Interested in a Reliable Source for Unique & Rare Small Molecules

news July 20 2020

New, unique and rare small molecules for Obesity, Cancer, Immuno-Oncology, & Infection Research.

Synthetic Antibiotics Effective Against Antibiotic-Resistant (MDR) Pathogens / Biofilm Modifying Agents

PK150 (Sorafenib Analog)

PK150 is a potent antibiotic against several pathogenic strains, including Methicillin-sensitive S. aureus (MSSA), Methicillin-resistant S. aureus (MRSA) and Vancomycin intermediate S. aureus (VISA). PK150 did not induce in vitro resistance and shows oral bioavailability and in vivo efficacy. PK150 interfers with the menaquinone biosynthesis by inhibiting demethylmenaquinone methyltransferase and efficiently reduces biofilms.

MAC-545496 

MAC-545496 is a potent antimicrobial agent against MRSA that works as a synthetic antibiotic adjuvant, antivirulence and antibiofilm agent. The mode of action includes the inhibition of GraR, a regulator of cell-envelope stress response.

Extracellular Vesicle Release Inhibitor Manumycin A 

Manumycin A  is an antibiotic that acts as a potent and selective farnesyltransferase (FTase) inhibitor with anti-tumor activity. Due to the involvement of Ras during exosomes release, manumycin A has been investigated as an inhibitor of exosomes secretion.

Potent Proteasome Inhibitor Salinosporamide A (Marizomib)

Salinosporamide A is a potent, irreversible inhibitor of all the 3 proteolytic activities of the mammalian 20S proteasome, β5 subunit: chymotrypsin-like (EC50 = 3.5nM), β2 subunit: trypsin-like (EC50 = 28nM) and β1 subunit: caspase-like or peptidyl-glutamyl peptide-hydrolyzing (PGPH) (EC50 = 430nM). It is a potent anticancer agent that triggers apoptosis, with distinct proteasome activity and mechanism of action compared to Bortezomib (Velcade).

Potent Autophagy Inducer Seriniquinone

Seriniquinone is a potent cytotoxic and melanoma-selective anticancer agent. Seriniquinone inhibits cell proliferation marked by autophagocytosis and induces cell death due to caspase-9 dependent apoptosis. Mode of action studies suggest that it specifically targets the skin protective antimicrobial peptide dermcidin (DCD), whose role as a cancer-protective protein has been recognized recently.

Potent & Selective NAE Inhibitor MLN4924

MLN4924  is a potent, selective and cell permeable inhibitor of Nedd8 E1 activating enzyme (IC50=4.7nM). NEDD8 is required to activate cullin-RING ubiquitin E3 ligases (CRLs) responsible for the ubiquitination and proteasome-dependent turnover of certain substrates relevant to cancer cell survival. In addition to its anticancer properties, MLN4924 has been proven to be a broad and potent antiviral agent.

Potent & Selective Gαq Family Inhibitor YM-254890

YM-254890  inhibits the signal transduction of Gαq, Gα11 and Gα14 (IC50=0.095μM) by blocking the exchange of GDP for GTP, preventing the activation of the G protein. Gαq signaling has been shown to regulate brown/beige adipocytes using the structurally similar specific Gαq family inhibitor FR900359. It is suggested that inhibition of this pathway may be a novel therapeutic approach to combat obesity.