pi 1

PI3Kα/mTOR-IN-1 is a potent dual inhibitor of PI3Kα/mTOR. PI3Kα/mTOR-IN-1 shows an IC50 of 7 nM for PI3Kα in a cell assay, and Kis of 12.5 nM and 10.6 nM for mTOR and PI3Kα in a cell free assay , respectively.

PI5P4K-β-IN-1 (compound vs1) is a potent PI5P4K-β inhibitor with an IC50 of 0.80 μM [1].

Chemodosimeter 1 is designed as a highly selective phosphate ion (PI) sensor capable of demonstrating exogenous and endogenous ATP-catalysed PI production and is the first probe capable of tracking PI production and enrichment through half-channel closure

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

PARP/PI3K-IN-1 is a novel dual poly (ADP-ribose) polymerase (PARP) and phosphatidylinositol 3-kinase (PI3K) dual inhibitor with anticancer, antitumour and antiproliferative activities for the study of breast, pancreatic and lung cancers.

Selective PI3Kδ Inhibitor 1 is a PI3Kδ Inhibitor( IC50 = 0.9 nM).

PI3Kδ-IN-1 is an efficacious PI3Kδ inhibitor (IC50 of 1.7 nM).

PI5P4Ks-IN-1 (compound 7) is an active compound which engages PI5P4Kγ[1].

PI3Kα/HDAC6-IN-1 (compound 21j) is a dual inhibitor of PI3Kα and HDAC6, exhibiting IC50 values of 2.9 nM and 26 nM, respectively. It effectively hinders AKT(Ser473) phosphorylation and promotes the build-up of acetylated α-tubulin, while not influencing acetylated histones H3 and H4. The compound demonstrates potent anti-cancer efficacy by inhibiting the L-363 cell line with an IC50 of 0.17 μM [1].

PI3K/Akt/CREB Activator 1 is a potent, orally active compound that acts as an activator for the PI3K/Akt/CREB pathway. It enhances neuronal proliferation, induces differentiation of Neuro-2a cells into neuron-like morphology, and accelerates axon-dendrite polarization in primary hippocampal neurons by upregulating brain-derived neurotrophic factor. This compound is utilized in vascular dementia (VaD) research.

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

PI3Kβ-IN-1 is a selective, orally active PI3Kβ inhibitor (IC50: 2 nM).

PI5P4Kα-IN-1 (Compound 13) is a phosphatidylinositol 5-phosphate 4-kinase (PI5P4K) inhibitor, displaying IC50 values of 2 μM for PI5P4Kα and 9.4 μM for PI5P4Kβ, with potential applications in the study of cancer, metabolic, and immunological disorders [1].

PI3Kδ/γ-IN-1 is a selective and effective inhibitor of PI3Kδ/γ that can be used in the treatment of hematologic malignancies.

COX-2/PI3K-IN-1 (compound 5d) is a potent inhibitor of PI3K (IC50: 1.14 nM). COX-2/PI3K-IN-1 is a selective inhibitor of COX-2 (Ki: 3.24 nM).

PI3K/AKT-IN-1 is a potent, dual PI3K/AKT inhibitor that acts on PI3Kγ (IC50: 6.99 μM), PI3Kδ (IC50: 4.01 μM) and AKT (IC50: 3.36 μM). PI3K/AKT-IN-1 induces caspase 3-dependent apoptosis by inhibiting the PI3K/AKT pathway. caspase 3-dependent apoptosis and exhibited anticancer effects.

PI3K/VEGFR2-IN-1 is a potent dual inhibitor targeting both PI3K and VEGFR2 with IC50 values of 2.21 μM for PI3K and 68 μM for VEGFR2, respectively. This compound also induces apoptosis and is utilized in cancer research [1].

MEK/PI3K-IN-1 (compound 6r) is a potent inhibitor targeting both MEK and PI3K, exhibiting IC50 values of 124 nM for MEK1, 130 nM for PI3Kα, and 236 nM for PI3Kδ. It effectively reduces levels of pAKT and pERK1/2, demonstrating anti-proliferative effects on various tumor cell lines [1].

FAP-PI3KI1, a fibroblast-activated protein (FAP)-targeted PI3K inhibitor, selectively targets FAP-expressing human idiopathic pulmonary fibrosis (IPF) cells. It effectively inhibits collagen synthesis and reduces collagen deposition [1].

Chloramphenicol (Chloromycetin), a broad-spectrum antibiotic, blocks bacterial protein synthesis.

Pristinamycin, synthesized by Streptomyces pristinaespiralis, is an orally administered antibiotic resembling streptogramin, comprising two distinct components: Pristinamycin I (PI) and Pristinamycin II (PII). This compound exhibits a high efficacy against various antibiotic-resistant pathogens, especially Gram-positive bacteria such as Methicillin-resistant Staphylococcus aureus (MRSA), Vancomycin-resistant S. aureus (VRSA), and Enterococcus faecium (VREF) [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.

Lanosta-7,9(11),23,25(27)-tetraen-26-oic acid, 23,27-epoxy-3-oxo-, a lanosterane-type compound, can be isolated from Tu-Jin-Pi, the root bark of Pseudolarix kaempferi [1].

ZK-PI-9 acts as an inhibitor of both trehalase and chitinase activities in female pupae and functions as an insecticide [1].

ZK-PI-5, a potent trehalase inhibitor, has the potential to regulate Spodoptera frugiperda reproduction and may serve as a novel insecticide with significant pest control capabilities [1].

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)

PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual inhibitor of PI3K/mTOR (PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ/mTOR with IC50s of 20/376/204/46/186 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.

PI3Kdelta inhibitor 1 is a potent, selective and orally available inhibitor of PI3Kδ with an IC50 of 1.3 nM.

Brecanavir is a tyrosyl-based arylsulfonamide, high affinity, protease inhibitor (PI) for the treatment of human immunodeficiency virus type 1.

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-(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.

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.

PI3K-IN-1 (Voxtalisib Analogue) is a dual inhibitor of mTOR/PI3K, mostly for p110γ , also inhibits DNA-PK and mTOR.

PI3Kγ inhibitor 1 is a inhibitor of PI3Kδ and PI3Kγ.

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].

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.

PI3kδ inhibitor 1 is a selective inhibitor of PI3Kδ (IC50 of 3.8 nM).

PI3K/HDAC-IN-1 is a potent PI3K and HDAC dual inhibitor(IC50s of 8.1 nM and 1.4 nM, respectively).

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].

Cyclopropenone probe 1 can specifically and efficiently modify a triple-negative breast cancer driver, glutathione S-transferase pi-1 (GSTP1) , by covalently binding at the catalytic active site.

CDKI-83 is a potent CDK9 inhibitor. The compound shows effective anti-proliferative activity in human tumour cell lines with GI50 <1 μM, and is capable of inducing apoptosis in A2780 human ovarian cancer cells as determined by the activated caspase-3, Annexin V/PI double staining and accumulated cells at the sub-G1 phase of cellcycle. The research results suggest that combined inhibition of CDK9 and CDK1 may result in the effective induction of apoptosis and CDKI-83 has the potential to be developed as an anti-cancer agent.

Fluorescein diacetate (Di-O-acetylfluorescein) is a cell permeable esterase-substrate for hGSTP1-1.

TPC2-A1-N is a novel, lipophilic, membrane permeable isoform-selective small molecule agonist of two-pore channel 2 (TPC2). TPC2-A1-N plays its role by mimicking the physiological actions of NAADP and PI(3,5)P2 through independent binding sites. TPC2-A1-N has inverse effects on key lysosomal activities and increases the pH in the lysosomal lumen in a TPC2-dependent manner[1]. Two-pore channels (TPC1-3) are ancient members of the voltage-gated ion channel superfamily. TPCs are expressed throughout the endo-lysosomal system and regulates the trafficking of various cargoes.TPC2 can mediate different physiological and possibly pathophysiological effects depending on how it is activated. The ion selectivity of TPC2 is not fixed but rather agonist-dependent. TPC2 is a unique example of an ion channel that conducts different ions in response to different activating ligands.TPC2-A1-N (10 μM) reproducibly evokes Ca2+ signals, and TPC2-A1-N response reachs its plateau faster than TPC2-A1-P. The EC50 in full concentration-effect relationships for the plateau response is 7.8 μM for TPC2-A1-N in a cell line stably expressing TPC2L11A/L12A.TPC2-A1-N (10 μM) evokes Ca2+ influx through the TPC2 pore evokes Ca2+ signals in cells expressing TPC2L11A/L12A but not TPC2L11A/L12A/L265P. Additionally, the responses to TPC2-A1-N can be selectively blocked by the identified TPC2 blockers Tetrandrine , Raloxifene , and Fluphenazine by removal of extracellular Ca2+[1].In endo-lysosomal patch-clamp experiments, TPC2-A1-N (30 μM) elicits currents using Na+ as the major permeant ion, in vacuolin-enlarged endo-lysosomes isolated from isolated from HEK293 cells transiently expressing human TPC2 (hTPC2) but not in cells expressing TPC1[1].In endo-lysosomal patch-clamp experiments, TPC2-A1-N (30 μM) induces larger currents in endo-lysosomes isolated from cells expressing a gain-of-function variant of TPC2 (TPC2M484L) compared to the wild-type isoform, and exhibits an EC50 value of 0.6 μM for TPC2-A1-N[1]. [1]. Susanne Gerndt, et al. Agonist-mediated switching of ion selectivity in TPC2 differentially promotes lysosomal function. Elife

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

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