membrane-permeable

Membrane-Permeable Sequence (MPS) is a cell-penetrating peptide (CPP) utilized in the investigation of membrane crossing mechanisms [1].

QX 314 (Lidocaine N-ethyl bromide) is a blocker of non-membrane-permeable,and Inhibits Acid-Induced Activation of Esophageal Nociceptive C Fiber Neurons.

ITSA-1 is membrane permeable and specifically suppresses TSA inhibition of HDAC (histone deacetylase), but shows no activity towards other HDAC inhibitors.

Leupeptin hemisulfate is a protease inhibitor with cell membrane-permeable, reversible, competitive, and oral activities. Leupeptin hemisulfate inhibits the activity of Cathepsin B, Cathepsin H, and Cathepsin L, and blocks fusion of amphipathic lysosomes. Leupeptin hemisulfate also has anti-inflammatory activity.

8-Bromo-cGMP sodium is a PKG activator, a membrane-permeable analog of cGMP. 8-Bromo-cGMP sodium has pain-relieving and vasodilatory effects, significantly inhibits Ca2+ macroscopic currents, and inhibits high K+-stimulated insulin release.

KHK-IN-1 (KHK-IN-8) is a selective and cell membrane permeable inhibitor of ketohexokinase (KHK, IC50=12 nM; F=34%). KHK-IN-1 inhibits F1P production in HepG2 cell lysates with IC50 of 400 nM. KHK-IN-1 has potential for the study of obesity and diabetes.

DA-3003-1 (DA-3003-1) is a membrane-permeable, potent and selective Cdc25 dual specificity phosphatase inhibitor with antitumor activity that inhibits Cdc25B2, Cdc25A, Cdc25B2 and Cdc25C.

DSS Crosslinker is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). It is a homobifunctional crosslinker that is cell membrane permeable, with amine-reactive NHS esters at both ends of an 8-atom [11.4 angstrom] spacer arm for conjugating proteins, including intracellular proteins.

Trolox is a vitamin E analogue, used in reducing oxidative stress or damage.

4-(Dimethylamino)phenol enhances extracellular lactate dehydrogenase (LDH) levels without significant effects on gluconeogenesis. Only when the membrane becomes permeable to LDH does 4-(Dimethylamino)phenol reduce ATP content.

TUN-92046 (Dimethyl 2-oxoglutarate) is a membrane-permeable alpha-ketoglutarate analogue that inhibits maladaptive autophagy in pressure overloading induced cardiomyopathy.

BAMB-4 (ITPKA-IN-C14) is a highly membrane-permeable inhibitor of inositol-1,4,5-trisphosphate-3-kinase A (ITPKA), effectively suppressing the metastasis-promoting effect of ITPKA in lung tumor cells (with IC50 of 37 μM in ADP-Glo Assay).

EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated. EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a.

NSC305787 hydrochloride ((Rac)-NSC305787 hydrochloride is a cell membrane permeable and selective and potent small molecule dual inhibitor of Cdc25 dual specificity phosphatase and EZR that displays antitumor activity in pancreatic cancer cells and inhibits Cdc25B2, Cdc25A, Cdc25B2 and Cdc25C.NSC 663284 inhibits NSD2 (IC50 of 170 nM) enzyme activity.

CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM). Which can be used for the study of heart failure. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively.

TFMB-(R)-2-HG is a cell membrane-permeable (R)-2-HG, an oncogenic factor in acute myeloid leukemia. It impairs SCF ER-Hoxb8 cell differentiation in response to estrogen withdrawal.

trans-Sulfo-SMCC is a non-cleavable, membrane-permeable ADC crosslinker.

DSSeb Crosslinker (Disuccinimidyl sebacate) is a dual N-hydroxyethyl ketone ester and cell-membrane-permeable amine-reactive crosslinker, suitable for protein crosslinking and investigating protein-protein interactions.

Iodoacetyl-LC-Biotin (Iaa-Biotin) is a biotinylated and haloacetyl-activated sulfhydryl-responsive probe that forms irreversible thioether bonds at alkaline pH (7.5-8.5), is membrane-permeable, and can be used to label protein cysteines and other sulfhydryl-containing molecules.

NMDAR antagonist 2 (compound 3I) is a blood-brain barrier permeable antagonist of NMDA receptors, exhibiting IC50 values of 4.42 μM and 214.75 μM at membrane potentials of -60 mV and 40 mV, respectively, for hGluN1/hGluN2A. This compound has been shown to mitigate hippocampal damage.

Vacuolin-1 is a cell-permeable inhibitor of Ca2+ dependent fusion of lysosomes to the cell membrane. It acts by inhibiting release of lysosomal content.vacuolin‐1 is a potent and selective PIKfyve inhibitor and inhibits late‐stage autophagy by impairing lysosomal maturation

TGX-221, an effective, specific, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, is utilized for cancer treatment.

Aloe emodin anthrone is a stimulant-laxative which has been shown to enhance colonic membrane permeability of water-soluble and poorly permeable compounds.

Aloe-emodin-glucoside is a stimulant-laxative which has been shown to enhance colonic membrane permeability of water-soluble and poorly permeable compounds.