cell-permeable

MHY1485 is an mTOR activator that is cell-permeable. MHY1485 inhibits autophagosome and lysosome fusion, leading to accumulation of LC3II proteins and increased autophagosomes, thereby inhibiting cellular autophagy.

OSMI-1 is an O-GlcNAc transferase (OGT) inhibitor (IC50=2.7 μM) that is orally active and cell-permeable. OSMI-1 inhibits protein O-GlcNA acetylation without qualitatively altering cell-surface N- or O- linked glycans.

(Z)-SMI-4a (TCS PIM-1 4a) is a selective ATP-competitive Pim-1 kinase inhibitor with an IC50 of 21 nM.

STAT3-IN-24, a cell-permeable (PpYLKTK-mts) peptide inhibitor, obstructs the recruitment of STAT3 to Jak2 and inhibits the phosphorylation of Y705, thereby preventing STAT3 dimerization and nuclear translocation [1].

NFAT inhibitor, Cell Permeable aceate is a cell-permeable nuclear factor of activated T cells (NFAT) inhibitor. It can be used for the research of podocyte and diabetic nephropathy.

Bucladesine sodium (DC2797) is a cAMP analog with cell-permeable properties. Bucladesine sodium is also a cAMP-dependent protein kinase (PKA) activator and a phosphodiester (PDE) inhibitor. Bucladesine sodium has anti-inflammatory activity.

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.

PFB-FDGlu is a lysosomal Glucocerebrosidase (GCase) substrate with cell-permeable specificity that is cleaved to produce fluorescein.PFB-FDGlu is often used in conjunction with a flow cytometer to measure GCase activity in living cells on an individual cell basis.

BML-284 (Wnt agonist 1) is a potent, selective and , cell-permeable Wnt signaling activator.

740 Y-P acetate (740YPDGFR acetate) is a potent and cell-permeable PI3K activator.740 Y-P acetate tends to bind to GST fusion proteins containing the N- and C-terminal SH2 structural domains of p85, but not to GST alone.

MG-132 (Z-Leu-Leu-Leu-al) is a 26S proteasome inhibitor (IC50=100 nM) that is cell-permeable and reversible. MG-132 acts as an autophagy activator and also induces apoptosis.

Suprafenacine (N'-[(E)-(4-methylphenyl)methylidene]-4,5,6,7-tetrahydro-1H-indazole-3-carbohydrazide) is a cell-permeable microtubule destabilizer that induces cell cycle arrest and apoptosis in G2 M phase. Suprafenacine binds to microtubules and inhibits aggregation at the colchicine junction. Suprafenacine is selective for cancer cells, including drug-resistant cancer cells.

G36 is a cell-permeable non-steroidal antagonist of GPER. G36 inhibits activation by either 17β-estradiol or the GPER-selective agonist G-1 (IC50 = 112 and 165 nM, respectively). G36 has no detectable binding activity to either ERα or ERβ. G36 blocks the activation of PI3K or calcium mobilization triggered by estrogen through GPER and it suppresses ERK activation by estrogen or G-1 but not by EGF. G-36 can be used in combination with GPER-selective agonists, like G-1, to distinguish the roles of GPER from those of ERα and ERβ in complex biological systems.

GSK-J4 (GSK J4 HCl) is a cell permeable prodrug of GSK-J1, a dual inhibitor of the H3K27me3 me2 demethylases JMJD3 KDM6B and UTX KDM6A (IC50=8.6 6.6 μM). GSK-J4 induces endoplasmic reticulum stress-related apoptosis.

KDM2A 7A-IN-1 is a cell-permeable and selective inhibitor of histone lysine demethylase KDM2A 7A, with potential antitumor activity for studying duodenal adenomas and ossifying fibromucoid tumors.

OSMI-3 is a potent and cell-permeable inhibitor of O-GlcNAc transferase (OGT) for the study of cancer and cardiovascular disease.

DC_C66 DC_C66 has good selectivity for CARM1, PRMT1 (IC50 = 21μM), PRMT6 (IC50 = 47μM) and PRMT5. It is a cell-permeable, selective co-activator related arginine methyltransferase 1 (CARM1) inhibitor with IC50 of 1.8 μM.

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.

p53 Activator 7 is a highly potent and cell-permeable activator of the p53 mutation Y220C (MDM-2 p53), which induces apoptosis.

Tyrphostin AG 538 is a chalcone compound, an IGF-1 receptor kinase inhibitor (IC₅0 : for 400 nM) that is potent, cell-permeable, reversible, and competitive.

AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeable trifluoromethyl ketone analog of arachidonic acid and a potent, selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). By blocking the production of arachidonate and 12-hydroxyeicosatetraenoic acid in calcium ionophore-challenged platelets, AACOCF3 hinders their synthesis. Additionally, AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets, making it promising for cardiovascular disease research.

CUR61414 hydrochloride is a potent and cell permeable inhibitor of Hedgehog signaling pathway (IC50 =100-200 nM). CUR61414 hydrochloride is a small-molecule aminoproline class compound. CUR61414 hydrochloride selectively binds to smoothened (Smo, Ki= 44 nM). CUR61414 hydrochloride can induce cancer cells apoptosis without affecting neighboring non-tumor cells.

INCA-6 (Triptycene-1,4-quinone) is a cell-permeable NFAT inhibitor that disrupts CN-NFAT signaling by targeting the NFAT(P) substrate at the calcineurin (CN) phosphatase site.

CUR61414 is a cell-permeable inhibitor of Hedgehog signaling pathway (IC50 =100-200 nM) and selectively binds to smoothened (Ki = 44 nM).