LTβR-IN-1

LTβR-IN-1 (Compound 919278) is a potent, selective lymphotoxin β receptor (LTβR) inhibitor. LTβR-IN-1 also selectively inhibits the nuclear translocation of p52 depended on TNF12A, instead of the nuclear translocation of p65 mediated by TNF-α receptor. LTβR-IN-1 regulates the NF-kB signaling pathway IN a ligand-independent manner^[1]. IC50 & Target:LTβR; p52 translocation; MAP3K14; NF-κB^[1] In Vitro:LTβR-IN-1 (compound 919278) (1 nM-100 μM; 30 min) inhibits p52 nuclear translocation in response to stimulation with Anti-LTβR or TWEAK (20 ng/mL, respectively; 4 h) with IC₅₀s of 0.169 μM and 0.167 μM, respectively^[1].
LTβR-IN-1 (3 nM-30 μM; 45 min) reduces the binding affinities of both CDK12 and its associated protein, CCNK in both TWEAK-stimulated and control U-2 OS cells, with IC₅₀s of 50-61 nM for CDK12 and 29-68 nM for CCNK, respectively^[1].
LTβR-IN-1 reduces the mRNA abundance of MAP3K14 in with an IC₅₀ value of 0.32 μM in U-2 OS cells^[1].
LTβR-IN-1 (1-10 μM; 30 min) decreases the phosphorylation of serine-2 (Ser2) on the C-terminal domain (CTD) of RNA polymerase (Pol) II^[1].
LTβR-IN-1 regulates the noncanonical pathway in a ligandindependent manner and selectively inhibits the noncanonical pathway while sparing the canonical NF-kB signaling pathway^[1].