PI3K

Phosphoinositide 3-kinases (PI3Ks) are lipid kinases that catalyze the phosphorylation of phosphatidylinositol 4,5-bisphosphate (PI(4,5)P₂) to generate the second messenger phosphatidylinositol (3,4,5)-trisphosphate (PI(3,4,5)P₃). The production of PI(3,4,5)P₃ facilitates the recruitment and activation of pleckstrin homology (PH) domain–containing proteins at the plasma membrane, thereby initiating downstream signaling cascades essential for cellular proliferation, survival, and migration.

PI3Ks are divided into three major classes, among which Class I PI3Ks are most prominently implicated in cancer biology. Class I enzymes comprise four distinct catalytic isoforms: PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ.

Class IA PI3Ks, the subclass most commonly associated with oncogenic signaling, function as heterodimeric lipid kinases composed of a catalytic p110 subunit (p110α, p110β, or p110δ, encoded by PIK3CA, PIK3CB, and PIK3CD, respectively) and a regulatory p85 subunit.

The PI3K signaling pathway plays a central role in diverse biological processes, including cell cycle progression, cellular growth, survival, actin cytoskeletal rearrangement, migration, and intracellular vesicular trafficking.

Frequently Asked Questions
What is PI3K?
Phosphoinositide 3-kinases (PI3Ks) are a family of lipid kinases that phosphorylate phosphatidylinositol lipids to regulate cell growth, survival, metabolism, and immune signaling. PI3K activation leads to downstream AKT and mTOR pathway signaling. Aberrant PI3K signaling is frequently observed in cancer due to PIK3CA mutations, PTEN loss, or receptor tyrosine kinase activation.
What are the different PI3K isoforms?
Class I PI3Ks include four catalytic isoforms: PI3Kα (PIK3CA) PI3Kβ (PIK3CB) PI3Kδ (PIK3CD) PI3Kγ (PIK3CG) PI3Kα and β are broadly expressed, while PI3Kδ and γ are enriched in leukocytes and play critical roles in immune regulation. Isoform selectivity is an important consideration in drug development due to toxicity and immune effects.
What are the major types of PI3K inhibitors?
PI3K inhibitors can be classified as: Pan-PI3K inhibitors Isoform-selective inhibitors (α, β, δ, γ) Dual PI3K/mTOR inhibitors Irreversible inhibitors Selectivity influences therapeutic window and toxicity profile.
How do PI3K inhibitors differ from mTOR inhibitors?
While PI3K inhibitors block upstream lipid kinase activity, mTOR inhibitors act downstream at the level of mTORC1 or mTORC2. Dual PI3K/mTOR inhibitors target both nodes of the pathway and may achieve broader pathway suppression.

Items 201-250 of 387

Page
per page
Set Descending Direction
Catalog No.
Product Name
Application
Product Information
Citations
  1. 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.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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.
  8. PI3K/mTOR Inhibitor

    FD274 is a potent dual inhibitor of PI3K and mTOR, exhibiting IC50 values of 0.65 nM for PI3Kα, 1.57 nM for PI3Kβ, 0.65 nM for PI3Kγ, 0.42 nM for PI3Kδ, and 2.03 nM for mTOR. This compound demonstrates significant anti-proliferative effects on acute myeloid leukemia (AML) cell lines, specifically HL-60 and MOLM-16, inducing G1 phase cell cycle arrest and promoting apoptosis. In vivo studies reveal dose-dependent inhibition of tumor growth in HL-60 xenograft models, making FD274 a valuable tool for research into acute myeloid leukemia therapies.
  9. PARP/PI3K Inhibitor

    PARP/PI3K-IN-1 is a potent inhibitor of both PARP and PI3K, exhibiting pIC50 values of 8.22 for PARP-1, 8.44 for PARP-2, and varying activity against PI3K isoforms with values of 8.25 for PI3Kα, 6.54 for PI3Kβ, 8.13 for PI3Kδ, and 6.08 for PI3Kγ. This compound demonstrates significant anticancer activity and is suitable for research applications targeting a variety of oncological disorders. Its dual inhibition may provide insights into therapeutic strategies for cancer treatment.
  10. PI3Kδ Inhibitor

    PI3Kδ-IN-16 is a highly selective inhibitor of the PI3Kδ isoform, displaying an impressive IC50 value of 0.9 nM. This compound exhibits significant anti-proliferative effects on SU-DHL-6 cells, leading to cell cycle arrest and the induction of apoptosis. PI3Kδ-IN-16 demonstrates substantial selectivity for PI3Kδ over other isoforms, with a kinase activity that is approximately 378-fold greater than PI3Kα, 412-fold greater than PI3Kβ, and 10-fold greater than PI3Kγ. It is a valuable tool for research into hematologic malignancies and the therapeutic targeting of PI3Kδ.
  11. PI3Kα/mTOR Inhibitor

    PWT-33597 free base is a dual inhibitor targeting PI3Kα and mTOR, effectively disrupting downstream signaling pathways associated with cell growth and metabolism. This compound induces apoptosis in tumor cells and demonstrates significant inhibitory effects on tumor proliferation. PWT-33597 free base is applicable in research focused on various tumors, including renal cell carcinoma, making it a valuable tool for cancer studies.
  12. PI3Kα/mTOR Inhibitor

    PWT-33597 is a potent dual inhibitor of PI3Kα and mTOR, effectively disrupting downstream signaling pathways associated with cell growth and survival. This reagent induces apoptosis in tumor cells and demonstrates significant anti-tumor activity. PWT-33597 is a valuable tool for research into various malignancies, including renal cell carcinoma, providing insights into tumor biology and therapeutic strategies.
  13. PI3Kα Inhibitor

    PI3Kα-IN-6 is a selective inhibitor of the phosphoinositide 3-kinase alpha (PI3Kα) pathway. This compound demonstrates significant anticancer activity by promoting the generation of reactive oxygen species (ROS), leading to a decrease in mitochondrial membrane potential (MMP) and subsequently inducing apoptosis in cancer cells. PI3Kα-IN-6 is valuable for research focused on cancer therapeutics and the exploration of PI3K signaling in cell survival and proliferation.
  14. PI3K Inhibitor

    Copanlisib dihydrochloride is a potent, selective pan-class I PI3K inhibitor that acts through ATP-competitive mechanisms. It exhibits remarkable inhibitory activity with IC50 values of 0.5 nM, 0.7 nM, 3.7 nM, and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ, and PI3Kγ, respectively, demonstrating over 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. This compound has been shown to possess significant antitumor activity, making it a valuable reagent for cancer research and therapeutic development focusing on the PI3K pathway.
  15. PI3Kα/β/δ Inhibitor

    BAY1082439 is a selective inhibitor of the PI3Kα, β, and δ isoforms, demonstrating oral bioavailability. This compound effectively inhibits both wild-type and mutated forms of PIK3CA, making it a valuable tool in cancer research. Notably, BAY1082439 has shown significant efficacy in suppressing the growth of Pten-null prostate cancer, highlighting its potential in therapeutic applications targeting specific tumors.
  16. PI3Kα Inhibitor

    PI3Kα-IN-9 is a selective inhibitor of PI3Kα, exhibiting an IC50 of 4.4 nM while demonstrating lesser potency against PI3Kγ, PI3Kδ, and PI3Kβ with IC50 values of 128, 146, and 153 nM, respectively. This compound is notable for its long-acting oral activity and ability to induce apoptosis alongside antiproliferative effects in cancer cells. PI3Kα-IN-9 serves as a valuable reagent for cancer research, particularly in studies focused on PI3K signaling pathways.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. PI3K/Akt Inhibitor, MAPK Inhibitor, NF-κB Inhibitor, Nrf2/ARE Activator

    JRN73958 is a potent inhibitor of the PI3K/Akt, MAPK, and NF-κB signaling pathways. This compound effectively reduces LPS/IFNγ-induced activation of these pathways, making it a valuable tool for investigating their roles in cancer biology, particularly in leukemia research. Additionally, JRN73958 acts as an Nrf2/ARE activator, further expanding its utility in studies related to oxidative stress and cell survival mechanisms.
  40. MAPK/PI3K Antagonist

    ST-162 is a dual antagonist of the MAPK and PI3K signaling pathways. It demonstrates significant antitumor activity and has been shown to enhance the efficacy of immune checkpoint inhibitors. This compound is suitable for cancer research, particularly in the study of melanoma and other malignancies.
  41. PI3K/PIKK Inhibitor

    PI3K/PIKK-IN-1 is a potent inhibitor of phosphoinositide 3-kinases (PI3K) and PI3-kinase-related kinases (PIKK). This compound is utilized in the development of antibody-drug conjugates (ADCs), making it valuable for therapeutic applications. It is particularly relevant in the research of various cancers, including breast cancer, multiple myeloma, Burkitt lymphoma, diffuse large B-cell lymphoma, and non-small cell lung cancer, aiding in the exploration of targeted cancer therapies.
  42. PI3Kδ/BET Inhibitor

    PI3Kδ/BET-IN-1 is a selective inhibitor targeting both PI3Kδ and the bromodomain BRD4-BD1. With an IC50 of 112 nM for PI3Kδ and 19 nM for BRD4-BD1, this compound demonstrates potent antiproliferative effects in diffuse large B-cell lymphoma (DLBCL) cells. Its dual inhibition mechanism makes it a valuable tool for research into cancer biology and therapeutic development.
  43. PI3Kα Inhibitor

    PI3Kα-IN-16 is a selective PI3Kα inhibitor with an IC50 value of 4.28 μM. It effectively suppresses PI3K-mediated colorectal cancer growth and migration, demonstrating its potential as a therapeutic agent. Additionally, PI3Kα-IN-16 inhibits the Wnt signaling pathway, making it a valuable tool for research in cancer biology and signaling pathways.
  44. PI3K Inhibitor

    ETP-45658 is a potent inhibitor of the phosphoinositide 3-kinase (PI3K) family, exhibiting IC50 values of 22.0 nM for PI3Kα, 39.8 nM for PI3Kδ, 129.0 nM for PI3Kβ, and 717.3 nM for PI3Kγ. Additionally, ETP-45658 demonstrates inhibitory effects on DNA-PK (IC50 = 70.6 nM) and mTOR (IC50 = 152.0 nM). This compound is valuable for cancer research, particularly in exploring the roles of PI3K signaling pathways in tumorigenesis and treatment resistance.
  45. PI3Kδ Inhibitor

    PI3Kδ-IN-27 is a selective inhibitor of PI3Kδ, exhibiting an IC50 value of 355.3 nM. This compound demonstrates notable antiviral activity against SARS-CoV-2, making it a valuable tool for studying viral infections, particularly COVID-19. Researchers can utilize PI3Kδ-IN-27 to explore pathways related to immune response and infection mechanisms.
  46. MEK/PI3K Inhibitor

    MEK/PI3K-IN-2 is a potent inhibitor targeting both MEK and PI3K pathways, exhibiting IC50 values of 352 nM for MEK1, 107 nM for PI3Kα, and 137 nM for PI3Kδ. This compound effectively reduces levels of phosphorylated AKT and ERK1/2, demonstrating significant anti-proliferative activity against various tumor cell lines. MEK/PI3K-IN-2 is valuable for research in cancer biology and therapeutic development aimed at disrupting these critical signaling pathways.
  47. MEK/PI3K Inhibitor

    MEK/PI3K-IN-1 is a potent inhibitor targeting MEK and PI3K pathways, exhibiting IC50 values of 124 nM for MEK1, 130 nM for PI3Kα, and 236 nM for PI3Kδ. This compound effectively reduces levels of phosphorylated AKT (pAKT) and ERK1/2 (pERK1/2), demonstrating significant anti-proliferative effects in various tumor cell lines. MEK/PI3K-IN-1 serves as a valuable tool for research in cancer therapeutics and signaling pathway analysis.
  48. 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.
  49. 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.
  50. 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.

Items 201-250 of 387

Page
per page
Set Descending Direction