Activators & Inhibitors

Activity: Cysteine protease inhibitor . Function/Pharmacology: Cell-permeable, epoxysuccinyl peptide irreversible inhibitor of calpain and other cysteine proteases.1,2 Inhibits calpain-dependent apoptosis pathway in T cells3 but promotes heat-induced apoptosis in FM3A cells. Typical working concentration is 0.5-10 µg/ml.4 Chemical Name: (2S.3S)-trans-Epoxy succinyl-L-leucylamido-(4-guanidino) butane

Activity: Trypsin-like cysteine protease inhibitor . Function/Pharmacology: A reversible inhibitor of trypsin-like proteases and cysteine proteases. Inhibits trypsin, plasmin, papain and cathepsin B, H and L.1-3 Blocks various apoptotic pathways in T cells.4 Commonly used in cell lysis buffers to protect proteins from degradation. Typical working concentration is 1µM (0.5 µg/ml). Chemical Name: Ac-Leu-Leu-Arg-CHO, hemisulfate

Activity: Cysteine protease inhibitor . Function/Pharmacology: Cell-permeable derivative of E-64c, an inhibitor of calpain and other cysteine proteases, such as papain, cathepsin B and cathepsin L.1,2 Addition to cell cultures should be done in serum-free media as esterases in serum will cleave the ethyl ester and reduce cell permeability. Typical working concentration is 0.5-10 µg/ml. Inhibits degradation of autophagic cargo inside autolysosomes3 Chemical Name: 2S,3S-trans-(Ethoxycarbonyloxirane-2-carbonyl)-L-leucine-(3-methylbutyl)amide

Activity: Protease inhibitor . Function/Pharmacology: Irreversible inhibitor of serine proteases including trypsin, chymotrypsin, plasmin, plasma kallikrein and thrombin. Stable, non-toxic and water-soluble alternative to PMSF1. Typical working concentrations are 0.1-1 mg/ml. May be used in cell culture or in cell lysis buffers. Inhibits NADPH oxidase activation2. Chemical Name: 4-(2-Aminoethyl)benzenesulfonyl fluoride hydrochloride

Activity: Calpain inhibitor . Function/Pharmacology: Cell-permeable, peptide aldehyde inhibitor of calpain (calpain I, Ki = 120 nM, calpain II, Ki = 230 nM) and other neutral cysteine proteases. Potent inhibitor of cathepsin L (Ki=0.6 nM) and cathepsin B (Ki=100 nM).1 Weak inhibitor of the chymotrypsin-like activity of the proteasome.2 Cell permeable. Chemical Name: N-Acetyl-Leu-Leu-Methional

Activity: p53/mdm2 inhibitor . Function/Pharmacology: MDM2 antagonist; inhibits the MDM2-p53 interaction (IC50 = 0.09 μM) and activates p531. Displays antiproliferative activity and induces apoptosis in a variety of tumor cells2-4. Chemical Name: (±)-4-[4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxy-phenyl)-4,5-dihydro-imidazole-1-carbonyl]-piperazin-2-one

Activity: DUB inhibitor . Function/Pharmacology: A novel DUB inhibitor directly inhibiting USP9x, USP5, USP14 and UCH37 inducing rapid accumulation of polyubiquitinated proteins. Triggers tumor cell apoptosis.1 Blocks Jak2 signaling via Jak2 ubiquitination.2 Causes ablation of the oncogenic transcription factor ERG in prostate cancer cells.3 Chemical Name: (S,E)-3-(6-bromopyridin-2-yl)-2-cyano-N-(1-phenylbutyl)acrylamide

Activity: Cdc25 phosphatase inhibitor . Function/Pharmacology: Potent, selective and irreversible inhibitor of CDC25 phosphatases, Ki=29, 95 and 89 nM for human CDC25A, B2 and C respectively and >20- and >450-fold selective over VHR and PTP1B1. Arrests cells at G1 and G2/M and inhibits cdk1 and 2 activation2. Inhibits the growth of a variety of human tumor cell lines3. Acts via irreversible oxidation of the catalytic cysteine of CDC254. Chemical Name: 6-Chloro-7-[[2-(4-morpholinyl)ethyl]amino]-5,8-quinolinedione

Activity: N-WASP inhibitor . Function/Pharmacology: A selective, reversible inhibitor of neural Wiskott-Aldrich syndrome protein (N-WASP) activity1. Binds to the regulatory domain of N-WASP and inhibits activation of Arp2/3 complex by forcing N-WASP into an inactive conformation2. Inhibits PIP2-induced actin polymerization (EC50=4 μM). Perturbs agrin-elicited acetylcholine receptor clustering3. Inhibits the formation of dendritic spines and synapses in hippocampal neurons4. Chemical Name: 1-(3,6-Dibromocarbazol-9-yl)-3-dimethylaminopropan-2-ol