Catalog No.
Product Name
Application
Product Information
Citations
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AKT1 Inhibitor
Tanerasertib is an inhibitor of AKT1, specifically targeting the AKT1E17K mutant with an EC50 range of 15-60 nM. This compound exhibits significant biological activity that may be leveraged in cancer research, particularly in studies focusing on the role of the AKT signaling pathway in tumorigenesis and treatment resistance. Its application in preclinical models can provide insights into therapeutic strategies for cancers harboring AKT1 mutations. -
Akt Inhibitor
K-80003 is a potent Akt inhibitor that specifically targets and inhibits tRXRα-dependent Akt activation. This compound exhibits significant biological activity in suppressing cancer cell growth, making it valuable in cancer research. K-80003 is useful for studies investigating Akt signaling pathways and therapeutic strategies against malignancies. -
Akt Inhibitor
1-Formyl-beta-carboline is an alkaloid that functions as an Akt inhibitor, disrupting key signaling pathways. It demonstrates significant inhibitory activity against Newcastle disease virus (NDV), with IC50 values below 10 μM and over 90% inhibition at 20 μM concentration. The compound primarily targets the adsorption and entry phases of the NDV life cycle by directly interacting with the NDV hemagglutinin-neuraminidase (HN) protein. Additionally, 1-Formyl-beta-carboline affects viral entry through modulation of the PI3K/Akt signaling pathway. -
Akt Inhibitor
Hu7691 is a selective Akt inhibitor that exhibits potent inhibitory activity with IC50 values of 4.0 nM, 97.5 nM, and 28 nM against Akt1, Akt2, and Akt3, respectively. This compound has been shown to inhibit tumor growth while reducing cutaneous toxicity in mouse models, making it a valuable tool for cancer research. Its specificity and efficacy position Hu7691 as a promising reagent for studies focused on the Akt signaling pathway and its role in tumorigenesis. -
pan-AKT Inhibitor
Vevorisertib is a potent and selective pan-AKT serine/threonine kinase inhibitor, effectively targeting AKT1 (IC50=0.55 nM), AKT2 (IC50=0.81 nM), and AKT3 (IC50=1.31 nM). This orally active compound demonstrates significant biological activity in inhibiting AKT pathways and is applicable in the study of solid tumors harboring PIK3CA, AKT, or PTEN mutations. Vevorisertib can be utilized as a monotherapy or in combination with other anti-cancer agents for enhanced therapeutic efficacy in cancer research. -
PI3K Inhibitor
HL-8 is a potent PI3Kα degrader that functions through the targeted protein degradation mechanism of PROTAC technology. By promoting the ubiquitination and subsequent degradation of PI3Kα, HL-8 effectively reduces phospho-AKT levels, thereby interfering with key signaling pathways associated with cancer progression. This compound exhibits significant anticancer activity against colon and cervical cancer, making it a valuable tool for research in cancer biology and therapeutic development. -
Pan-PI3K Inhibitor
KTC1101 is a potent oral pan-PI3K inhibitor targeting the phosphoinositide 3-kinase (PI3K) signaling pathway. It effectively reduces downstream phosphorylation of AKT and mTOR, leading to decreased expression of Ki67. KTC1101 exhibits dual anti-tumor mechanisms by directly inhibiting tumor cell proliferation and enhancing the immune response, making it a valuable tool for cancer research and therapeutic applications. -
Insulin Receptor Agonist/Akt Activator
Demethylasterriquinone B1 is an orally active insulin receptor agonist that functions as an AKT activator. This compound enhances eNOS expression and activity, resulting in increased nitric oxide production, while simultaneously downregulating the NADPH oxidase subunit p22phox to mitigate oxidative stress and improve vascular endothelial function. Additionally, Demethylasterriquinone B1, when combined with an AKT inhibitor, can modulate the insulin signaling pathway to activate antiviral pathways, including RNA interference and JAK/STAT, in mosquitoes, thereby demonstrating potential in reducing Zika virus infection. -
Akt Inhibitor
GSK2110183 analog 1 hydrochloride is a structural analogue designed to inhibit Akt, a critical signaling protein involved in various cellular processes such as growth, survival, and metabolism. This compound demonstrates potent Akt inhibitory activity, making it a valuable tool for studying the role of Akt in cancer progression and treatment. Its applications extend to exploring therapeutic strategies targeting the Akt pathway in various disease models. -
Akt Substrate
Crosstide is a peptide analog derived from the glycogen synthase kinase α/β fusion protein sequence, serving as a substrate for Akt. This compound is widely used in research to investigate Akt signaling pathways and assess kinase activity. Crosstide facilitates studies focused on cellular metabolism, growth, and survival, providing valuable insights into the roles of Akt in various biological processes and diseases. -
PI3K/Akt Activator
Hydroxy celecoxib is a derivative of Celecoxib that functions as a PI3K/Akt signaling activator, facilitating epithelial repair processes. Its activation of the PI3K/Akt pathway supports cellular survival and proliferation, making it a valuable tool for investigating mechanisms of tissue regeneration. Hydroxy celecoxib is particularly relevant in asthma research, where it may contribute to understanding airway epithelial function and repair. -
PI3K-Akt Inhibitor
AKT Inhibitor IV is a potent PI3K-Akt pathway inhibitor that selectively targets the E isomer. This compound exhibits significant cytotoxic effects, making it valuable for research applications focusing on cell proliferation, survival, and apoptosis. It is ideal for studies investigating the role of the PI3K-Akt signaling pathway in cancer and other diseases. -
AKT Inhibitor
CCT128930 hydrochloride is a selective inhibitor of AKT, demonstrating an IC50 of 6 nM. It exhibits significant selectivity, being 28-fold more potent against AKT than the closely related PKA kinase (IC50 of 168 nM) and 20-fold more effective than p70S6K (IC50 of 120 nM). CCT128930 hydrochloride is recognized for its ability to induce cell cycle arrest, promote DNA damage, and stimulate autophagy, enabling its application in cancer research and potential antitumor strategies. -
Allosteric Akt Inhibitor
Pifusertib is a selective, orally active allosteric inhibitor of Akt, exhibiting IC50 values of 4.8, 1.6, and 44 nM for Akt1, Akt2, and Akt3, respectively. This compound demonstrates significant anti-myeloma activity and intensifies lethal endoplasmic reticulum (ER) stress resulting from proteasome inhibition. In addition, Pifusertib promotes both apoptosis and autophagy, making it a useful tool for research in cancer biology and therapeutic development. -
Allosteric Akt Inhibitor
MK-2206 is a highly potent and selective allosteric inhibitor of the Akt signaling pathway, exhibiting IC50 values of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. This compound demonstrates significant anticancer activity, particularly in breast cancer cell lines and those harboring PIK3CA mutations or loss of PTEN function. MK-2206 is valuable for research investigating Akt's role in cancer progression and therapeutic resistance. -
AKT1/2 Inhibitor
Engasertib is a potent and selective inhibitor of AKT1 and AKT2, displaying IC50 values of 0.13 µM and 0.09 µM, respectively, with a slightly lower potency against AKT3 at 2.75 µM. This compound effectively inhibits AKT phosphorylation, leading to modulation of downstream signaling pathways in vitro. Due to its ability to suppress cancer cell proliferation and tumor growth, Engasertib serves as a valuable tool for cancer research and therapeutic development. -
ERK/Akt Activator
H-Ile-Lys-Val-Ala-Val-OH is a potent activator of the MAPK/ERK1/2 and PI3K/Akt signaling pathways. This compound enhances cell adhesion, promotes neurite outgrowth, and supports tumor growth. It is particularly effective in stimulating the proliferation of bone marrow-derived mesenchymal stem cells (BMMSCs), making it valuable for research applications in cell biology and regenerative medicine. -
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. -
pan-AKT/AKT1-E17K Mutant Inhibitor
Vevorisertib trihydrochloride is a selective, allosteric inhibitor targeting pan-AKT and the AKT1-E17K mutant. It effectively inhibits AKT phosphorylation, demonstrating Kd values of 1.2 nM for AKT1 and 8.6 nM for AKT1-E17K, along with IC50 values of 0.55 nM, 0.81 nM, and 1.3 nM for AKT1, AKT2, and AKT3, respectively. This compound is valuable for cancer research, aiding in the exploration of therapeutic strategies targeting the AKT signaling pathway. -
Allosteric Akt Inhibitor
Pifusertib hydrochloride is a selective allosteric inhibitor of Akt, exhibiting IC50 values of 4.8 nM, 1.6 nM, and 44 nM for Akt1, Akt2, and Akt3, respectively. This compound demonstrates significant anti-myeloma activity by enhancing endoplasmic reticulum stress in the context of proteasome inhibition. Additionally, Pifusertib hydrochloride induces both apoptosis and autophagy, making it a valuable tool for research into cancer therapies and the modulation of cellular stress responses. -
AMPK Activator
Candidusin A is a potent AMPK activator with a KD of 47.28 nM, isolated from the marine fungus Aspergillus candidus. This compound demonstrates significant cytotoxicity, inducing apoptosis in human prostate cancer cell lines such as 22Rv1, PC-3, and LNCaP. Additionally, Candidusin A reduces the expression of adipogenesis-related genes and fat deposition, while negatively regulating the NF-κB-TNFα inflammatory axis to mitigate inflammation. Its diverse biological activities make Candidusin A a valuable tool for research into non-alcoholic steatohepatitis (NASH) and liver injury. -
PI3K/HDAC Inhibitor
PI3K/HDAC-IN-3 is a dual inhibitor targeting PI3K and HDAC, with IC50 values of 0.23 nM for PI3Kα and 172 nM for HDAC1. It effectively suppresses AKT phosphorylation while enhancing H3 acetylation in MV4-11 cells. Additionally, PI3K/HDAC-IN-3 demonstrates notable anticancer efficacy in a dose-dependent manner within an MV4-11 xenograft model, making it a valuable tool for studying cancer biology and potential therapeutic interventions. -
PI3Kα/HDAC6 Inhibitor
PI3Kα/HDAC6-IN-1 is a dual inhibitor targeting PI3Kα and HDAC6, exhibiting IC50 values of 2.9 nM and 26 nM, respectively. This compound effectively inhibits AKT (Ser473) phosphorylation and promotes the accumulation of acetylated α-tubulin, while not influencing acetylated histones H3 and H4. Its potent anti-cancer activity is demonstrated in the L-363 cell line with an IC50 of 0.17 μM, highlighting its potential for therapeutic applications in cancer research. -
PI3K Inhibitor
PI3K/HDAC-IN-1 is a potent dual inhibitor targeting phosphoinositide 3-kinase (PI3K) and histone deacetylase (HDAC). It effectively inhibits PI3Kδ and HDAC1 with IC50 values of 8.1 nM and 1.4 nM, respectively. This compound is valuable for studying the roles of PI3K and HDAC in various cellular processes and can aid in cancer research by exploring the therapeutic potential of dual inhibition in tumor models. -
AMPK Activator
Danthron is an AMPK activator that plays a critical role in regulating glucose and lipid metabolism. Derived from the traditional Chinese medicinal plant Salvia miltiorrhiza Bunge, Danthron has demonstrated potential in enhancing cellular energy balance. Its biological activity makes it a valuable reagent for research in metabolic disorders and related therapeutic applications. -
ATR PROTAC Degrader
PROTAC ATR degrader-2 is a selective degrader targeting the ATR protein. It effectively induces degradation of ATR in acute myeloid leukemia (AML) cell lines MV-4-11 and MOLM-13, demonstrating DC50 values of 22.9 nM and 34.5 nM, respectively. This compound has an IC50 of 29.6 nM against ATR, while exhibiting minimal activity against ATM and PI3K. PROTAC ATR degrader-2 promotes apoptosis, causes DNA damage, and upregulates p53 expression, thereby inhibiting cancer cell proliferation. This reagent is suitable for research applications focused on understanding mechanisms in acute myeloid leukemia. -
PI3Kδ Inhibitor
FD223 is a potent and selective inhibitor of phosphoinositide 3-kinase delta (PI3Kδ), demonstrating an IC50 of 1 nM. It shows significant selectivity over other isoforms, with IC50 values of 51 nM, 29 nM, and 37 nM for α, β, and γ, respectively. FD223 effectively inhibits the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473, leading to G1 phase arrest in the cell cycle. This compound holds potential for research into leukemia, particularly AML. -
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. -
PI3K/HDAC Inhibitor
PI3K/HDAC-IN-2 is a potent dual inhibitor of phosphoinositide 3-kinase (PI3K) and histone deacetylase (HDAC), demonstrating IC50 values of 226 nM for PI3Kα, 279 nM for PI3Kβ, 467 nM for PI3Kγ, and 29 nM for PI3Kδ. It also exhibits selective inhibition with IC50 values of 1.3 nM for HDAC1, 3.4 nM for HDAC2, 972 nM for HDAC4, 17 nM for HDAC6, and 12 nM for HDAC8. Due to its significant anticancer properties, PI3K/HDAC-IN-2 is valuable for research applications in cancer biology and therapeutic development. -
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. -
GSK-3β/G9a Inhibitor
GSK-3β/G9a-IN-1 is a selective inhibitor of GSK-3β and G9a, acting through competitive mechanisms with IC50 values of 0.8 μM and 1.1 μM, respectively. This compound is effective in lowering tau phosphorylation and reducing Aβ aggregation, making it relevant for Alzheimer's disease research. Additionally, GSK-3β/G9a-IN-1 influences chromatin dynamics by inhibiting H3K9me2 and modulating members of the SAGA complex. Its ability to improve memory and restore social behaviors highlights its potential as a therapeutic agent in neurodegenerative conditions. -
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. -
Tubulin Polymerization/Akt Pathway Inhibitor
KS-99 is an inhibitor that targets both tubulin polymerization and the Akt signaling pathway. This compound demonstrates significant biological activity by inhibiting cancer cell proliferation and inducing apoptosis in various cancer cell types. KS-99 is suitable for research applications involving colorectal cancer, breast cancer, lung epithelial cancer, and melanoma. -
PI3Kα Inhibitor
VVD-442 is a selective inhibitor of PI3Kα that covalently binds to cysteine 242 within the RAS-binding domain of the PI3K p110α subunit. This binding induces conformational changes that disrupt the interaction between PI3K p110α and RAS proteins, effectively blocking RAS-mediated activation of PI3K. VVD-442 is applicable in research focusing on RAS-mutant cancers and HER2-overexpressing tumors, providing valuable insights into therapeutic strategies targeting these pathways. -
PI3Kδ Inhibitor
LAS195319 is a potent and orally active inhibitor of PI3Kδ, exhibiting an IC50 of 0.5 nM. This compound demonstrates high selectivity against a wide array of proteins, lipid kinases, and GPCRs. LAS195319 effectively inhibits the infiltration of neutrophils and eosinophils, making it a valuable tool for research into respiratory diseases, including asthma and chronic obstructive pulmonary disease (COPD). -
PI3Kγ Inhibitor
SH-273 is a potent dual-function compound that acts as a selective inhibitor of PI3Kγ with an IC50 of 7 nM while also stimulating STING function with an EC50 of 100 nM. This unique profile makes SH-273 a valuable tool for investigating signaling pathways involved in pancreatic cancer. Researchers can utilize SH-273 to explore the therapeutic potential of targeting PI3Kγ and enhancing STING-mediated immune responses in cancer models. -
COX-2/PI3K Inhibitor
COX-2/PI3K-IN-2 is a potent inhibitor targeting both COX-2 and PI3K pathways, exhibiting an IC50 value of 2.78 nM for PI3K and a Ki value of 3.02 nM for COX-2. This compound demonstrates significant anti-inflammatory and anti-cancer activities, making it valuable for research in oncology and inflammatory disease studies. Its dual-target mechanism provides insights into the therapeutic potential of modulating these critical pathways. -
PI3K-δ/PI3K-γ inhibitor
IPI-145, also known as INK-1197, is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities. -
AKT inhibitor
TIC10 inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. -
PDK1 Inhibitor
GSK 2334470 is a potent 3-phosphoinositide-dependent protein kinase (PDK1) inhibitor (IC50 ~ 10 nM).
