lx-3

LX-3 is a selective activator of the p38 mitogen-activated protein kinase (MAPK) pathway, which de-represses a subset of endogenous genes repressed by DNA methylation.

RLX-33 is a potent and selective antagonist of relaxin family peptide 3 (RXFP3) that crosses the blood-brain barrier and also blocks relaxin 3-induced ERK1 2 phosphorylation. RLX-33 can block the increase in food intake induced by the RXFP3 selective agonist R3 I5 in rats.RLX-33 can be used to study the metabolic syndrome.

PLX-3618 is a monovalent direct degrader capable of degrading BRD4 with a DC50 of 12.2 nM. It promotes the polyubiquitination and subsequent proteasomal degradation of BRD4 by recruiting the E3 ubiquitin ligase substrate receptor DCAF11. Furthermore, PLX-3618 inhibits the proliferation of various cancer cells and induces apoptosis in AML cells. It also demonstrates anti-tumor activity against AML in mouse models.

Dual Galectin-3 EGFR-IN-1 (Compound 29) is a dual inhibitor targeting Galectin-3 and EGFR, with dissociation constants (KD) of 52.29 μM and 3.31 μM, respectively. It inhibits TGF-β-induced hepatic stellate cell (HSC) activation, induces apoptosis in LX-2 cells, and shows antifibrotic activity in the liver.

C18 dihydro Ceramide is a bioactive sphingolipid and precursor in the de novo synthesis of C18 ceramide that lacks the 4,5-trans double bond. [1] Increased C18 dihydroceramide lipid levels lead to increased triacylglycerol storage and autophagosome accumulation as well as upregulation of the fibrosis markers α-SMA and FGF2 in Chang and LX-2 liver cells. C18 dihydro Ceramide is elevated in the plasma of pre-diabetics up to 9 years prior to the onset of type 2 diabetes. [2] It is also elevated in the skin of patients with lesional atopic dermatitis.[3]

LX2343 is a BACE1 enzyme inhibitor with an IC50 value of 11.43±0.36 μM and acts as a non-ATP competitive PI3K inhibitor with an IC50 of 15.99±3.23 μM. Additionally, LX2343 stimulates autophagy, promoting Aβ clearance.

LX-039 is a potent, selective, orally active estrogen receptor degrader (EC50: 2.99 nM) with antitumor effects.LX-039 has indole C-3 chloride atoms.LX-039 has good pharmacokinetic properties in mice, low clearance, high blood levels and oral exposure.