VD/VDR Agonist

LG190155 is a nonsteroidal vitamin D receptor (VDR) agonist. LG190155 activates VDR in mesenchymal stem cells, thereby upregulating the BMP6-IL6 autocrine axis. Pretreatment of mesenchymal stem cells with LG190155 significantly enhances their ability to induce differentiation of acute myeloid leukemia cells, without inducing hypercalcemia. LG190155 is applicable to research related to acute myeloid leukemia (AML).

ZG-126 is an agonist for vitamin D receptor (VDR) and an inhibitor for histone deacetylase (HDAC) (IC₅₀=0.63-67.6 μM). ZG-126 exhibits cytotoxicity in cancer cells MDA-MB-231 and 4T1. ZG-126 exhibits antitumor and anti-metastatic efficacy against melanoma and triple-negative breast cancer (TNBC) in mouse models. ZG-126 also exhibits anti-inflammatory activity, through the reduction of macrophage infiltration and immunosuppressive M2-polarization.

Ro-65-2299 is an orally active retiferol Vitamin D analogue and a potential VDR agonist (ED₅₀ = 180 nM). Ro-65-2299 can induce thickening of the epidermis and exhibits antipsoriatic effect in hairless mice (ED₅₀ = 7.5 mg/kg). Ro-65-2299 can be used for the researches of inflammation and immunology, such as psoriasis.