Ribociclib (LEE011)
Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor. Phase 3.
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Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor. Phase 3.
ME0328 is a potent and selective PARP inhibitor with IC50 of 0.89 μM for PARP3, about 7-fold selectivity over PARP1.
Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor.
NH125 is a selective eEF-2 kinase inhibitor with IC50 of 60 nM, >125-fold selectivity over PKC, PKA, and CaMKII, and also a potent histidine kinase inhibitor.
AR-A014418 is an ATP-competitive, and selective GSK3β inhibitor with IC50 and Ki of 104 nM and 38 nM in cell-free assays, without significant inhibition on 26 other kinases tested.
TAPI-1 is an ADAM17/TACE inhibitor, which blocks shedding of cytokine receptors.
SB-3CT is an effective and selective gelatinase inhibitor with Ki of 13.9 nM and 600 nM for MMP-2 and MMP-9, respectively.
MI-2 (MALT1 inhibitor) is an irreversible MALT1 inhibitor with IC50 of 5.84 μM.
PD 151746 is a selective, cell-permeable calpain inhibitor with Ki of 0.26 μM for μ-Calpain, about 20-fold selectivity over m-calpain.
KN-93 Phosphate is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.37 μM, no remarkable inhibitory effects on APK, PKC, MLCK or Ca2+-PDE activities.
KN-62 is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.9 μM also a non-competitive antagonist of the purinergic receptor P2RX7 (IC50 = 15 nM). It is selective for CaMKII relative to PKA, PKC and MLCK, but inhibits CaMKI and CaMKIV equally well, The Ki value of KN-62 for CaMK V is 0.8 μM.
CA-074 Me is a membrane-permeable derivative of CA-074 and acts as an irreversible cathepsin B inhibitor.
Blasticidin S HCl is a nucleoside antibiotic isolated from Stretomyces girseochromogenes, and acts as a DNA and protein synthesis inhibitor, used to select transfected cells carrying bsr or BSD resistance genes.
Puromycin 2HCl is an aminonucleoside antibiotic, which acts as a protein synthesis inhibitor.
Caffeic acid phenethyl ester is a potent and specific inhibitor of NF-κB activation, and also displays antioxidant, immunomodulatory and antiinflammatory activities.
Ascomycin (FK520), an FK-506 analog, is a neutral macrolide immunosuppressant, which prevents rejection after an organ transplant. Phase 3.