pi 2

PI5P4Ks-IN-2 is an inhibitor of the phosphatidylinositol 5-phosphate 4-kinase PI5P4Kγ. Targeting the PI5P4K isoforms, PI5P4Ks-IN-2 inhibited PI5P4Kα, PI5P4Kβ, PI5P4Kγ, and PI5P4Kγ+, with IC50 values of <4.3, <4.6, 6.2, and 0.32, respectively.

PI3K Akt mTOR-IN-2 is a potent PI3K AKT mTOR inhibitor with anticancer effects and selectivity for MDA-MB-231 cells (IC50 2.29 μM). It induces cell cycle arrest and apoptosis in cancer cells.

Hydroxyzine dihydrochloride-d10 is a deuterated compound of Hydroxyzine dihydrochloride.

PI3K mTOR Inhibitor-2 is a potent pan inhibitor of PI3K and mTOR with IC50s of 3.4, 34, 16.1, and 4.7 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, and mTOR, respectively. PI3K mTOR Inhibitor-2 demonstrates antitumor activity.

PI3-Kinase α Inhibitor 2 (hydrochloride) is a PI3-Kinase α inhibitor.

Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3' hydroxyl position of PIs to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits, whereas PI3Kγ is a class 1B PI3K composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit. PI3Kα inhibitor 2 is a selective inhibitor of PI3Kα with IC50 values of 2, 16, 660, and 220 nM for the α, β, γ, and 2Cβ isoforms, respectively. It inhibits PKA, KDR, PKCα, and cyclin E/Cdk2 significantly less effectively (IC50 = 91, 3.4, 466, and 28 μM, respectively). PI3Kα inhibitor 2 inhibits A375 melanoma cell proliferation with an IC50 value of 580 nM.

PI3Kδ γ-IN-2 is a potent, orally bioavailable dual inhibitor of PI3Kδ (IC50: 1 nM) and PI3Kγ (IC50: 4.3 nM), with potential for use in anti-B-cell malignancy studies.

PI3K/AKT-IN-2, a dual inhibitor of PI3K and AKT, prevents the epithelial-mesenchymal transition (EMT) and promotes apoptosis. Additionally, it impedes tubulin polymerization.

MEK PI3K-IN-2 (compound 6s), a potent inhibitor of both MEK and PI3K, demonstrates IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), effectively reducing pAKT and pERK1 2 levels and exhibiting anti-proliferative activity against various tumor cell lines [1].

Bimiralisib (PI3K-IN-2) is an orally bioavailable pan inhibitor of PI3K and inhibitor of the mTOR, with potential antineoplastic activity. PI3K-IN-2 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy.

PI3K HDAC-IN-2 is a potent dual PI3K HDAC inhibitor with IC50 values of 226 nM for PI3Kα, 279 nM for PI3Kβ, 467 nM for PI3Kγ, 29 nM for PI3Kδ, and 1.3 nM for HDAC1. PI3K HDAC-IN-2 is selective for PI3Kδ and class I and IIb HDACs, exhibiting significant anticancer effects.

PI3KC2α-IN-1 is a potent inhibitor of PI3KC2α with an IC50 value of 95 nM, interacting with the ATP binding site of PI3KC2α. It impairs the kinetics of endocytosis and membrane remodelling and can be used to study thrombosis, diabetes, and cancer.

PI3K-IN-2 are orally active PI3Kβ/δ inhibitors with IC50 values of 7.1 nM, 8.6 nM, and higher selectivity than PI3Kσ (IC50: 13 nM) and PI3Kγ (IC50: 190 nM), respectively.

COX-2 PI3K-IN-2 (compound 5f) possesses anti-inflammatory and anti-cancer properties, functioning as a selective inhibitor of COX-2 (Ki = 3.02 nM) and a potent inhibitor of PI3K (IC50 = 2.78 nM) [1].

PI3KC2α-IN-3 is a highly selective and potent PI3KC2α inhibitor with an IC50 value of 126 nM. PI3KC2α-IN-3 interacts with the ATP binding site of PI3KC2α and impairs endocytic membrane kinetics and membrane remodelling. PI3KC2α-IN-3 can be used to study thrombosis, diabetes and cancer.

Linperlisib (PI3Kδ-IN-2) is a potent and selective inhibitor of PI3Kδ

PI5P4K-β-IN-2 (compound d5) is a potent inhibitor of the PI5P4K-β enzyme with an IC50 value of 0.35 μM and exhibits antitumor activity.

COX-2 PI3K-IN-1 (compound 5d) is a potent inhibitor of PI3K with an IC50 of 1.14 nM and selectively inhibits COX-2 with a Ki of 3.24 nM.

PI3K VEGFR2-IN-1 is a potent dual inhibitor targeting PI3K (IC50: 2.21 μM) and VEGFR2 (IC50: 68 μM), which induces apoptosis and is utilized in cancer research [1].

PI3KC2α-IN-2 is a selective and potent PI3KC2α inhibitor with an IC50 value of 121 nM that interacts with the ATP binding site of PI3KC2α. PI3KC2α-IN-2 can be used to study thrombosis, diabetes and cancer.

PI-1840（IC50 = 27 nM）is a reversible and selective chymotrypsin-like (CT-L) inhibitor, with little proteasome proteolytic effects on trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L).

AC-55541 (AOB2796) is a novel PAR2 agonist; activated PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2+) mobilization assays, with potencies ranging from 200 to 1000 nM.

PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of PI3K family members (IC50s: 2/3/3/15/30/23 nM for p110α/β/δ/γ, mTOR, and DNA-PK).

PI3Kγ inhibitor 2 is an orally bioavailable inhibitor of PI3Kγ(Ki of 4 nM).

Tipranavir is a protease inhibitor that inhibits HIV-1 resistant to more than 1 protease inhibitor .Tipranavir effectively inhibits HIV-1 protease enzyme activity and dimerisation and has potent activity against multiple protease inhibitor (PI) HIV-1 isolates (IC50 of 66-410 nM). Tipranavir inhibits SARS-CoV-2 3CLpro activity.

LY367385 hydrochloride is a potent and selective mGluR1a antagonist with an IC50 value of 8.8 μM for inhibiting quisqualate-induced phosphoinositide (PI) hydrolysis, showing significantly higher selectivity compared to its >100 μM IC50 value for mGlu5a. This compound exhibits neuroprotective, anticonvulsant, and antiepileptic effects [1] [2].

MHY219 is a novel HDAC inhibitor. MHY219 induces apoptosis via up-regulation of androgen receptor expression in human prostate cancer cells. MHY219 was shown to enhance the cytotoxicity on DU145 cells (IC50, 0.36 μM) when compared with LNCaP (IC50, 0.97 μM) and PC3 cells (IC50, 5.12 μM). MHY219 showed a potent inhibition of total HDAC activity when compared with SAHA. MHY219 increased histone H3 hyperacetylation and reduced the expression of class I HDACs (1, 2 and 3) in prostate cancer cells. MHY219 effectively increased the sub-G1 fraction of cells through p21 and p27 dependent pathways in DU145 cells. MHY219 significantly induced a G2/M phase arrest in DU145 and PC3 cells and arrested the cell cycle at G0/G1 phase in LNCaP cells. Furthermore, MHY219 effectively increased apoptosis in DU145 and LNCaP cells, but not PC3 cells, according to Annexin V/PI staining and Western blot analysis. These results indicate that MHY219 is a potent HDAC inhibitor that targets regulating mu......

Phosphatidylinositol-(4,5)-P2(1,2-dipalmitoyl), a synthetic analog of natural phosphatidylinositol (PtdIns) with C16:0 fatty acids at the sn-1 and sn-2 positions, maintains the inositol and diacylglycerol (DAG) stereochemistry of its natural counterpart. Although phosphatidylinositol phosphates constitute a minor fraction of total membrane phospholipids, they are pivotal in initiating and propagating cellular signals. This compound mirrors the activity of the natural phosphatidylinositol produced by PtdIns-4-phosphate 5-kinase's action on PtdIns-(4)-P1. Its hydrolysis by phosphoinositide (PI)-specific phospholipase C yields inositol triphosphate (IP3) and DAG, crucial secondary messengers in a complex signal transduction pathway.

The phosphatidylinositol (PtdIns) phosphates represent a small percentage of total membrane phospholipids. However, they play a critical role in the generation and transmission of cellular signals. PtdIns-(1,2-dioctanoyl) is a synthetic analog of natural phosphatidylinositol (PtdIns) containing C8:0 fatty acids at the sn-1 and sn-2 positions. The compound features the same inositol and diacyl glycerol (DAG) stereochemistry as that of the natural compound. The short fatty acid chains of this analog, compared to naturally-occurring PtdIns, gives it different physical properties including high solubility in aqueous media. PtdIns are phosphorylated to mono- (PtdIns-P; PIP), di- (PtdIns-P2; PIP2), and triphosphates (PtdIns-P3; PIP3). Hydrolysis of PtdIns-(4,5)-P2 by phosphoinositide (PI)-specific phospholipase C generates inositol triphosphate (IP3) and DAG which are key second messengers in an intricate biochemical signal transduction cascade.

PI-55 (6-(2-hydroxy-3-methylbenzylamino)purine) is a cytokinin receptor inhibitor that exhibits structural similarity to 6-benzylaminopurine (BAP). It competitively inhibits BAP binding on the specific Arabidopsis receptors CRE1 AHK4 and AHK3. Furthermore, PI-55 effectively suppresses cytokinins-induced haustorium formation and enhances parasite aggressiveness [1].

The phosphatidylinositol (PtdIns) phosphates represent a small percentage of total membrane phospholipids. However, they play a critical role in the generation and transmission of cellular signals. PtdIns-(3,4,5)-P3, also known as PIP3, is resistant to cleavage by PI-specific phospholipase C (PLC). Thus, it is likely to function in signal transduction as a modulator in its own right, rather than as a source of inositol tetraphosphates. PIP3 can serve as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking. PtdIns-(3,4,5)-P3 (1,2-dihexanoyl) is a synthetic analog of natural PIP3 with C6:0 fatty acids at the sn-1 and sn-2 positions. The compound features the same inositol and diacylglycerol (DAG) stereochemistry as that of the natural compound. The short fatty acid chains of this analog give it different physical properties from naturally-occurring PIP3, including higher solubility in aqueous media.

The phosphatidylinositol (PtdIns) phosphates represent a small percentage of total membrane phospholipids. However, they play a critical role in the generation and transmission of cellular signals. PtdIns-(3)-P1 (1,2-dioctanoyl) is a synthetic analog of natural PtdIns featuring C8:0 fatty acids at the sn-1 and sn-2 positions. The compound features the same inositol and DAG stereochemistry as the natural compound. PtdIns-(3)-P1 can be phosphorylated to di- (PtdIns-P2; PIP2) and triphosphates (PtdIns-P3; PIP3) by phosphatidyl inositol (PI)-specific kinases.

The phosphatidylinositol (PtdIns) phosphates represent a small percentage of total membrane phospholipids. However, they play a critical role in the generation and transmission of cellular signals. PtdIns-(4)-P1 (1,2-dioctanoyl) is a synthetic analog of natural phosphatidylinositol (PtdIns) featuring C8:0 fatty acids at the sn-1 and sn-2 positions. The compound contains the same inositol and diacylglycerol (DAG) stereochemistry as the natural compound. PtdIns-(4)-P1 can be phosphorylated to di- (PtdIns-P2; PIP2) and triphosphates (PtdIns-P3; PIP3). Hydrolysis of PtdIns-(4,5)-P2 by phosphoinositide (PI)-specific phospholipase C generates inositol triphosphate (IP3) and DAG which are key second messengers in an intricate biochemical signal transduction cascade.

TPC2-A1-P is a potent, membrane-permeable agonist of the two-pore channel 2 (TPC2), exhibiting an EC50 of 10.5 μM. It exerts its effects by mimicking the physiological actions of PI(3,5)P2, and demonstrates greater efficacy in inducing Na2+ mobilization from TPC2 compared to TPC-A1-N. This compound serves as a valuable tool for probing various functions of TPC2 channels in intact cells[1][2][3].

(Rac)-Z-Phe-Phe-FMK (Cathepsin L-IN-2) is a cathepsin L inhibitor that inhibits the tendency of β-amyloid to induce apoptotic changes .

PI-103 Hydrochloride is a potent dual inhibitor of PI3K and mTOR, demonstrating inhibitory IC50 values of 8 nM for p110α, 88 nM for p110β, 48 nM for p110δ, 150 nM for p110γ, 20 nM for mTORC1, and 83 nM for mTORC2, respectively. Additionally, it inhibits DNA-PK with an IC50 of 2 nM and induces autophagy [1] [2] [3] [4].

1,2,3-Triundecanoyl glycerol is a triacylglycerol that contains undecanoic acid at thesn-1,sn-2, andsn-3 positions. Dietary administration of a 7:3 (w/w) mixture of 1,2,3-triundecanoyl glycerol and corn oil prevents fasting-induced decreases in plasma glucose, alanine, and insulin levels, as well as the ratio of insulin to glucagon, in rats compared with dietary administration of corn oil alone.1 1.Pi-Sunyer, F.X., Conway, J.M., Lavau, M., et al.Glucagon, insulin, and gluconeogenesis in fasted odd carbon fatty acid-enriched ratsAm. J. Physiol.231(2)366-369(1976)

Hydroxyzine dihydrochloride-d4 is a deuterated compound of Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride has a CAS number of 2192-20-3. Hydroxyzine hydrochloride is a histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.

Hydroxyzine D4 is a deuterium-labeled variation of Hydroxyzine, a chemical compound known for its anticholinergic, anxiolytic, and analgesic properties. It is classified as a heterocyclic histamine H1-receptor antagonist.

Hydroxyzine (Hydroxyzine free base) is an antagonist of histamine H1-receptor.

Hydroxyzine dihydrochloride (Hydroxyzine 2HCl) is a histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.

Hydroxyzine dihydrochloride-d8 is a deuterated compound of Hydroxyzine dihydrochloride.

Hydroxyzine D8, a deuterium-labeled version of Hydroxyzine, acts as a histamine H1-receptor antagonist.