sk-1-i

TASK-1-IN-1 is a potent and selective inhibitor of TASK-1 (Potassium Channel) with an IC50 of 148 nM, and exhibits a reduced inhibitory effect on the TASK-3 channel with an IC50 of 1750 nM. TASK-1-IN-1 also demonstrates anticancer effects.

BML-258 HCl was removed and discontinued.

Scyllatoxin (Leiurotoxin I), a peptide toxin derived from the venom of the scorpion (Leiurus quinquestriatus hebraeus), acts as a blocker of small-conductance K Ca (SK) channels. It notably enhances the release of norepinephrine (NE) and epinephrine (Epi) in vivo [1].

Dendrogenin A (DDA) is a compound acting as a selective liver X receptor (LXR) modulator, cholesterol epoxide hydrolase inhibitor (Ki = 120 nM), and a metabolic product of cholesterol, originating from 5,6α-epoxy cholesterol through histamine conjugation via DDA synthase. This compound is present in non-cancerous human mammary epithelial cells and melanocytes, but absent or minimally present in various breast carcinoma, melanoma cells, and isolated human breast tumor tissues. DDA impedes the activation of LXRβ and LXRα induced by 22(R)-hydroxy cholesterol (IC50s = 76 and 362 nM, respectively), yet it also functions as a partial LXR agonist, boosting the protein levels of Nur77, NOR-1, LC3-I, and LC3-II in B16/F10 murine melanoma cells. It shows a preference for LXRα and LXRβ modulation while displaying selectivity over other receptors including pregnane X receptor (PXR), and various others at a concentration of 2.5 µM. Moreover, DDA enhances LC3-II protein levels in cancer cells and prompts autophagic cell death at specific concentrations. Notably, DDA (0.37 µg/kg) has been shown to diminish tumor growth in melanoma and mammary cancer murine models and promotes cancer cell differentiation both in vitro and in vivo.