BMP-22 is an inhibitor of autotaxin (IC50 = 170 nM). It is selective for autotaxin over the phosphodiesterases NPP6 and NPP7 at 10 μM. BMP-22 (0.1-1,000 nM) inhibits autotaxin-mediated production of lysophosphatidic acid (LPA) from lysophosphatidylcholine in vitro in a concentration-dependent manner. It inhibits LPC-dependent MM1 cell invasion of a human umbilical vein endothelial cell (HUVEC) monolayer. BMP-22 (0.5 mg/kg per day) decreases the number of lung metastatic foci in a B16/F10 syngeneic mouse melanoma model of lung metastasis.
SB02024 is a VPS34 inhibitor. SB02024 activates cGAS-STING signaling and sensitizes tumors to STING agonist. SB02024 blocked autophagy in vitro and reduced xenograft growth of two breast cancer cell lines, MDA-MB-231 and MCF-7, in vivo. Vps34 inhibitor significantly potentiated cytotoxicity of Sunitinib and Erlotinib in MCF-7 and MDA-MB-231 in vitro in monolayer cultures and when grown as multicellular spheroids. Our data suggests that inhibition of autophagy significantly improves sensitivity to Sunitinib and Erlotinib and that Vps34 is a promising therapeutic target for combination strategies in breast cancer.
1-Palmitoyl-d9-2-palmitoyl-sn-glycero-3-PE serves as an internal standard for the quantification of 1,2-dipalmitoyl-sn-glycero-3-PE (1,2-DPPE) using GC- or LC-MS. 1,2-DPPE, a prevalent PE (phospholipid), contains C16:0 fatty acids at the sn-1 and sn-2 positions and is essential in the inner plasma membrane leaflet. This compound forms a condensed lipid monolayer with cholesterol through tight hydrogen bonding between 1,2-DPPE headgroups, enhancing membrane fluidity to support transport and signaling.
1,2-Dipalmitoyl-sn-glycero-3-N,N-dimethyl-PE is a derivative of 1,2-dipalmitoyl-sn-glycero-3-PE (1,2-DPPE) with two added methyl groups on its sn-3 moiety, which in aqueous suspensions, reduces the phase transition temperature relative to those of 1,2-DPPE and 1,2-dipalmitoyl-sn-glycero-3-N-methyl-PE (1,2-NMeDPPE). It is utilized in creating liposomes and monolayers for investigating membrane permeability and monolayer viscosity.
4beta-Hydroxywithanolide E(4bHWE) can inhibit the growth of colon cancer monolayer and spheroid cultures, it assert its anti-tumor activity in carcinogenic progression and develop into a dietary chemopreventive agent, it affects alternative splicing by mo