trpm7

Fingolimod hydrochloride (FTY720) , a novel immune modulator, is a sphingosine 1-phosphate (S1P) antagonist (IC50: 0.033 nM in K562 and NK cells).

Mesendogen is an inhibitor of TRPM6. Mesendogen alters magnesium homeostasis, promotes mesoderm and definitive endoderm differentiation.

TRPM7-IN-1 (compound SUD) is a benzamide-urea derivative and an effective inhibitor of TRPM7. This compound induces cell cycle arrest and apoptosis in MCF-7 and BGC-823 cells, reducing their migration capabilities. It decreases vimentin expression while increasing E-cadherin expression. TRPM7-IN-1 reduces TRPM7-like currents and inhibits TRPM7 expression by activating the PI3K/Akt signaling pathway. This compound shows potential as a therapeutic agent for reducing breast and gastric cancer metastasis by targeting TRPM7 expression and activity.

AAL-149, an analog of FTY720 and a TRPM7 inhibitor (IC50 = 1.081 μM), exhibits multiple anti-inflammatory effects without targeting S1P receptors. It is applicable in anti-inflammatory research.

Xeniafaraunol A (compound 31) is a potent inhibitor of the transient receptor potential melastatin 7 (TRPM7) channel [1].

VPC01091.4 (VPC4) is a TRPM7 inhibitor that blocks TRPM7 current at low micromolar concentrations and serves as an efficacious anti-inflammatory agent, arresting systemic inflammation in vivo [1].

BTB 06061 is a TRPM7 inhibitor utilized in the study of ischemic diseases.

Scalaradial is an inhibitor of bee venom phospholipase A2 (PLA2) and TRPM ion channels (TRPM2) with IC50 values of 0.07 and 0.21 μM. It regulates ERK phosphorylation by inhibiting secretory PLA2 and Akt. Additionally, Scalaradial prevents the release of Arachidonic acid in mouse peritoneal macrophages induced by PMA.