Shop By
Catalog No.
Product Name
Application
Product Information
Citations
-
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. -
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. -
GSK-3β Inhibitor
GSK-3β inhibitor 24 is a highly potent inhibitor of glycogen synthase kinase 3 beta (GSK-3β), exhibiting an IC50 of 0.22 nM. This compound effectively enhances GSK-3β phosphorylation at the Ser9 site in a dose-dependent manner, while reducing hyperphosphorylation of tau protein, specifically lowering p-tau-Ser396 levels. Additionally, GSK-3β inhibitor 24 promotes the upregulation of β-catenin and neurogenesis-related markers such as GAP43 and MAP-2, making it a valuable tool in Alzheimer's disease research and therapeutic studies. -
GSK-3α/β Selective Inhibitor
GSK-3α/β-IN-1 is a selective inhibitor of glycogen synthase kinase-3 alpha and beta (GSK-3α/β), demonstrating IC50 values of 0.265 μM for GSK-3α and 0.255 μM for GSK-3β. Additionally, GSK-3α/β-IN-1 exhibits PKA inhibition with an IC50 of 0.188 μM. This compound effectively reduces cell viability in several glioblastoma (GBM) cell lines, with IC50 values ranging from 3 to 6 μM over 72 hours, while displaying minimal toxicity to human astrocytes. GSK-3α/β-IN-1 also shows promising central nervous system activity in human blood-brain barrier models of GBM, supporting its potential as a therapeutic agent in cancer research. -
AKT/mTOR Inhibitor
19-epi-Scholaricine is a potent AKT/mTOR inhibitor, classified as an orally active indole alkaloid. This compound downregulates profibrotic and apoptotic proteins, such as HRAS, HSP90AA1, and KDR, while upregulating the cell cycle regulator CDK2. Furthermore, 19-epi-Scholaricine inhibits ROS production and reduces inflammatory mediator release, leading to decreased podocyte apoptosis, renal inflammation, and oxidative stress. It is a valuable tool for research into chronic glomerulonephritis and membranous nephropathy. -
mTOR Inhibitor
Rapamycin-d3 is a deuterium-labeled analog of Rapamycin, a highly potent and selective inhibitor of the mechanistic target of rapamycin (mTOR), exhibiting an IC50 of 0.1 nM in HEK293 cells. It functions by binding to FKBP12, leading to allosteric inhibition of mTORC1. This compound is notable for its roles in autophagy activation and immunosuppression, making it valuable for various research applications including cancer biology, metabolic disorders, and studies of cellular growth and proliferation. -
PI3K/mTOR Inhibitor
Dactolisib hydrochloride is a potent dual inhibitor of class I phosphoinositide 3-kinases (PI3K) and the mammalian target of rapamycin (mTOR), specifically targeting p110α, p110γ, p110δ, and p110β with IC50 values of 4 nM, 5 nM, 7 nM, 75 nM, and 20.7 nM, respectively. This compound effectively inhibits both mTORC1 and mTORC2, making it a valuable tool for studying the PI3K/mTOR signaling pathway. Its applications include cancer research, drug development, and exploring therapeutic strategies for various diseases associated with dysregulated PI3K/mTOR signaling. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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.
