INO-4995 has potential in treatment of Cystic Fibrosis (CF)
INO-4995 (1-O-octyl-2-O-butyryl-D-myo-inositol 3,4,5,6-tetrakisphosphate octakis(propionoxymethyl)ester) is an ion channel modulator that is slowly metabolized in cells. Studies have shown that it inhibits ENaC activity while promoting expression of the calcium-activated chloride channel, TMEM16a, in membranes. Thus it has potential therapeutic activity in the treatment of cystic fibrosis where it normalized nasal potential difference (NPD) in a murine CF knock-out model and promoted fluid secretion in human CF airway epithelia.
Strong preclinical efficacy of INO-4995: a membrane-permeant Inositol-phosphate derivative has potential in treatment of Cystic Fibrosis (CF)
This graph is showing the difference in NPD between mice before and after 4-day treatment with INO-4995 (0.0008mg/kg):
Am J Respir Cell Mol Biol 2010, 42(1), 105
PDP3: New Tool to study the biology of Protein Phosphatase-1 (PP1)
SiChem expanded its portfolio toward peptides: PP1-Disrupting Peptides (PDPs) can be used as selective tools to study acute and long-term effects of PP1 activation in intact cells. This membrane-permeant peptide competes with endogenous, the motif RVxF containing PIPs to bind to PP1 in living cells. This PDP3 does not bind to the closely related phosphatase PP2A.
In addition, PDPs can be used to sensitize cells for clinically relevant kinase inhibitors (SC-0100)
Rapidly reversible Chemical Dimerizer rCD1 is now available at SiChem
The first rapidly reversible chemical dimerization system – rCD1 - , which permits to determine kinetics of lipid metabolizing enzymes in living cells, is now available at SiChem . This new system was applied to induce and stop the activity of phosphatidyl 3-kinase (PI3K) (product information) rCD1 is available in 2 sizes: 100µg (for app. 20 experiments) and 500µg (SC-7000)
Chemical Dimerizer rCD1
A representative time-lapse fluorescence movie of HeLa cells co-transfected
with NLS2-SNAPf-ECFP and mRFP-FKBP constructs. rCD1 (1 μM) induces
translocation of mRFP-FKBP into the nucleus; addition of FK506 (1 μM) leads to
release of mRFP-FKBP from the nucleus !
Mayor of Bremen visits SiChem
In his series of company visits in Bremen, Mayor Jens Böhrnsen visited on June 4 SiChem. After a tour through the new laboratories of SiChem and a detailed discussion about the current situation and the former founding situation in 2001, the mayor was very impressed. He complimented the created high-tech jobs and entrepreneurial spirit - it is important and necessary to transfer this entrepreneurial spirit to new potential founders. (more about the mayor's visit)
Mayor Jens Böhrnsen, Dr. Hartmut Gillandt (SiChem, left.), Dr. Ralph Baumheier (Senatskanzlei, centre),
Dr. Miriam Rittner (SiChem) im Labor [Foto: Senatspressestelle]
New Click-Amino Acids for In Vivo Protein Labeling - now available at SiChem !
There is a growing demand in advanced fluorescence microscopy for small and highly photostable fluorescent probes. These probes consists of unnatural clickable Amino Acids (UAAs) which can be labeled in vivo with a clickable dye. The corresponding click-Amino Acids are now available at SiChem.
Insulin Receptors - expressed with two unnatural amino acids (UAAs) TCO*1 (TCOstar) and SCO labeled with Cy5-CH3-Tetrazin (cyan) und Atto532-H-Tetrazin (magenta) (Nikic et al. Angew. Chem. Int. Ed. 2014, 53 (8): 2245)
Custom synthesis and Lifescience tools made by SiChem
Sirius Fine Chemicals SiChem GmbH synthesizes APIs for early stage (Toxicology) drug design. A special field of expertise is the preparation of biologically and pharmacologically active compounds with increased bioavailability (prodrugs).
We are one of the leading providers for inositol phosphates as well as a large variety of membranepermeant and photoactivatable derivatives. Our portfolio has recently been supplemented by clickable unnatural amino acids and other useful tools for Click-Chemistry.
SiChem was founded in 2001 by Hartmut Gillandt, Miriam Rittner, Tanja Meyerdierks, and Carsten Schultz as a Spin-Off from the University of Bremen.