CGP 57380 is potent MNK1 inhibitor with IC50 of 2.2 μM, exhibiting no inhibitory activity on p38, JNK1, ERK1 and -2, PKC, or c-Src-like kinases.
Ro 25-6981 maleate salt is a potent and selective antagonist of NMDA glutamate receptors containing the NR2B subunit with IC50 values of .009 μM for NR2B vs. 52 μM for NR2A subunits. Ro 25-6981 has been shown to have neuroprotectant effects and to reduce inflammatory and neuropathic pain in rodent models.
Ripasudil (K-115) hydrochloride dihydrate is potent ROCK inhibitor with IC50 of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension.
Clascoterone (Cortexolone 17α-propionate, CB-03-01) is a new selective androgen receptor (AR) antagonist.
Lubiprostone is a gastrointestinal agent used for the treatment of idiopathic chronic constipation.
Bergaptol is a hydroxylated psoralen that acts as a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 uM.
Aminopurvalanol A is a selective, cell-permeable, reversible and ATP-competitive cyclin-dependent kinase (CDK) inhibitor, inhibiting cdk1/cyclin B, cdk2/cyclin A, cdk2/cyclin E, and cdk5/p35. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization.
Zearalenone is a mycotoxin obtained from Fusarium oxysporum and a non-steroidal oestrogen that acts by binding to the oestrogen receptor (ER) and has endocrine modulating or disrupting functions in animals.
Echistatin TFA is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of the BET family of proteins with IC50 values of 4-18 nM for BRD2, BRD3, BRD4, and BRDT for AML and metastatic desmoplasia-resistant prostate cancer.
Sotrastaurin is a potent and orally-active pan-PKC inhibitor, with Kis of 0.22 nM, 0.64nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively.