Activators & Inhibitors

Activity: Microtubule depolymerizer . Function/Pharmacology: Ansamitocin P3 (66547-09-9) is a fungal metabolite from Actinosynnema pretiosum which binds to the phomopsin A/rhizoxin site on tubulin1,2. Ansamitocin P3 is a maytansine analog which displays potent cytotoxicity against various human tumor cell lines2,3. Maytansine and its analogs cause extensive disassembly of microtubules and totally prevent tubulin spiralization4. Chemical Name: null

Activity: Anticancer agent . Function/Pharmacology: Induces intra- and interstrand DNA adducts which poison topoisomerase I.1 Synergizes with topoisomerase I inhibitors such as topotecan.1 Induces apoptosis by sequential activation of caspase-8, -3 and -6 in osteosarcoma cells.2 Inhibits expression of X-linked inhibitor of apoptosis protein (XIAP) in human LNCaP cells.3 Numerous mechanisms inhibit propagation of cisplatin-induced DNA damage to signal apoptosis resulting in resistance.4 Clinically useful anticancer agent. Chemical Name: Cis-Diaminodichloroplatinum

Activity: SR calcium release inhibitor . Function/Pharmacology: Inhibits release of Ca2+ from sarcoplasmic reticulum via inhibition of ryanodine receptor channels with selectivity for RYR1 and RYR3 over RYR2.1 Protects against quisqualate and NMDA-induced cytotoxicity in cultured cerebral cortical neurons.2 Displays neuroprotective effects.3 Prevents cell death in neural progenitor cells derived from Wolfram syndrome iPS cells.4 Chemical Name: 1-[(5-(p-Nitrophenyl)furfurylidene)amino]hydantoin sodium salt

Activity: Iron Chelator antioxidant . Function/Pharmacology: Hinokitiol is a potent metal chelator that induces differentiation and apoptosis in teratocarcinoma F9 cells.1 It acts as a reversible inhibitor of platelet-type 12-lipoxygenase (IC50 = 100 nM).2 Reported to have strong antibacterial activity3, suppress cell growth and disrupt androgen receptor signaling4 and activate hypoxia-inducible factor5. Chemical Name: β-Thujaplicin, 2-Hydroxy-4-isopropyl-2,4,6-cycloheptatrien-1-one

Activity: Serine protease inhibitor . Function/Pharmacology: A serine protease inhibitor inhibiting plasmin, kallikrein, thrombin as well as trypsin, which attenuates pancreatic fibrosis.1 Reduces weight gain and improves metabol-ism in obese rodent models.2 In clinical use (in Japan) for pancreatitis.3 Inhibits influenza virus replication in human tracheal epithelial cells.4 Reduces infection of Calu-3 lung cells by SARS-CoV-2 (responsible for COVID-19) via inhibition of the serine protease TMPRSS2 required for viral spike protein priming.5 Chemical Name: 4-[[6-[(Aminoiminomethyl)amino]-1-oxohexyl]oxy]benzoic acid, ethyl ester, methanesulfonate

Activity: Actin depolymerizing agent . Function/Pharmacology: A novel marine natural product which binds to actin in a 1:1 molar ratio (Kd=13-20 nM).1 It selectively and completely depolymerizes F-actin to G-actin via a novel mechanism different from that of the cytochalasin D.2 It is a novel and specific inhibitor of actomyosin ATPase.3 Chemical Name: From Mycale sp.

Activity: Selective plasma kalikrein inhibitor . Function/Pharmacology: Selective plasma kallikrein inhibitor (Ki = 0.81 µM)1 that can be used for affinity purification of kalikrein2. Synergizes with NO donors to produce antithrombic effects ex-vivo.3 Suppresses collagen-induced arthritis in mouse models.4 Chemical Name: trans-4-Aminomethylcyclohexanecarbonyl-phenylalanyl-4-carboxymethylanilide

Activity: Mitochondrial benzodiazepine receptor ligand . Function/Pharmacology: PK-11195 is a selective and potent peripheral benzodiazepine receptor, PBR (or TSPO, translocator protein) antagonist.1,2 It has been shown to chemosensitize tumor cells to a variety of chemotherapeutic agents via PBR-independent pathways.3,4 PK11195 is also able to induce apoptosis in a variety of cell lines.5-7 Chemical Name: 1-(2-Chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinolinecarboxamide

Activity: Immunomodulator; IDO2 inhibitor . Function/Pharmacology: A indoloquinazoline alkaloid found in various plant species and possessing intriguing pharmacological activities.1 Suppresses activation of BV2 microglia cells following LPS treatment and reduces production of proinflammatory cytokines via Nrf2, HO-1 and NFκB signaling.2 Displays antiinflammatory activity targeting IL-17.3 Inhibits indoleamine 2,3-dioxygenase 2 (IDO2) with an IC50 of 5-17 μM.4 Induces growth inhibition and neuronal differentiation in human neuroblastoma LA-N-1 cells.5 Chemical Name: Indolo(2,1-b)quinazoline-6,12-dione