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Xanomeline oxalate (LY246708 oxalate) is a potent and selective muscarinic receptor agonist (SMRA) and stimulates phosphoinositide hydrolysis in vivo. Xanomeline oxalate can be used for the research of Alzheimer’s disease .
LY367385 is a highly selective and potent mGluR1a antagonist. LY367385 has an IC50 of 8.8 μM for inhibiting of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with >100 μM for mGlu5a. LY367385 has neuroprotective, anticonvulsant and antiepileptic effects .
LY367385 hydrochloride is a highly selective and potent mGluR1a antagonist. LY367385 hydrochloride has an IC50 of 8.8 μM for inhibiting of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with >100 μM for mGlu5a. LY367385 hydrochloride has neuroprotective, anticonvulsant and antiepileptic effects .
(Rac)-3-Hydroxyphenylglycine (3HPG) is a racemic mixture of (S)-3-hydroxyphenylglycine and (R)-3-hydroxyphenylglycine. (S)-3-Hydroxyphenylglycine is a potent and selective mGluR1 agonist .
Xanomeline (oxalate) (Standard) is the analytical standard of Xanomeline (oxalate). This product is intended for research and analytical applications. Xanomeline oxalate (LY246708 oxalate) is a potent and selective muscarinic receptor agonist (SMRA) and stimulates phosphoinositide hydrolysis in vivo. Xanomeline oxalate can be used for the research of Alzheimer’s disease .
α-Methylserotonin is a potent and selective agonist of 5-HT2 receptor. α-Methylserotonin is an analogue of serotonin formed in vivo from α-methyltryptophan. α-Methylserotonin mediates the lymphatic smooth muscle contraction and prevents the up-regulation of serotonin-receptor-mediated phosphoinositide hydrolysis .
TCL1(10-24) is a encompassing the betaA strand of human TCL1. TCL1(10-24) is a Akt inhibitor. TCL1(10-24) interacts with the Akt PH domain prevented phosphoinositide binding and hence inhibits membrane translocation and activation of Akt. TCL1(10-24) inhibits cellular proliferation and anti-apoptosis. TCL1(10-24) has tumor growth in vivo .
L 363851 is a Neurokinin 2 receptor agonist, and induces the contractile response of tracheal smooth muscle devoid of epithelium (IC50 of 3.2 nM) and phosphoinositide hydrolysis (IC50 of 36 μM).
18:1-6:0 DNP-C11 BODIPY 505/515 TG is a fluorescently-labeled triglyceride that can be used to study the effects of phosphoinositides (Ex/Em = 495/503 nm) .
bpV(bipy) hydrate is the inhibitor for phosphoinositide 3-phosphatase (PTEN) and protein tyrosine phosphatases (PTP-β and PTP-1B) with IC50s of 18, 60.3, and 164 nM, respectively .
Deramciclane fumarate is an antagonist of 5-HT Receptor. Deramciclane fumarate is an inverse agonist of 5-HT2C Receptor with an IC50 of 168 nM. Deramciclane fumarate also decreases basal phosphoinositide hydrolysis .
LY456236 is a selective, non-competitive and orally active mGlu1 receptor antagonist that inhibits phosphoinositide hydrolysis with an IC50 of 0.145 μM. LY456236 also inhibits EGFR with an IC50 of 0.91 μM .
MK-212 (CPP) monohydrochloride is a centrally acting 5-HT1C/5-HT2 agonist. MK-212 monohydrochloride can stimulate phosphoinositide hydrolysis in cerebral cortex .
(±)-LY367385 is the racemate of LY367385. LY367385 is a highly potent and selective mGluR1a antagonist. LY367385 has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis，compared with > 100 μM for mGlu5a .
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 .
Phosphatidylinositols, soya, sodium salts is a mixture of phosphatidylinositols. Phosphoinositides are lipids involved in the vesicular transport of proteins and lipids between the different compartments of eukaryotic cells. They act by recruiting and/or activating effector proteins and thus are involved in regulating various cellular functions, such as vesicular budding, membrane fusion and cytoskeleton dynamics .
UNC3230 is a potent, selective and ATP-competitive PIP5K1C inhibitor with an IC50 of ~41 nM. UNC3230 also inhibits PIP4K2C and does not inhibit any of the other lipid kinases that regulate phosphoinositide levels. UNC3230 has antinociceptive and anticancer effects .
PI3Kα-IN-19 (Compound 1) is a PI3Kα inhibitor with a targeted binding site at the p110α catalytic subunit. PI3Kα is one of the most common dysregulated kinases used in cancer research .
α-Methylserotonin maleate is a potent and selective agonist of 5-HT2 receptor. α-Methylserotonin maleate is an analogue of serotonin formed in vivo from α-Methyltryptophan. α-Methylserotonin maleate mediates the lymphatic smooth muscle contraction and prevents the up-regulation of serotonin-receptor-mediated phosphoinositide hydrolysis .
A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC50s for A-71623 are 3.7 nM in guinea pig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively .
MPEP Hydrochloride is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP Hydrochloride has anxiolytic-or antidepressant-like effects . MPEP (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
MPEP is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP has anxiolytic-or antidepressant-like effects . MPEP is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
MK-212 (monohydrochloride) (Standard) is the analytical standard of MK-212 (monohydrochloride). This product is intended for research and analytical applications. MK-212 (CPP) monohydrochloride is a centrally acting 5-HT1C/5-HT2 agonist. MK-212 monohydrochloride can stimulate phosphoinositide hydrolysis in cerebral cortex .
D-myo-Inositol 1,4,5-trisphosphate tripotassium, a second messenger, elicits Ca 2+ mobilization. D-myo-Inositol 1,4,5-trisphosphate tripotassium inhibits the binding of phosphoinositide-specific phospholipase C-delta 1 (PLC-delta 1) to bilayer membranes composed of phosphatidylcholine (PC) and phosphatidylinositol 4,5-bisphosphate (PIP2) .
Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally activeendothelin A receptor (ETA) antagonist with an IC50 of 1.4 nM and a Ki of 0.43 nM. Sitaxsentan sodium exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan sodium inhibits ET-1-induced phosphoinositide turnover. Sitaxsentan sodium can significantly alleviate pulmonary arterial hypertension (PAH) symptoms. Sitaxsentan sodium can be used for the study of PAH .
MPEP (Hydrochloride) (Standard) is the analytical standard of MPEP (Hydrochloride). This product is intended for research and analytical applications. MPEP Hydrochloride is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP Hydrochloride has anxiolytic-or antidepressant-like effects . MPEP (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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 .
A-70874 is a tyrosine-free tetrapeptide analog of cholecystokinin (30-33) (CCK-4). A-70874 is an agonist that stimulates pancreatic amylase release and a partial agonist that stimulates pancreatic phosphoinositide decomposition. A-70874 has an IC50 of 4.9 nM for the guinea pig pancreatic CCK receptor. Cholecystokinin (CCK) receptors are divided into CCK-A (digestive tract) and CCK-B (brain). A-70874 has an affinity of 1.6 μM for the CCK-B/gastrin receptor .
AMP-PNP (Adenylyl imidodiphosphate) lithium hydrate is a non-hydrolyzable ATP analog. AMP-PNP lithium hydrate binds to ATP binding sites competely but is not hydrolyzed by enzymes, providing stable experimental conditions for studying ATP-dependent processes. AMP-PNP lithium hydrate can also be used to study enzyme activity, kinase regulation, DNA/RNA metabolism, ion channel function, and protein complex assembly .
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 .
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 .
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 .
R-PSOP is highly potent and selective nonpeptidic NMUR2 antagonist. R-PSOP binds to NMUR2 with the Kis of 52 and 32 nM for the human and rat NMUR2, respectively. R-PSOP shows moderate CNS penetration. R-PSOP can be used for the research of the eating disorders, obesity, pain, and stress-related disorders .
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 .
MTX-211 (Mol 211) is a dual inhibitor of EGFR and PI3K with IC50 values of ＜100 nM. MTX-211 can be used for the research of cancer and other diseases .
α-Methylserotonin maleate is a potent and selective agonist of 5-HT2 receptor. α-Methylserotonin maleate is an analogue of serotonin formed in vivo from α-Methyltryptophan. α-Methylserotonin maleate mediates the lymphatic smooth muscle contraction and prevents the up-regulation of serotonin-receptor-mediated phosphoinositide hydrolysis .
AMP-PNP (Adenylyl imidodiphosphate) lithium hydrate is a non-hydrolyzable ATP analog. AMP-PNP lithium hydrate binds to ATP binding sites competely but is not hydrolyzed by enzymes, providing stable experimental conditions for studying ATP-dependent processes. AMP-PNP lithium hydrate can also be used to study enzyme activity, kinase regulation, DNA/RNA metabolism, ion channel function, and protein complex assembly .
IRS1-derived peptide is a biological active peptide. (This is a peptide fragment (979-989) of the insulin receptor substrate-1 containing the sequence motif YMXM known to bind to the two domains of SH2 on the 85kDa subunit of phosphoinositide 3-kinase.)
A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC50s for A-71623 are 3.7 nM in guinea pig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively .
TCL1(10-24) is a encompassing the betaA strand of human TCL1. TCL1(10-24) is a Akt inhibitor. TCL1(10-24) interacts with the Akt PH domain prevented phosphoinositide binding and hence inhibits membrane translocation and activation of Akt. TCL1(10-24) inhibits cellular proliferation and anti-apoptosis. TCL1(10-24) has tumor growth in vivo .
18:1-6:0 DNP-C11 BODIPY 505/515 TG is a fluorescently-labeled triglyceride that can be used to study the effects of phosphoinositides (Ex/Em = 495/503 nm) .
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 .
PDPK1 protein is the core kinase of the AGC family and can phosphorylate and activate various downstream kinases, including PKB/AKT1, RPS6KB1, PRKACA, PRKCD, SGK1, PAK1 and PKN. It transduces insulin signals and regulates cellular processes such as proliferation, survival, and nutrient absorption. PDPK1 Protein, Human (sf9, His) is the recombinant human-derived PDPK1 protein, expressed by sf9 insect cells , with N-8*His 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.
PDPK1 protein is the core kinase of the AGC family and can phosphorylate and activate various downstream kinases, including PKB/AKT1, RPS6KB1, PRKACA, PRKCD, SGK1, PAK1 and PKN. It transduces insulin signals and regulates cellular processes such as proliferation, survival, and nutrient absorption. PDPK1 Protein, Human (sf9) is the recombinant human-derived PDPK1 protein, expressed by sf9 insect cells , with tag free.
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.
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