TL4-12

TL4 12 is a potent and selective GCK (germinal center kinase) inhibitor. TL4 12 shows antiproliferation activity. TL4 12 induces apoptosis and cell-cycle arrest in the G0/G1 phase. TL4-12 decreases the protein expression of IKZF1, c-MYC, and BCL-6 and increases the expression of p53 level. TL4 12 has the potential for the research of RAS-mutated multiple myeloma^[1]. In Vitro: TL4 12 (0-5 µM; 4 days) shows antiproliferation activity with an IC₅₀ value of 37 nM for MM cells, and with IC₅₀s of 1.62, 3.7, 4.4, 5.7, 10, 32, 49, 19 µM for JJN3, MM1.S, H929, RPMI-8226, MOLP-8, SKMM2, LP-1, U266 cells, respectively^[1].
. TL4-12 (0, 1, 3 µM; 24 h) dose-dependently decreases IKZF1, c-MYC, and BCL-6 protein expression and increases p53 level in K-RASG12A MM.1S cells^[1].
TL4-12 dose-dependently increases Annexin-V positive cell from 6% (dimethyl sulfoxide) to 13% (1 μM) and 22% (3 μM), respectively^[1].
TL4-12 induces apoptosis and cell-cycle arrest in the G0/G1 phase in MM.1S, RPMI-8226, RPMI-8226 cells^[1].