polarized

SR33805 is a potent antagonist of Ca2+ channel(EC50s of 4.1 nM and 33 nM in depolarized and polarized conditions, respectively)

7β,27-dihydroxy Cholesterol is an oxysterol and agonist of retinoic acid receptor-related orphan receptor γ (RORγ) and RORγt. [1] It activates RORγ- or RORγt-dependent signaling with EC50 values of 691 and 1,045 nM, respectively, in reporter assays using HEK293T cells expressing the recombinant human receptors. 7β,27-dihydroxy Cholesterol is selective for RORγ and RORγt over a panel of eight additional nuclear receptors at 30 µM. It increases IL-17A production in Th17-polarized isolated human na ve CD4+ T cells when used at a concentration of 300 nM. 7β,27-dihydroxy Cholesterol (60 mg/kg) increases IL-17A production in isolated mouse γδ T cells stimulated with 12-myristate 13-acetate and ionomycin .

Potent and selective GPR84 biased agonist (EC50 = 33 nM). Exhibits no significant activity in a panel of 168 other GPCRs. Exhibits bias for G protein signaling pathways. Induces morphological changes in primary murine bone marrow-derived macrophages (BMDMs) in a cellular impedance assay, and promotes phagocytosis by M1 polarized U937 cells. Induces migration of primary human monocytes, but has no effect on macrophage chemotaxis.

CRT-0066854 is a PKCι and PKCζ inhibitor. CRT0066854 was able to restore polarized morphogenesis in the dysplastic H-Ras spheroids.

Endosidin-2 is an exocyst inhibitor, a cell-permeable benzylidene benzoylhydrazine, that binds to the exocyst component of the 70 kDa (EXO70) subunit of the exocyst complex (Kd = 253 μM, EXO70A1).Endosidin-2 disrupts protein translocation between the endosomes and plasma membrane, thereby facilitating translocation of proteins to the vesicle for degradation. It also inhibits recirculation of endocytosed transferrin to the plasma membrane in HeLa cells and targets multiple isoforms of mammalian EXO70, leading to dysregulation of exocytosis.Endosidin2 can be used as a tool molecule to study cytosolization.