PKR Inhibitor is an oxindole/imidazole derivative that binds the ATP-binding site of PKR and blocks autophosphorylation with an IC50 value of 186-210 nM.3 PKR Inhibitor protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress.
GZ-793A is a selective inhibitor of vesicular monoamine transporter 2 (VMAT2), which transports the monoamine neurotransmitters from cellular cytosol into synaptic vesicles.
NBMPR is a nucleoside analog that competitively inhibits the equilibrative nucleoside transporter 1 (Kd = 0.1-1.0 nM, IC50s = 4.6 and 3.6 nM in rat and human, respectively).
TNP 470 is an analog of Fumagillin that displays potent antiangiogenic activity in vitro. Shown to inhibit MetAP-2 (methionine aminopeptidase type II ).
Meclofenoxate HCl is an anti-aging drug used to treat the symptoms of senile dementia and Alzheimer's disease, and also inhibits the activity of cholinephosphotransferase.
HAMNO, also known as NSC-111847, is a potent and selective inhibitor of replication protein A (RPA) interactions with proteins involved in the replication stress response.
KL-1 is an inhibitor of SEC and transcription elongation by Pol II which disrupts the cyclin T1-AFF4 interaction within SEC, and attenuates SEC-dependent rapid transcriptional responses. KL-1 inhibits MYC transcriptional programs.
SKF-34288 hydrochloride (3-Mercaptopicolinic acid) is a phosphoenolpyruvate carboxykinase (PEPCK) inhibitor. SKF-34288 hydrochloride is a potent hypoglycemic agent via inhibition of glucose synthesis through the specific inhibition of PEPCK in the gluconeogenesis pathway.
NIC3 is a selective nucleus accumbens-associated protein-1 (NAC1) inhibitor, binds to the conserved Leu-90 of NAC1, prevents its homodimerization, and leads to proteasomal NAC1 degradation. Anti-cancer activity.
BEC HCl is a slow-binding, and competitive arginase inhibitor with Ki of 0.31 μM (pH7.5) and 0.4-0.6 μM for Arginase II and rat Arginase I, respectively.
Sardomozide is a second-generation polyamine synthesis inhibitor, which inhibits the activity of the polyamine biosynthetic enzyme S-adenosylmethionine decarboxylase (SAMDC).
PXS-4728A is a very potent and highly selective compound in development for the treatment of cardiometabolic diseases like the liver-related disease Nonalcoholic Steatohepatitis (NASH).
SPL-B, Orally active inhibitor of transforming acidic coiled-coil protein (TACC3) that selectively inhibits the nucleation of centrosome microtubules in ovarian cancer cells, without affecting spindle assembly in normal cells.
Eprodisate is an orally available disodium salt form of eprodisate, a negatively charged sulfonated inhibitor of fibrillogenesis, that can be used in the treatment of amyloid A (AA) amyloidosis.
SecinH3 is a selective cytohesin inhibitor with IC50 of 2.4 μM, 5.4 μM, 5.4 μM, 5.6 μM, 5.6 μM, and 65 μM for hCyh2, hCyh1, mCyh3, hCyh3, drosophila steppke, and yGea2-S7, respectively.
Amcasertib (BBI503), a first-in-class cancer stemness kinase inhibitor, is claimed to inhibit Nanog and other CSC pathways by targeting kinases with potential anticancer activity.