Activators & Inhibitors

Activity: p53/mdm2 inhibitor . Function/Pharmacology: A novel inhibitor of the MDM2-p53 interaction. Mimics three p53 residues involved in binding to MDM2. Binds to MDM2 with a Ki of 120 nM. Activates p53 in cancer cells. Cell permeable. Chemical Name: 2-Methyl-7-[Phenyl(phenylamino)methyl]-8-quinolinol

Activity: Histone Methyl transferase inhibitor+D257 . Function/Pharmacology: BIX-01294 is a selective inhibitor of G9a histone methyltransferase (G9aHMTase; IC50 = 1.7 µM) as well as GLP HMTase (IC50 = 38 µM) leading to a decrease in H3K9me2(histone H3 lysine 9 methylation) in vitro.1 BIX-01294 facilitates the reactivation of pluripotency genes and induces passive demethylation, thus promoting reprogramming. BIX-01294, in combination with BAY K8644 (a calcium channel agonist), was found to improve reprogramming efficiencies of Oct4-Klf4-(OK)-infected neural progenitor cells.3 Chemical Name: 2-(Hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine trihydrochloride

Activity: SIRT inhibitor . Function/Pharmacology: Inhibitor of sirtuin family enzymes including human SIRT1 (IC50=60μM), human SIRT2 (IC50=58μM), and yeast Sir2 (IC50=48μM) with no inhibition of human HDAC1. Active in vivo and in purified enzyme studies. Cell permeable. Chemical Name: 2-[[(2-Hydroxy-1-naphthalenyl)methylene]amino]-N-(1-phenylethyl)benzamide

Activity: HAT inhibitor . Function/Pharmacology: Garcinol is a HAT (histone acetyltransferase) inhibitor (p300 IC50=7µM and PCAF IC50=5µM) both in vitro and in vivo.1 It potentiates TRAIL-induced apoptosis of cancer cells. Garcinol, independent of the cell type, induces both of the TRAIL receptors, death receptor 4 (DR4) and DR5. Garcinol neither induces the receptors of normal cells nor sensitizes them to TRAIL.2 Chemical Name: null

Activity: Dopamine agonist . Function/Pharmacology: Archetypal dopamine pan-receptor agonist. Displays anti-Parkinsons activity in vivo.1 Protects against MPTP-induced neurotoxicity in a mouse model.2 In clinical use for Parkinson’s disease.4,5 Chemical Name: (R)-5,6,6a,7-Tetrahydro-6-methyl-4H-dibenzo[de,g]quinolone-10,11-diol hydrochloride

Activity: MMP inhibitor . Function/Pharmacology: Potent pan-specific inhibitor of matrix metalloproteinases (MMPs).1 Ki values have been reported for the following human MMPs: MMP-1, 0.4nM; MMP-2, 0.5nM; MMP-3, 27nM; MMP-7, 3.7nM; MMP-8, 0.1nM; MMP-9, 0.2nM; MMP-12, 3.6nM; MMP-14, 13.4nM; MMP-26, 0.36nM.2-4 Also inhibits MMP-10, MMP-13, MMP-15, MMP-17, MMP-20, MMP-21, TACE and ADAM19. Chemical Name: N-[(2R)-2-(Hydroxamidocarbonylmethyl)-4-methylpentanoyl]-L-tryptophan methylamide

Activity: DUB inhibitor . Function/Pharmacology: Abrogates the deubiquitinating activity of the 19S regulatory particle by inhibiting ubiquitin C-terminal hydrolase 5 (UCHL5) and ubiquitin-specific peptidase 14 (USP14) resulting in accumulation of polyubiquitin in cells. b-AP15 induces tumor cell apoptosis and tumor progression in four different solid tumor models in vivo. Chemical Name: 3,5-bis[(4-Nitrophenyl)methylidene]-1-prop-2-enoylpiperidin-4-one

Activity: PKCδ inhibitor . Function/Pharmacology: Reported to inhibit PKCδ selectively however this result has been called into question1. Displays neuroprotective effects2. Induces autophagy3. Cell permeable. Chemical Name: 3'-[(8-Cinnamoyl-5,7-dihydroxy-2,2-dimethyl-2H-1-benzopyran-6-yl)methyl]-2',4',6'-trihydroxy-5'-methylacetophenone

Activity: α2 adrenergic antagonist . Function/Pharmacology: Selective α2-adrenergic receptor antagonist1 (selectivity ratio of α2/α1 = 724)4 and imidazoline receptor antagonist2. Induces release of insulin in the rat insulinoma cell line RIN-5AH by interaction with ATP-sensitive potassium channels independently from imidazoline I1 or I2 receptors.3 Increases resting plasma insulin levels and markedly potentiates the rise in insulin levels produced by adrenaline in the rat.4 Chemical Name: 2-Ethyl-2-(imidazolin-2-yl)-2,3-dihydrobenzofuran, hydrochloride