cell permeability

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

LDL-IN-3 belongs to synthetic compounds and is an antioxidant and anti-atherosclerotic agent with good cell permeability and cardiovascular protective properties. This compound is used for the treatment of atherosclerosis-related diseases, effectively inhibiting oxidative stress and lipid deposition, and reducing arterial plaque formation.

Candoxatril (UK 79300) is a small-molecule inhibitor and a neutral endopeptidase (NEP) inhibitor with oral activity and cell permeability, used for the treatment of chronic heart failure and capable of improving exercise capacity in patients receiving angiotensin-converting enzyme inhibitor therapy.

D18024 belongs to phthalazinone derivatives and is a histamine H1 receptor antagonist with anti-allergic activity. This compound exhibits good selectivity and cell permeability, and can be used in research on allergic diseases such as chronic spontaneous urticaria.

Orforglipron (LY3502970) belongs to non-peptide small molecule GLP-1 receptor agonists and is a highly selective, orally effective GLP-1 receptor agonist with good cell permeability and oral bioavailability. This compound is used in research on type 2 diabetes and obesity, demonstrating significant glucose-lowering and weight-reducing activities.

Pentiapine (CGS 10746) is a small-molecule inhibitor and a dopamine release inhibitor with cell permeability, used in neuropharmacological research to modulate dopaminergic signaling, holding significant application value in studies related to nervous system mechanisms.

MIK665 (S-64315) is a small-molecule inhibitor and a myeloid cell leukemia sequence 1 (MCL1) inhibitor (IC50 = 1.81 nM) with high selectivity and cell permeability. Used in experimental research, this compound exhibits antitumor activity in hematologic malignancies such as acute myeloid leukemia.

Benin (Butocine) is a natural product and a cell growth inhibitor with antitumor activity. This compound can be used in breast cancer-related research, exhibiting potential to inhibit proliferation of multiple breast cancer cell lines, with favorable cell permeability, suitable for in vitro and in vivo exploration of antitumor mechanisms.

Meclinertant (SR 48692) is a small-molecule compound and a neurotensin receptor-1 (NTSR1) antagonist with good selectivity and cell permeability. This compound can be used to study neurotensin signaling pathways and related neurological diseases, and serves as a potential diagnostic and therapeutic probe targeting NTSR1-positive tumors.

Remibrutinib (Rhapsido) belongs to small molecule inhibitors and is a highly selective, covalent Bruton's tyrosine kinase (BTK) inhibitor (IC50 = 1 nM) with oral activity and cell permeability. The IC50 for inhibiting BTK activity in blood is 0.23 μM. This compound can be used in research on chronic urticaria.

PND-1186 (VS-4718) is a small molecule inhibitor, a highly specific, reversible FAK inhibitor (IC50=1.5 nM) with good selectivity and cell permeability. This compound inhibits FAK phosphorylation, blocking tumor cell survival, proliferation, migration, and angiogenesis, and is primarily used for anti-tumor research on solid tumors.

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.

Digitonin is a natural product of the glycoside family and is a detergent. Digitonin has antitumor activity, binds to cholesterol molecules to increase the permeability of cell membranes, and is active in the cleavage of cell membranes in a wide range of cells.

AZD3965 (AZD-3965) belongs to small molecule inhibitors, serving as a monocarboxylate transporter 1 (MCT1) inhibitor (Ki=1.6 nM), with 6-fold higher selectivity for MCT1 over MCT2, featuring favorable selectivity, cell permeability, and oral activity, for antitumor research.

D-GsMTx4 TFA belongs to natural products and is a TRPC1/6 and Piezo2 channel inhibitor with high selectivity and cell permeability, inhibiting Ca2+ influx and the mTOR pathway. This compound is used in research on myocardial infarction, chronic pain, and pulmonary fibrosis.

PFB-FDGlu belongs to fluorescent dyes and is a lysosomal β-glucocerebrosidase (GCase) substrate that releases fluorescein upon hydrolysis by GCase, possessing cell permeability. This compound can be used for flow cytometric detection of GCase activity in live cells.

BLU0588 is a small-molecule inhibitor and a PRKACA-targeted inhibitor (IC50 = 1 nM, Kd = 4 nM), featuring high selectivity, cell permeability, and oral activity, suitable for experimental research and therapeutic development in fibrolamellar hepatocellular carcinoma (FLC).

Linsitinib (OSI-906) belongs to small molecule inhibitors and is a dual IGF-1/IR inhibitor (IC50 = 35 and 75 nM, respectively) with selectivity, cell permeability, and oral activity. This compound is used in antitumor research and can effectively inhibit cell proliferation and induce apoptosis.

Saracatinib (AZD0530) is a small molecule inhibitor belonging to the Src family kinase inhibitors (IC50=2.7–11 nM), featuring high selectivity, cell permeability, and oral bioavailability, with anti-fibrotic, anti-inflammatory, and potential anti-tumor activities.

Fostamatinib (R788) is a small-molecule inhibitor and an oral prodrug of R406, a Syk/FLT3-targeted inhibitor (IC50 = 41 nM) that also inhibits Lyn (IC50 = 63 nM) and Lck (IC50 = 37 nM), featuring oral activity and cell permeability, used for the treatment of immune thrombocytopenia.

Bemcentinib (R428) belongs to small molecule inhibitors and is a highly selective oral Axl inhibitor (IC50 = 14 nM) with oral bioavailability and potent cell permeability. This compound effectively inhibits cancer cell migration and invasion, blocks tumor dissemination, and prolongs survival in various tumor models.

GW3965 hydrochloride (GW3965 HCl) belongs to synthetic small molecules and is a liver X receptor (LXR) agonist (hLXRα EC50 = 190 nM; hLXRβ EC50 = 30 nM) with subtype selectivity, cell permeability, and oral activity. This compound is used in research related to metabolism, inflammation, and neuropathic pain.

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.

VER-155008 is an Hsp70 inhibitor (IC50 = 0.5 μM), exhibiting over 100-fold selectivity against Hsp90, and capable of inhibiting Hsc70 and Grp78 (IC50 = 2.6 μM for both). This compound possesses good selectivity and cell permeability, and is used in anti-tumor research, showing therapeutic potential in leukemia and solid tumor models.