. Additionally, it can reduce apoptosis and enhance sperm motility and membrane integrity, making it a valuable reagent for research related to diabetes and metabolic disorders. -
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. -
PI3Kδ Inhibitor
IHMT-PI3Kδ-372 is a highly selective inhibitor of PI3Kδ, exhibiting an IC50 of 14 nM. This compound demonstrates significant selectivity over other class I PI3Ks, with 56 to 83-fold differences, as well as over various protein kinases. IHMT-PI3Kδ-372 is suitable for research applications related to chronic obstructive pulmonary disease (COPD), enabling investigations into therapeutic strategies targeting this pathway. -
PI3K Inhibitor
Isopsoralidin is a phosphatidylinositol 3-kinase (PI3K) inhibitor that demonstrates potentially hepatotoxic properties and exhibits inhibitory activity on CYP2D6. This compound plays a significant role in research focused on cell signaling pathways related to cancer and metabolic disorders. Its unique mechanism of action makes it a valuable tool for studying PI3K-related biological processes and evaluating therapeutic approaches involving PI3K modulation. -
PI3K Kinase Ligand
HL-2 is a selective ligand for the phosphoinositide 3-kinase (PI3K) kinase, utilized in the synthesis of proteolysis-targeting chimeras (PROTACs). Its role in modulating PI3K activity makes it a valuable tool for studying signal transduction pathways and cancer biology. HL-2's application extends to drug development and the investigation of therapeutic strategies targeting PI3K-related diseases. -
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.
