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Vulolisib is a potent and orally active phosphatidylinositol 3-kinase(PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. Antiproliferative and antineoplastic activity .
PI3K/mTOR Inhibitor-13 sodium is an orally active dual inhibitor of phosphoinositol 3-kinase(PI3K) and mTORkinase. PI3K/mTOR Inhibitor-13 sodium has potential applications in sexual diseases, solid tumor and idiopathic pulmonary fibrosis (IPF) .
Dezapelisib (NCB040093) is a potent inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ). Dezapelisib is a promising research strategy for select R/R B-cell lymphomas .
PI3K/mTOR Inhibitor-13 is an orally active dual inhibitor of phosphoinositol 3-kinase(PI3K) and mTORkinase. PI3K/mTOR Inhibitor-13 has potential applications in sexual diseases, solid tumor and idiopathic pulmonary fibrosis (IPF) .
PI3K-IN-60 (Compound 34) is a highly selective phosphatidylinositol 3-kinase gamma (PI3Kγ) inhibitor. PI3K-IN-60 is promising for research of autoimmune diseases (e.g., multiple sclerosis) and cancers (e.g., breast cancer, pancreatic ductal adenocarcinoma) .
Demethoxyviridiol is a mycotoxin originally isolated from N. hinnuleum. Demethoxyviridiol induces lethality in day-old cockerels (LD50=4.2 mg/kg). Demethoxyviridiol is also an inhibitor of phosphatidylinositol 3-kinase (PI3K).
Phosphatidylinositol 4,5-bisphosphate (L-alpha-Phosphatidylinositol-4,5-bisphosphate), a phospholipid component of cell membranes, is a substrate for phospholipase C (PLC) and phosphoinositide 3-kinase (PI3K) and as a primary messenger .
PI3K-IN-6 (compound 20a) is an oral active and highly selective phosphoinositide 3-kinase (PI3K) β/δ inhibitor, with IC50 values of 7.8 nM/5.3 nM for PI3K β/δ, respectively. PI3K-IN-6 (compound 20a) has potential top treat phosphatase and tensin homolog (PTEN) feficient tumors .
WJD008 is a potent dual phosphatidylinositol 3-kinase(PI3K)/mammalian target of rapamycin (mTOR) inhibitor with antiproliferative and anticlonogenic activity in tumor cells and transformed cells with PIK3CA mutant. WJD008 inhibits kinase activity of PI3K α and mTOR and abrogates insulin-like growth factor-I-activated PI3K-Akt-mTOR signaling cascade. WJD008 is promising for research of cancers .
PI3K-IN-56 (Compound 1) is an orally active, potent and selective irreversible inhibitor of phosphoinositide 3-kinase(PI3K).PI3K-IN-56 irreversibly blocks the phosphatidylinositol-3,4,5-triphosphate (PIP3) production and downstream AKT signaling pathway. PI3K-IN-56 is promising for research of PI3Kα-driven cancers, such as breast and ovarian cancers .
OMS14 is exhibits inhibitory activity for phosphoinositide 3-kinase γ (PI3Kγ) and PIK3CD/PIK3R1, which inhibits 19% PI3Kγ and 65% PIK3CD/PIK3R1 activity at 100 μM. OMS14 exhibits anticancer efficacy in various cancer cells .
FD223 is a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. FD223 displays high potency (IC50=1 nM) and good selectivity over other isoforms (IC50s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cell cycle. FD223 has potential for the research of leukemia such as AML .
17β-Hydroxywortmannin (Wortmannin-17β-ol) is an orally active inhibitor for phosphatidylinositol-3-kinase(PI-3-kinase) with an IC50 of 0.5 nM, suppresses the osteoclast resorption with an IC50 of 10 nM . 17β-Hydroxywortmannin exhibits antitumor activity .
T7 peptide is an endothelial cell-specific inhibitor. T7 peptide interacts with αVβ3 integrin to inhibit the FAK, PI3-kinase, PKB/Akt, and mTOR signaling pathways in endothelial cells, ultimately suppressing protein synthesis and inducing apoptosis .
PI3Kδ-IN-21 (Compound 31) is a selective inhibitor for phosphoinositide 3-kinases δ (PI3Kδ), with an IC50 of 13.6 nM. PI3Kδ-IN-21 inhibits proliferation and differentation of T cells through PI3K/AKT/mTOR signaling pathway. PI3Kδ-IN-21 exhibits good pharmacokinetic characters in rat model, and attenuates the experimental autoimmune encephalomyelitis in myelin oligodendrocyte glycoprotein (MOG)-induced EAE model .
GNE-493 is a potent, selective, and orally available dual pan-PI3-kinase/mTOR inhibitor with IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.
AIM-100 is a potent and selective Ack1 inhibitor with an IC50 of 21.58 nM. AIM-100 also inhibits Tyr 267 phosphorylation. AIM-100 does not inhibits other kinases including PI3-kinase and AKT subfamily members. AIM-100 has an anticancer effect .
PI(3,4)P2 (18:1) ammonium salt is a phosphatidylinositol 3 kinase(PI3K) activator. PI(3,4)P2 (18:1) ammonium salt is a polyphosphorylated phosphatidylinositol that promotes the activation of AKT (protein kinase B) by activating PI3K, which affects cell metabolism, growth and survival. PI(3,4)P2 (18:1) ammonium salt is also involved in regulating dynamic changes in the cytoskeleton, affecting cell morphology and movement. PI(3,4)P2 (18:1) ammonium salt can be used in research on the development of cancer, diabetes and cardiovascular disease .
Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a?Ki?of 17 nM for mTOR.
Apitolisib (Standard) is the analytical standard of Apitolisib. This product is intended for research and analytical applications. Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a Ki of 17 nM for mTOR.
SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells . SPP-86 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
RV-1729 is an inhibitor of the phosphatidylinositol 3-kinase-δ (PI3Kδ). RV-1729 identifies inhibition of the PI3K isotype by quantifying the release of phosphatidylinositol 3,4, 5-triphosphate (PIP3) (IC50=12 nM), showing twice the selectivity for PI3Kδ relative to PI3Kγ. RV-1729 is also 16 times more selective to PI3Kα. RV-1729 regulates immune and inflammatory responses by inhibiting PI3Kδ. RV-1729 can be used in studies of asthma and chronic obstructive pulmonary disease (COPD) .
MDVN1003 is a Bruton's tyrosine kinase (BTK) and phosphatidylinositol-3-kinase delta (PI3Kδ) dual inhibitor which prevents the activation of B cells and inhibits the phosphorylation of protein kinase B (AKT) and extracellular signal-regulated kinase 1/2 (ERK 1/2). MDVN1003 can be used for non-Hodgkin’s lymphoma (NHL) research .
Human IL10RA mRNA encodes the human interleukin 10 receptor subunit alpha (IL10RA) protein, a receptor for interleukin 10. IL10RA been shown to mediate the immunosuppressive signal of interleukin 10, and thus inhibits the synthesis of proinflammatory cytokines. It is also reported to promote survival of progenitor myeloid cells through the insulin receptor substrate-2/PI3-kinase/AKT pathway.
Skimmianine is an orally active furoquiniline alkaloid present mainly in the Rutaceae family. Skimmianine has analgesic, antispastic, sedative, and anti-inflammatory properties. Skimmianine inhibits acetylcholinesterase (AChE) (IC50 = 8.6 μg/mL). Skimmianine exhibits cytotoxicity against a variety of cancer cell lines and genotoxicity. Skimmianine has antioxidant and anti-inflammatory effects on ischemia-reperfusion (IR) injury. Skimmianine exerts anti-inflammatory effects through activation of the phosphatidylinositol-3-kinase (PI3K)-protein kinase B (AKT) pathway. Skimmianine is neuroprotective by targeting the NF-κB activation pathway to prevent neuroinflammation. Skimmianine inhibits the release of histamine, intracellular Ca 2+ signaling and protein kinase C signaling .
Skimmianine (Standard) is the analytical standard of Skimmianine. This product is intended for research and analytical applications. Skimmianine is an orally active furoquiniline alkaloid present mainly in the Rutaceae family. Skimmianine has analgesic, antispastic, sedative, and anti-inflammatory properties. Skimmianine inhibits acetylcholinesterase (AChE) (IC50 = 8.6 μg/mL). Skimmianine exhibits cytotoxicity against a variety of cancer cell lines and genotoxicity. Skimmianine has antioxidant and anti-inflammatory effects on ischemia-reperfusion (IR) injury. Skimmianine exerts anti-inflammatory effects through activation of the phosphatidylinositol-3-kinase (PI3K)-protein kinase B (AKT) pathway. Skimmianine is neuroprotective by targeting the NF-κB activation pathway to prevent neuroinflammation. Skimmianine inhibits the release of histamine, intracellular Ca 2+ signaling and protein kinase C signaling .
Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM .
PP487 is a dual inhibitor of tyrosine kinase/PI(3)Ks with IC50 values of 0.017 μM, 0.072 μM, 0.004 μM, 0.01 μM, 0.55 μM, 0.22 μM, and < 0.01 μM against DNA-PK, mTOR, Hck, Src, EGFR, EphB4, and PDGFR, respectively. PP487 can be used for cancer research .
MTX-241F is a selective small molecule inhibitor targeting EGFR and PI3 kinase family members. MTX-241F is able to penetrate the blood-brain barrier and control tumor growth over the long term. MTX-241F exhibits radiosensitizing activity in patient-derived DIPG neurospheres and may be used in the study of diffuse intrinsic pontine glioma (DIPG) .
PH11 is a novel focal adhesion kinase (FAK) inhibitor that rapidly induces apoptosis in TRAIL-resistant PANC-1 cells when combined with TRAIL, but has no effect on normal human fibroblasts. The study found that PH11 downregulates c-FLIP through inhibition of FAK and phosphatidylinositol-3-kinase (PI3K)/AKT pathways, thereby restoring the TRAIL apoptotic pathway, suggesting that this combination therapy may provide an attractive therapeutic strategy for the safe and effective treatment of pancreatic cancer. PH11 selectively inhibits c-FLIP expression by modulating upstream signaling pathways and may represent an innovative therapeutic strategy. Although further work is needed to fully elucidate the mechanism of PH11-induced TRAIL sensitization, we believe that our results will provide a new approach to target c-FLIP without the risk of interfering with caspase-8 processing, which could potentially lead to TRAIL resistance. This study also suggests a role for the FAK/AKT signaling pathway in regulating c-FLIP expression in TRAIL-induced apoptosis, and this understanding will provide important clues to control the resistance mechanism to optimize the potential of TRAIL-based pancreatic cancer treatment.
T7 peptide is an endothelial cell-specific inhibitor. T7 peptide interacts with αVβ3 integrin to inhibit the FAK, PI3-kinase, PKB/Akt, and mTOR signaling pathways in endothelial cells, ultimately suppressing protein synthesis and inducing apoptosis .
Skimmianine is an orally active furoquiniline alkaloid present mainly in the Rutaceae family. Skimmianine has analgesic, antispastic, sedative, and anti-inflammatory properties. Skimmianine inhibits acetylcholinesterase (AChE) (IC50 = 8.6 μg/mL). Skimmianine exhibits cytotoxicity against a variety of cancer cell lines and genotoxicity. Skimmianine has antioxidant and anti-inflammatory effects on ischemia-reperfusion (IR) injury. Skimmianine exerts anti-inflammatory effects through activation of the phosphatidylinositol-3-kinase (PI3K)-protein kinase B (AKT) pathway. Skimmianine is neuroprotective by targeting the NF-κB activation pathway to prevent neuroinflammation. Skimmianine inhibits the release of histamine, intracellular Ca 2+ signaling and protein kinase C signaling .
Phosphatidylinositol 4,5-bisphosphate (L-alpha-Phosphatidylinositol-4,5-bisphosphate), a phospholipid component of cell membranes, is a substrate for phospholipase C (PLC) and phosphoinositide 3-kinase (PI3K) and as a primary messenger .
Skimmianine (Standard) is the analytical standard of Skimmianine. This product is intended for research and analytical applications. Skimmianine is an orally active furoquiniline alkaloid present mainly in the Rutaceae family. Skimmianine has analgesic, antispastic, sedative, and anti-inflammatory properties. Skimmianine inhibits acetylcholinesterase (AChE) (IC50 = 8.6 μg/mL). Skimmianine exhibits cytotoxicity against a variety of cancer cell lines and genotoxicity. Skimmianine has antioxidant and anti-inflammatory effects on ischemia-reperfusion (IR) injury. Skimmianine exerts anti-inflammatory effects through activation of the phosphatidylinositol-3-kinase (PI3K)-protein kinase B (AKT) pathway. Skimmianine is neuroprotective by targeting the NF-κB activation pathway to prevent neuroinflammation. Skimmianine inhibits the release of histamine, intracellular Ca 2+ signaling and protein kinase C signaling .
PIK3R3 protein, through its SH2 domain, interacts with phosphorylated protein-tyrosine kinases, crucially regulating their kinase activity. During insulin stimulation, PIK3R3 binds to IRS-1. Operating as a heterodimer with a p110 catalytic subunit, it interacts with AXL, expanding its functional network. PIK3R3 Protein, Human (sf9, His, GST) is the recombinant human-derived PIK3R3 protein, expressed by sf9 insect cells , with N-8*His, N-GST labeled tag.
PIK3C3; Phosphatidylinositol 3-kinase catalytic subunit type 3; PI3-kinase type 3; PI3K type 3; PtdIns-3-kinase type 3; Phosphatidylinositol 3-kinase p100 subunit; Phosphoinositide-3-kinase class 3; hVps34
The PI3KC3 protein is the catalytic subunit of the PI3K complex and mediates the formation of phosphatidylinositol 3-phosphate. PI3KC3-C1 initiates autophagosomes, whereas PI3KC3-C2 promotes autophagosome maturation and endocytosis. PK3C3 Protein, Human (sf9, His, GST) is the recombinant human-derived PK3C3 protein, expressed by sf9 insect cells , with N-8*His, N-GST labeled tag.
PIK3CA Protein, Human (Active, sf9, His, Strep) is the recombinant human-derived PIK3CA, expressed by sf9 insect cells , with Strep, His labeled tag. ,
PI3 Kinase p110 alpha/PIK3CA Antibody (YA3537) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to PI3 Kinase p110 alpha/PIK3CA.
PI3 Kinase p110 alpha/PIK3CA Antibody (YA5770) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to PI3 Kinase p110 alpha/PIK3CA.
Phospho-PI3 Kinase p85/p55 (Tyr467/Tyr199) Antibody is a Rabbit-derived and non-conjugated IgG polyclonal antibody, targeting to Phospho-PI3 Kinase p85/p55 (Tyr467/Tyr199).
PI(3,4)P2 (18:1) ammonium salt is a phosphatidylinositol 3 kinase(PI3K) activator. PI(3,4)P2 (18:1) ammonium salt is a polyphosphorylated phosphatidylinositol that promotes the activation of AKT (protein kinase B) by activating PI3K, which affects cell metabolism, growth and survival. PI(3,4)P2 (18:1) ammonium salt is also involved in regulating dynamic changes in the cytoskeleton, affecting cell morphology and movement. PI(3,4)P2 (18:1) ammonium salt can be used in research on the development of cancer, diabetes and cardiovascular disease .
Human IL10RA mRNA encodes the human interleukin 10 receptor subunit alpha (IL10RA) protein, a receptor for interleukin 10. IL10RA been shown to mediate the immunosuppressive signal of interleukin 10, and thus inhibits the synthesis of proinflammatory cytokines. It is also reported to promote survival of progenitor myeloid cells through the insulin receptor substrate-2/PI3-kinase/AKT pathway.
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