Activators & Inhibitors

Activity: Nedd8 activating enzyme inhibitor . Function/Pharmacology: MLN4924 is a potent and selective NEDD8-activating enzyme (NAE) inhibitor.1 It disrupts cullin-RING ligase-mediated protein turnover leading to apoptosis in human tumor cells. Suppresses the growth of human tumor xenografts in mice.2 Upregulates PD-L1 expression and enhances the efficacy of immune checkpoint blockade in glioblastoma.3 Modulates tumor microenvironment.4 Blocks the neddylation of the DNA endonuclease CtIP, which promotes HDR in Cas9- and Cpf1-mediated gene editing. Part of the CRISPY mix for increasing precise gene editing.5 Cell permeable. Chemical Name: ((1S,2S,4R)-4-(4-(((S)-2,3-dihydro-1H-inden-1-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-2-hydroxycyclopentyl)methyl sulfamate

Activity: Kinesin Eg5 inhibitor . Function/Pharmacology: Selective mitotic kinesin Eg5 inhibitor (IC50 = 1.3 μM) which acts in an ATP-noncompetitive manner1,2. It is at least 150-fold more selective for Eg5 than other members of the kinesin superfamily. K858 blocks centrosome separation, activates the spindle checkpoint and induces mitotic arrest accompanied by the formation of monopolar spindles. Displays no effect on microtubule polymerization. Selectively displays antiproliferative effects via induction of mitotic cell death in cancer cells over nontransformed cells1. Chemical Name: N-(4-Acetyl-4,5-dihydro-5-methyl-5-phenyl-1,3,4-thiadiazol-2-yl)acetamide

Activity: omega-3 fatty acid . Function/Pharmacology: Dietary enrichment of eicosapentaenoic acid may have anti-inflammatory effects by inhibiting the 5-lipoxygenase pathway and LTB4-mediated neutrophil functions1. Displays various cardiovascular protective properties2. Chemical Name: Eicosa-5Z,8Z,11Z,14Z,17Z-pentaenoic acid (20:5, n-3)

Activity: Proteasome inhibitor . Function/Pharmacology: Specific inhibitor of three proteolytic activities of the proteasome. Chymotrypsin-like activity is inhibited most potently followed by trypsin-like activity. Inhibition of the peptidyl-glutamyl peptide hydrolytic activity is relatively weak. Chemical Name: Fermentation product from Streptomyces lactacystinaeus

Activity: PI3-K inhibitor . Function/Pharmacology: Inhibits PI-3 Kinase with selectivity for p110α (IC50=0.1 nM). Displays antitumor activity. Irreversible. Cell permeable. Chemical Name: null

Activity: Endogenous lipo-amino acid . Function/Pharmacology: Endogenous lipoamino acid. Chemical Name: N-Docosahexaenoylglycine

Activity: p97 inhibitor . Function/Pharmacology: An irreversible inhibitor of p97 (IC50<10 M). Cell permeable Chemical Name: 3,4-Methylenedioxy-ß-nitrostyrene

Activity: PDE2 inhibitor . Function/Pharmacology: Potent and selective inhibitor of phosphodiesterase PDE2, IC50 = 40 nM. More potent than EHNA, another commonly used PDE2 inhibitor. Displays no effect on a panel of over 80 receptors, ion channels and enzymes.1 Cell permeable Chemical Name: 6,7-Dihydro-5-methyl-6-oxo-N-(1,3,4-thiadiazol-2-yl)-5H-furo[2,3-f]indole-7-carboxamide

Activity: L-type calcium channel blocker . Function/Pharmacology: An L-type calcium channel blocker.1 Prevents age-induced learning deficits in a rat model.2 Facilitates recovery of function after brain damage3 and displays neuroprotective effects4. Promotes remyelination in a mouse model of multiple sclerosis.5 In clinical use for reduction of cerebral vasospasm following subarachnoid hemorrhage.6 Chemical Name: 1,4-Dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid 2-methyloxyethyl 1-methylethyl ester