All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Biological Description

Description: Leupeptin hemisulfate is a reversible, competitive serine/cysteine protease inhibitor. It is an orally active, antioxidant and anti-inflammatory agent.

Kinase Assay: Determination of BET Protein Binding Affinities to I-BET726: For determination of binding affinities to BET protein bromodomains, I-BET726 is titrated against truncates containing both BD1 and BD2 of BRD2 (10 nM), BRD3 (10 nM), and BRD4 (10 nM) in 50 mM HEPES pH7.5, 150 mM NaCl, 5% Glycerol, 1 mM DTT and 1 mM CHAPS in the presence of an Alexa 647 derivative (50 nM) of fluorescent ligand. After equilibrating for 1 h, the bromodomain protein: ligand interaction is detected using Time Resolved Fluorescence Resonance Energy Transfer (TR-FRET) following the addition of 1.5 nM europium chelate labeled anti-6His antibody. Plates are read using an Envision Plate reader (λEX = 337 nm, λEM = 615 nm, λEM = 665 nm; dual dichroic = 400 nm & 630 nm). These data are fitted to a four parameter IC50 model using Graphit data analysis software.

Chemical Properties

Molecular Weight: 951.2

Formula: C40H78N12O12S

CAS No.: 103476-89-7

Storage & Solubility Information

Storage

store at low temperture

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: 87 mg/mL (182.9 mM)

DMSO: 88 mg/mL (185 mM)

Ethanol: 88 mg/mL (185 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Catalog #: T6564

Please email us at cs@medikonia.com for any enquiry. To place an order, please include the catalog number(s) of the product(s) in the email.

References and Literature

1. Aoyagi T, et al. J Antibiot (Tokyo). 1969, 22(11), 558-568.

2. Morejohn LC, et al. Cell Biol Int Rep. 1985, 9(9), 849-857.

3. Ganapathi TR, et al. Plant Cell Rep. 2007, 26(9), 1575-1584.

4. Tao L, Cao Y, Wei Z, et al. Xanthatin triggers Chk1-mediated DNA damage response and destabilizes Cdc25C via lysosomal degradation in lung cancer cells[J]. Toxicology and applied pharmacology. 2017 Dec 15;337:85-94.

5. Jiang T Y, Pan Y F, Wan Z H, et al. PTEN status determines chemosensitivity to proteasome inhibition in cholangiocarcinoma[J]. Science Translational Medicine. 2020, 12(562).