Activators & Inhibitors

Activity: SREBP activation inhibitor . Function/Pharmacology: Blocks adipogenesis by inhibiting the activation of SREBP. Inhibits the ER-Golgi translocation of SREBPs via binding to their escort protein (SCAP). Prevents increases in body weight, blood glucose and hepatic fat accumulation in obese ob/ob mice1. Inhibits high glucose-induced TGF-β in mesangial cells2. Cell permeable. Chemical Name: 2-(2-Propylpyridin-4-yl)-4-(p-tolyl)thiazole

Activity: E3 UB ligase inhibitor . Function/Pharmacology: Small Molecule Enhancer of Rapamycin 3 (SMER3) is a specific inhibitor if the ubiquitin E3 ligase SCFMET30 both in vitro and in vivo. Chemical Name: 9H-Indeno[1,2-e][1,2,5]oxadiazolo[3,4-b]pyrazin-9-one

Activity: Neurogenic differentiation inducer . Function/Pharmacology: Pomotes neurogenesis in vivo enhancing the proliferation and differentiation of hippocampal subgranular zone neuroblasts and enhances memory.1 Induces robust neuronal differentiation in adult neural stem cells.2 Increases insulin production by pancreatic β cells.3 ISX9 blocks malignant astrocyte proliferation, downregulates their astrocyte character, induces reentry into the cell cycle and upregulates neuronal gene expression.4 Induces sensory neurons rom neuroepithelial stem cells.5 Potentiates cell proliferation and neuronal commitment in the rat dentate gyrus.6 Chemical Name: N-cyclopropyl-5-(2-thienyl)-3-isoxazolecarboxamide

Activity: Prostaglandin E (EP) agonist . Function/Pharmacology: Prostaglandin E2 (PGE2) is an endogenous prostaglandin derived from the action of cyclooxygenase on arachidonic acid. PGE2 has diverse biological actions in the areas of inflammation, cancer, immune modulation, fertility, smooth muscle relaxation and hematopoietic stem cell homeostasis. PGE2 acts through four distinct receptors: EP1, EP2, EP3, EP4. Chemical Name: (5Z,11α,13E,15S)-11,15-Dihydroxy-9-oxoprosta-5,13-dienoic acid

Activity: PIM1 inhibitor . Function/Pharmacology: A selective, ATP-competitive inhibitor of the Pim protein kinases (IC50 = 24 and 100 nM for Pim-1 and Pim-2 respectively). Selective over a panel of ~50 other kinases1. Induces cell cycle arrest in leukemia and prostate cancer cells2. Blocks the growth of a wide range of myeloid and lymphoid cell lines with precursor T-cell lymphoblastic leukemia/lymphoma (pre-T-LBL/T-ALL) being highly sensitive3. A useful tool for exploring the involvement of Pim in cellular signaling4. Cell permeable. Chemical Name: 5-(3-Trifluoromethylbenzylidene)thiazolidine

Activity: LSF inhibitor . Function/Pharmacology: Inhibitor of transcription factor LSF specifically targeting its DNA binding and corresponding transcriptional activity (IC50=2.1 M). Rapidly induces apoptosis in an aggressive hepatocellular carcinoma (HCC) cell line and dramatically inhibits tumor growth in a mouse xenograft model with no general tissue cytotoxicity.1,2 In human HCC cells, FQI1 induced mitotic arrest with an accompanying increase in cyclin B1.3 Blocks LSF-stimulated activation of DNA methyltransferase 1.4 Cell permeable. Chemical Name: 8-(2-Ethoxyphenyl)-7,8-dihydro-[1,3]dioxolo[4,5-g]quinoline-6(5H)-one

Activity: Bromodomain inhibitor . Function/Pharmacology: JQ1 is a potent BET bromodomain inhibitor. IC50 = 17.7, 32.6, 76.9 and 12942 nM respectively for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP respectively. Competitive binding by JQ1 displaces the BRD4 fusion oncoprotein from chromatin, prompting squamous differentiation and specific antiproliferative effects in BRD4-dependent cell lines and patient-derived xenograft models establishing proof-of-concept for targeting protein-protein interactions of epigenetic readers1. Chemical Name: (6R,S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid 1,1-dimethylethyl ester

Activity: Mitochondria-targeted antioxidant . Function/Pharmacology: A mitochondria-targeted antioxidant. Displays cardio- and neuroprotective effects1. Displays beneficial effects in mouse models of Alzheimer’s disease2. Protects pancreatic β-cells against oxidative stress and improves insulin secretion3. Cell permeable. Chemical Name: 10-(6’-Ubiquinonyl)decyltriphenylphosphonium bromide

Activity: Ub-ligase inhibitor . Function/Pharmacology: TAME binds to the ubiquitin ligase anaphase-promoting complex (APC) preventing its activation by Cdc20 and Cdh1 and resulting in mitotic arrest.1,2 Chemical Name: N-p-Tosyl-L-arginine methyl ester hydrochloride