cell permeability

ML167 (CID44968231) is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor.

PAF (C16) is a potent MAPK and MEK ERK activator that induces increased vascular permeability. PAF (C16) (PAF (C16)) is a platelet-activating factor, a phospholipid-derived mediator and a ligand for PAF G protein-coupled receptor (PAFR). PAF (C16) has shown anti-apoptotic and anti-inflammatory activity in vitro, inhibiting Caspase-dependent apoptosis by interacting with its receptor (PAF-R) to perform cell signaling.

PX-478 is a HIF-1α inhibitor with selectivity, oral activity, and blood-brain barrier permeability. PX-478 has antitumor activity and also protects pancreatic β-cell function in diabetes mellitus and is used in type 2 diabetes mellitus research.

Vancomycin is a glycopeptide antibiotic that exerts its antibacterial activity by inhibiting the second stage of cell wall synthesis in susceptible bacteria. It also alters cell membrane permeability and selectively inhibits RNA synthesis. Vancomycin is commonly used to treat severe infections resistant to other antibiotics and is frequently employed in experimental studies to induce kidney injury models.

Sulfo-ara-F-NMN is an analogue of nicotinamide mononucleotide (NMN) with cellular permeability. Sulfo-ara-F-NMN was selective to activate SARM1 and inhibited CD38 with an IC50 of about 10 μM. Activation by Sulfo-ara-F-NMN to Z-48 or NMN, which has a higher cyclase activity, causes conformational changes in SARM1, resulting in cADPR production, NAD depletion, and non-apoptotic cell death.

Stafib-2 is a potent and selective inhibitor of the transcription factor STAT5b, with IC50 values of 82 nM and 1.7 μM for STAT5b and STAT5a, respectively. Stafib-2 has poor cell permeability.

Tioconazole (Vagistat) is a synthetic imidazole derivative, inhibits cell wall synthesis by inhibiting the biosynthesis of ergosterol or other sterols, damaging the fungal cell membrane, altering its permeability, and promoting loss of essential intracellular elements.

Cholesterol is the primary sterol in mammals, accounting for approximately 20–25% of the plasma membrane structure. It plays a key role in regulating membrane fluidity, permeability, and protein function. As an endogenous agonist of estrogen-related receptor α (ERRα), cholesterol is widely involved in metabolic regulation and serves as a precursor for the synthesis of hormones and bile acids. It is commonly used in experimental models of hyperlipidemia.

Ceramides Mixture, an endogenous ceramide, consists of hydroxy and non-hydroxy fatty acid-containing ceramides. It is involved in the regulation of cell cycle arrest, growth inhibition, and modulation of telomerase activity.

Butoconazole Nitrate is the nitrate salt form of butoconazole, a synthetic imidazole derivative with fungistatic properties. Butoconazole nitrate (RS 35887) interferes with steroid biosynthesis by inhibiting the conversion of lanosterol to ergosterol, thereby changing the fungal cell membrane lipid composition. This alters cell permeability and leads to growth inhibition. Butoconazole nitrate is active against many dermatophytes and yeasts. It also contains antibacterial effects against some gram-positive organisms.

Liranaftate (Piritetrate) is a thiocarbamate and squalene epoxidase inhibitor with antifungal activity. Liranaftate inhibits fungal squalene epoxidase, an enzyme that plays a key role in the synthesis of sterol which is essential for cell membrane integrity. By preventing ergosterol synthesis and causing accumulation of squalene, this agent increases cell membrane permeability, cell leakage and eventually cell lysis.

Terconazole (Terazol 7) is a synthetic triazole derivative structurally related to fluconazole, antifungal Terconazole seems to disrupt cell wall synthesis by inhibiting biosynthesis of ergosterol or other sterols, damaging the fungal cell membrane, altering its permeability, and promoting loss of essential intracellular elements. Terconazole is active against Candida sp.

2-Aminoimidazole is a potent antimicrobial agent that effectively targets drug-resistant Mycobacterium tuberculosis by disrupting the proton motive force and blocking the electron transport chain, potentiates the action of beta-lactam antibiotics against Mycobacterium tuberculosis by decreasing the secretion of beta-lactamases and increasing the permeability of cell membranes, activates drug-resistant bacteria and improves therapeutic efficacy.

N-Acetylcysteine amide is a thiol antioxidant and a neuroprotective agent with cell permeability and blood-brain barrier permeability. N-Acetylcysteine amide reduces ROS production.

Sulconazole mononitrate (Exelderm) is the nitrate salt form of sulconazole, a synthetic imidazole derivative with the antifungal property. Sulconazole mononitrate inhibits fungal cytochrome P-450 sterol C-14 alpha-demethylation, resulting in the accumulation of fungal 14 alpha-methyl sterols and inhibition of the synthesis of ergosterol, an important component of the fungal cell membrane. Inhibition of ergosterol synthesis leads to a disruption of cell membrane permeability, and ultimately inhibition of cell wall synthesis. In addition, Sulconazole mononitrate seems to interfere with the autolytic degradation of fungal DNA and RNA.

sCNH240 (2-Fluoro-N-[3-(3-thienyl)-5-isoxazolyl]benzenesulfonamide) is a potential and selective Rv1625c Cya activator with good cell permeability and oral activity, IC90=1.24 μM in cholesterol-supplemented 7H12 medium against Mycobacterium tuberculosis (Mtb) H37Rv strain, and inhibition of CYP2C19, CYP2C9 and hERG channels.

BMS 183920 is a potent Angiotensin II Receptor antagonist that improves improves Caco-2 cell permeability in vivo.

Z-DEVD-FMK (Caspase-3 Inhibitor) is a Caspase-3 inhibitor (IC50=18 μM), featuring selectivity, irreversibility and cell permeability. Z-DEVD-FMK can inhibit caspase activation induced apoptosis.

DI-591 is an effective, high-affinity and cell-permeability inhibitor for DCN1-UBC12 interaction. DI-591 binds to DCN1 and DCN2 with Ki values of 12 and nM and 10.4 nM, respectively, and has no obvious binding to DCN3, DCN4 and DCN5 proteins.

Oxiconazole nitrate (Ro 13-8996) is the nitrate salt form of oxiconazole, a broad-spectrum imidazole derivative with antifungal activity. Likely inhibiting cytochrome P450-dependent demethylation of lanosterol, it prevents ergosterol synthesis, a crucial component of the fungal cell membrane. This disruption of membrane synthesis and integrity alters permeability, promotes loss of essential intracellular components, and inhibits fungal cell growth.

Lanoconazole is an antifungal imidazole drug used primarily for the treatment of fungal skin infections that is potent and orally available. It acts by inhibiting the synthesis of ergosterol in fungal cell membranes, increasing the permeability of fungal cell membranes, leading to cell lysis and death. Lanoconazole exhibits potent antifungal activity against a wide range of pathogenic fungi including yeast, dermatophytes, dermatiaceous fungi, dimorphic fungi, Aspergihs spp., and Candida spp..

Anti-MRSA agent 18 (E17) is an inhibitor of MRSA, exhibiting MIC values of 2 μg mL for S. aureus and 4 μg mL for MRSA. This compound accelerates bacterial death by interacting with the bacterial cell membrane constituents, phosphatidylglycerol and cardiolipin, leading to changes in membrane permeability and polarization. Additionally, it increases intracellular ROS, along with leakage of DNA and proteins.

Antifungalagent 117 is a bipyrrole carboxamide derivative with antifungal activity, exhibiting an EC50 value of 11.58 mg L against Sclerotinia sclerotiorum. This compound induces cell death by increasing cell membrane permeability, causing an imbalance in osmotic pressure between the interior and exterior of the cell. It also promotes oxidative damage to the cell membrane by inducing the accumulation of reactive oxygen species (ROS), leading to the leakage of cellular contents. RNA sequencing analysis has demonstrated that Antifungalagent 117 disrupts cell membrane structure by downregulating catalase genes and upregulating neutral ceramidase genes, accelerating ceramide metabolism and hastening cell death. The compound holds significant potential for application in plant protection and the control of fungal infections.

Antibiofilm agent-13 (compound 14b) is an effective broad-spectrum antibacterial agent that functions by disrupting the integrity of bacterial cell membranes. It achieves this through the degradation of transmembrane potential and increased membrane permeability, which leads to the production of intracellular ROS and the leakage of DNA and proteins, ultimately resulting in bacterial death. Antibiofilm agent-13 effectively inhibits both Gram-positive bacteria (MIC ranging from 0.5-1 μg mL) and Gram-negative bacteria (MIC ranging from 1-32 μg mL).