69 products were found matching "K02737"!

Lactacystin is a microbial metabolite isolated from Streptomyces that is now widely used as a selective inhibitor of the 20S proteasome. Lactacystin was first characterized by its ability to induce differentiation and inhibit cell cycle progression in several tumor cell lines. At concentrations from 2 to 10 µM,...

PI-1840 is an inhibitor of chymotrypsin-like (CTL) proteasome activity (IC50 = 27 nM). It is selective for the CTL activity over the trypsin-like (TL) and peptidylglutamyl peptide hydrolyzing (PGPH) activities (IC50s = >100 µM for both), as well as for the 20S constitutive proteasome over the immunoproteasome (IC50s...

Bortezomib is a dipeptide boronic acid derivative that reversibly inhibits the 20S proteasome (Ki = 0.6 nM). It binds the beta5-subunit of the 20S proteasome and selectively inhibits chymotryptic activity. In part by blocking the degradation of tumor-suppressing and proapoptotic proteins, bortezomib drives cell...

Lactacystin is a microbial metabolite isolated from Streptomyces that is now widely used as a selective inhibitor of the 20S proteasome. Clasto-lactacystin beta-lactone was later identified as the active metabolite of lactacystin, resulting from the elimination of cysteine and the formation of a reactive...

White solid. Soluble in DMSO, ethanol or methanol. Slightly soluble in water. Highly potent, selective and reversible cell permeable inhibitor of the proteasome. Inhibits the chymotrypsin-like and caspase-like peptidase activity of the proteasome, Calpain and cathepsin inhibitor, Autophagy activator, Anticancer...

Solid lyophilized powder. Soluble in DMSO. Fluorogenic substrate for measuring the chymotrypsin-like peptidase activity of the 20S proteasome, calpains and other chymotrypsin-like proteases, Extinction: 380nm. Emission: 460 nm, This substrate is useful for inhibitor screening and kinetic analysis.

White to off-white solid. Soluble in DMSO. Insoluble in water. Antibiotic, Potent anticancer compound, Cell permeable, potent, selective and irreversible 20S proteasome inhibitor. Predominantly inhibits the chymotrypsin-like (CTRL) activity of the proteasome. Exhibits lower level inhibition of proteasome...

Carfilzomib is a second-generation, irreversible, peptide epoxyketone class proteasome inhibitor that targets the chymotrypsin-like beta5 subunit of the constitutive 20S proteasome (IC50 = 5.2 nM) and the beta5i subunit of the immunoproteasome 20Si (LMP7, IC50 = 14 nM) with minimal cross reactivity to other...

Suc-Leu-Leu-Val-Tyr-AMC is a fluorescent substrate for the 20S proteasome, other chymotrypsin-like proteases, and calpains (excitation max: 360 nm, emission max: 460 nm).Formal Name: N-(3-carboxy-1-oxopropyl)-L-leucyl-L-leucyl-L-valyl-N-(4-methyl-2-oxo-2H-1-benzopyran-7-yl)-L-tyrosinamide. CAS Number: 94367-21-2....

Ac-WLA-AMC is a fluorogenic substrate for the beta5c subunit of the 20S proteasome. Upon cleavage, 7-amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify the activity of the beta5c subunit of the 20S proteasome. AMC displays excitation/emission maxima of 351/430 nm,...

Induces neuritogenesis, Potent and selective irreversible proteasome inhibitor. Specifically inhibits 20S proteasome (MCP, multicatalytic complex). Blocks proteasome activity by targeting the catalytic beta-subunit, apoptosis inducer, anticancer compound, upregulates HSP70 and HSP22, induces differentiation and...

Salinosporamide A is a natural proteasome inhibitor. It is a beta-lactone-gamma-lactam that irreversibly inhibits all three protease activities within the proteasome (IC50s = 3.5, 28, and 430 nM for beta5 (chymotrypsin), beta2 (macropain), and beta1 (C5) subunits, respectively), both in vitro and in vivo....