Catalog No.
Product Name
Application
Product Information
Citations
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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. -
PI3K Inhibitor
PI3K-IN-34 is a selective inhibitor of phosphoinositide 3-kinases (PI3Ks), specifically demonstrating IC50 values of 11.73 μM for PI3K-α, 6.09 μM for PI3K-β, and 11.18 μM for PI3K-δ. This compound effectively induces G2/M cell cycle arrest and promotes apoptotic pathways in targeted cells. PI3K-IN-34 is particularly useful in preclinical studies involving leukemia, providing insights into therapeutic strategies for this malignancy. -
ATM Inhibitor
ATM Inhibitor-7 is a selective inhibitor of ataxia-telangiectasia mutated (ATM) with an IC50 of 1.0 nM. This compound effectively induces apoptosis and causes G2/M phase cell cycle arrest, particularly when combined with CPT-11. ATM Inhibitor-7 is utilized in research applications focused on elucidating mechanisms of tumor biology and enhancing the efficacy of chemotherapeutic agents. -
Estrogen Receptor Agonist, Voltage-Gated Sodium Channel Blocker, PI3K-AKT/JNK Signaling Modulator,
Propylparaben sodium acts as a weak estrogen receptor agonist and serves as a voltage-gated sodium channel blocker, while also modulating the PI3K-AKT and JNK signaling pathways. It is known to induce oxidative stress, affecting the estrous cycle and hormone levels, as well as ovarian reserve function. Propylparaben sodium can inhibit the growth of antral follicles and influence the accumulation of steroid hormones in follicle culture media. This compound is suitable for research related to ovarian aging and myocardial ischemia-reperfusion injury. -
NF-κB/MAPK/FAK/Akt Inhibitor
Ephemeranthol A is an inhibitor of NF-κB, MAPK, FAK, and Akt signaling pathways. This phenanthrene compound demonstrates notable anti-inflammatory effects through the inhibition of NF-κB and MAPK pathways in macrophages. Additionally, Ephemeranthol A induces apoptosis and inhibits metastasis in non-small cell lung cancer by suppressing FAK/Akt signaling and epithelial-mesenchymal transition (EMT) processes. It is applicable for research into acute and chronic inflammatory diseases as well as non-small cell lung cancer. -
PI3Kδ/γ Inhibitor
PI3Kδ/γ-IN-3 is a potent dual inhibitor of PI3Kδ and PI3Kγ, with IC50 values of 1 nM and 16 nM, respectively. This compound effectively induces apoptosis in tumor cells, making it a valuable tool for research in B-cell malignancies. Its oral bioavailability further enhances its utility in preclinical studies aimed at understanding and targeting these pathways in cancer therapy. -
PI3Kα Inhibitor
PI3Kα-IN-7 is a potent inhibitor of the PI3Kα isoform, with additional inhibitory effects on PI3Kβ. This compound is known to reduce mitochondrial membrane potential in cancer cells, leading to the induction of apoptosis. It is valuable for research applications focused on cancer biology and therapeutic development targeting the PI3K signaling pathway. -
PI3K Inhibitor
PI3K-IN-35 is a selective inhibitor of phosphoinositide 3-kinases (PI3Ks) with IC50 values of 13.98, 7.22, and 10.94 μM for PI3K-α, PI3K-β, and PI3K-δ, respectively. This compound effectively induces cell cycle arrest at the G2/M phase and promotes apoptosis, making it a valuable tool for studies in leukemia research. Investigators can utilize PI3K-IN-35 to explore the role of PI3K signaling in cancer progression and therapeutic responses. -
PI3K/HDAC Inhibitor
Fimepinostat mesylate is a potent dual inhibitor targeting class I phosphoinositide 3-kinases (PI3Ks) and histone deacetylases (HDACs). It exhibits IC50 values of 19 nM for PI3Kα, 54 nM for PI3Kβ, 39 nM for PI3Kδ, and 1.7 nM for HDAC1, 5.0 nM for HDAC2, 1.8 nM for HDAC3, and 2.8 nM for HDAC10. This compound is valuable for research applications focusing on cancer biology, epigenetic regulation, and cellular signaling pathways. -
PI3Kδ Inhibitor
WNY1613 is a potent and selective inhibitor of phosphoinositide 3-kinase delta (PI3Kδ) featuring a piperazinone-containing purine scaffold. This compound effectively induces apoptosis in cancer cells and inhibits the phosphorylation of downstream components of the PI3K signaling pathway in non-Hodgkin lymphoma (NHL) cell lines. WNY1613 demonstrates significant anti-NHL activity both in vitro and in vivo, making it a valuable tool for cancer research and therapeutic investigations. -
PI3Kα Inhibitor
XJTU-L453 is a selective inhibitor of PI3Kα, exhibiting an IC50 of 0.4 nM. It effectively suppresses the proliferation of breast cancer cell lines, T47D and MCF7, with IC50 values of 0.2 μM and 0.5 μM, respectively. By inhibiting the PI3K pathway, XJTU-L453 induces cell cycle arrest and promotes apoptosis, demonstrating significant antitumor activity in MCF7 xenograft models. This compound is valuable for research in cancer biology and therapeutic development targeting the PI3K signaling pathway. -
AMPK Activator
GL-V9 is an AMPK activator that modulates cellular metabolism and promotes apoptosis in HepG2 cells, with an IC50 of 35.2 μM. It induces cell cycle arrest at the G2/M phase and alters mitochondrial membrane potential, leading to increased intracellular reactive oxygen species. By inhibiting the pentose phosphate pathway and enhancing fatty acid oxidation via AMPK activation, GL-V9 significantly impedes cancer cell metastasis and demonstrates antitumor efficacy in mouse models, making it a valuable tool for cancer research. -
PI3K-α Inhibitor
PI3Kα-IN-27 is a potent inhibitor of the PI3K-α enzyme, exhibiting an IC50 value of 40 nM. This compound effectively targets and inhibits key signaling proteins, including PAK3, p110α, phospho-mTOR, and phospho-ERK1/2, leading to the induction of early apoptosis. Its significant anticancer activity has been demonstrated in various cancer models, including pancreatic, lung, and breast cancers, making it a valuable tool for research in cancer biology and targeted therapies. -
ATM Inhibitor
Lartesertib is a potent inhibitor of the serine/threonine protein kinase ATM. This compound has demonstrated the ability to inhibit the growth of various hematopoietic cell lines. Furthermore, in combination with the ATR inhibitor Tuvusertib, Lartesertib enhances tumor cell apoptosis and activates immune signaling pathways, showcasing significant anti-tumor efficacy. -
ATM Inhibitor
(Rac)-Lartesertib is a potent inhibitor of the serine/threonine protein kinase ATM. This compound has demonstrated the ability to inhibit cell proliferation in various hematopoietic cell lines. Moreover, when used in conjunction with the ATR inhibitor Tuvusertib, (Rac)-Lartesertib can enhance tumor cell death, activate immune signaling pathways, and exhibit notable anti-tumor efficacy, making it a valuable tool for cancer research. -
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. -
PI3Kδ/CSF1R Inhibitor
JMC14 is a selective PI3Kδ and CSF1R inhibitor, exhibiting IC50 values of 12 nM and 143 nM, respectively. This compound preferentially disrupts PI3Kδ-mediated signaling within cells, demonstrating significant antitumor activity against B-cell lymphomas and triple-negative breast cancer (TNBC) in both in vitro and in vivo models. JMC14 is an important tool for research into antitumor immunity and the mechanisms of cancer progression. -
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. -
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. -
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. -
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. -
ATR Inhibitor
ART0380 is a potent and selective ATR kinase inhibitor that targets the ATR-ATRIP complex. With an IC50 of 51.7 nM, ART0380 effectively inhibits ATR-dependent Chk1 serine 345 phosphorylation, leading to cell cycle disruption and DNA damage. This compound exhibits significant antitumor activity in preclinical models featuring various ataxia-telangiectasia mutated (ATM) gene alterations. ART0380 is applicable for cancer research, particularly in studies related to colorectal and prostate cancer. -
Akt Activator
9(10)-Nitrooleate is an Akt activator that enhances enzymatic activity and promotes nitric oxide bioavailability. By inducing the phosphorylation of Akt and ERK1/2, it regulates the multi-site phosphorylation of eNOS and optimizes its interaction with Hsp90, contributing to its vasoprotective effects. Additionally, 9(10)-Nitrooleate activates PPARα, PPARδ, and PPARγ receptors, influencing adipogenesis, glucose uptake, and inflammatory gene expression. Its immunosuppressive properties also inhibit neutrophil migration and cytokine secretion, making it valuable for research on sepsis and related inflammatory conditions. -
PI3K/AKT/ERK/CREB Activator
PI3K/AKT/ERK/CREB Activator 1 is a small molecule that stimulates the PI3K/AKT/ERK/CREB signaling pathway. It enhances neuronal survival and proliferation, promoting the viability of damaged neurons and facilitating synapse formation. This compound also reduces neuroinflammation by decreasing pro-inflammatory cytokine levels, and it has shown potential in preserving synaptic structure and improving spatial memory in Alzheimer's disease models. PI3K/AKT/ERK/CREB Activator 1 is a valuable tool for research focused on neurodegenerative disorders, particularly Alzheimer's disease. -
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. -
PI3Kδ/CK1ε Inhibitor
Umbralisib tosylate is a potent and selective dual inhibitor of PI3Kδ and casein kinase-1-ε (CK1ε), exhibiting an EC50 of 22.2 nM and 6.0 μM, respectively. This compound demonstrates significant immunomodulatory effects on T cells from chronic lymphocytic leukemia (CLL) patients. Umbralisib tosylate is primarily utilized in research focused on hematological malignancies to elucidate its therapeutic potential and mechanisms of action. -
PI3Kδ/CK1ε Inhibitor
Umbralisib sulfate is a potent and selective dual inhibitor of PI3Kδ and casein kinase-1-ε (CK1ε), with EC50 values of 22.2 nM and 6.0 μM, respectively. This compound demonstrates notable immunomodulatory effects on T cells in chronic lymphocytic leukemia (CLL). Umbralisib sulfate is a valuable tool for research into hematological malignancies, facilitating studies on cell signaling pathways and potential therapeutic strategies. -
HSF1/AMPK Axis Activator
HSF1/AMPK activator 1 is a potent modulator of the HSF1/AMPK axis, targeting the TGF-β1/Smad signaling pathway. This compound demonstrates significant anti-hepatic fibrosis activity by inhibiting fibrosis formation and cell proliferation in activated hepatic stellate cells. Additionally, HSF1/AMPK activator 1 effectively alleviates liver injury and symptoms of hepatic fibrosis in fibrotic mouse models. It is a valuable tool for research focused on hepatic fibrosis and related metabolic disorders. -
GSK3β Inhibitor
GSK3β-IN-2 is a potent GSK3β inhibitor with an IC50 of 0.35 nM. This compound activates the Wnt/β-catenin signaling pathway, leading to enhanced neurogenesis and neurite outgrowth. Additionally, GSK3β-IN-2 effectively inhibits Aβ-induced tau hyperphosphorylation at Ser396 and reduces neurofibrillary tangle formation. Its efficacy in ameliorating Alzheimer's disease has been demonstrated in zebrafish models, making it a valuable tool for neurological research. -
GSK-3 Inhibitor
Laduviglusib dihydrochloride is a selective inhibitor of glycogen synthase kinase-3 (GSK-3), an enzyme involved in numerous cellular processes including glycogen synthesis, cell differentiation, and apoptosis. By inhibiting GSK-3, Laduviglusib dihydrochloride promotes cell survival and has been extensively studied in the context of neurodegenerative diseases, diabetes, and cancer research. This compound serves as a valuable tool for elucidating the role of GSK-3 in various signaling pathways and therapeutic applications. -
GSK3β Inhibitor
BRD1172 is a selective inhibitor of glycogen synthase kinase 3 beta (GSK3β), exhibiting an IC50 of 24 nM. This compound effectively inhibits GSK3β-mediated Tau phosphorylation in SH-SY5Y cells and alleviates the negative regulation of GSK3β on β-catenin degradation and TCF/LEF promoter activity. BRD1172 is applicable in research related to Alzheimer’s disease, cardiac hypertrophy, and various cancers. -
AMPK Activator
Isovaleric acid is an AMPK activator known for its role in inhibiting osteoclast differentiation through the stimulation of AMPK phosphorylation. Additionally, it promotes colonic smooth muscle relaxation via the activation of the cAMP/PKA pathway. This compound is applicable in research focusing on skeletal diseases, including osteoporosis, as well as intestinal disorders. -
AMPK Activator
NFAT-133 is an aromatic polyketide that functions as an AMPK activator. It enhances glucose uptake in muscle cells, showing potential as an antidiabetic agent. Additionally, NFAT-133 suppresses T-cell proliferation and IL-2 expression by inhibiting the transcriptional activity of nuclear factor of activated T-cells (NFAT), exhibiting immunosuppressive properties. This compound also reduces nitric oxide production in RAW264.7 cells stimulated by lipopolysaccharide (LPS), without displaying antibacterial or cytotoxic effects. -
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. -
AMPK Activator
RSVA405 is a potent, orally bioavailable activator of AMP-activated protein kinase (AMPK), exhibiting an EC50 of 1 μM. This compound enhances CaMKKβ-mediated activation of AMPK, leading to the inhibition of mTOR and promotion of autophagy, which in turn increases the degradation of amyloid beta (Aβ). Additionally, RSVA405 demonstrates anti-inflammatory properties by inhibiting STAT3 activity, and is applicable in obesity research. -
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. -
AMPK Inducer
Malvidin-3-O-arabinoside chloride is an AMPK inducer that enhances cellular autophagy. This compound is recognized for its ability to mitigate oxidative damage induced by ethyl carbamate through the activation of AMPK signaling pathways. Its biological activity supports research applications focused on metabolic disorders and oxidative stress-related conditions. -
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. -
PDK1/Akt Phosphorylation Activator
Sexangularetin 3-sophoroside is an activator of PDK1 and Akt phosphorylation pathways, demonstrating significant neuroprotective effects. This compound restores levels of phosphorylated GSK-3β protein and functions as a reactive oxygen species (ROS) inhibitor. Additionally, it modulates the expression of superoxide dismutase 1 and catalase mRNA, making it a valuable tool for research related to neurodegenerative conditions such as Parkinson’s disease. -
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.
