pip2

Inavolisib (GDC-0077) is an orally available selective PI3Kα inhibitor with an IC50 value of 0.038 nM.It exerts its activity by binding to the ATP-binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3.

UNC3230 is a potent, selective, and ATP-competitive PIP5K1C inhibitor with an IC50 of approximately 41 nM. UNC3230 (UNC 3230) also inhibits PIP4K2C.

NA 382 is a staurosporine derivative that inhibits multidrug resistance.

BA6b9 is an allosteric inhibitor targeting the SK4 channel via the CaM-PIP2 binding domain. It interacts with two critical residues, Arg191 and His192, located in the S4-S5 linker to inhibit the SK4 channel, with an IC50 of 8.6 μM (WT SK4). BA6b9 significantly prolongs the effective refractory period (ERP) of the atria and atrioventricular node in isolated rat hearts, reducing the induction of atrial fibrillation (AF), highlighting its potential for arrhythmia research.

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.

187-1, N-WASP Inhibitor TFA, a 14-amino acid cyclic peptide, serves as an allosteric inhibitor of the neural Wiskott-Aldrich syndrome protein (N-WASP). This compound effectively suppresses actin assembly triggered by phosphatidylinositol 4,5-bisphosphate (PIP2), exhibiting a potent inhibitory concentration (IC 50) of 2 μM. Furthermore, 187-1, N-WASP Inhibitor TFA inhibits the activation of the Arp2/3 complex by N-WASP, maintaining the protein in its autoinhibited state, ensuring the prevention of its activation.

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.

Inhibits neural Wiskott-Aldrich syndrome protein (N-WASP) by stabilizing the autoinhibited state of the protein. Blocks phosphatidylinositol 4,5-bisphosphate (PIP2)-stimulated actin assembly (IC50 ~ 2 μM) but does not directly inhibit actin polymerization

Selective formyl peptide receptor 2 (FPR2) antagonist; cell permeable. Selectively inhibits FPR2-mediated NADPH oxidase activity but has no effect on FPR1 signaling in neutrophils. Displays PIP2 binding activity in vitro and blocks cell motility. Also exh

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.