TL4-12 is a selectiveMAP4K2/GCKinhibitor, dose-dependently downregulates IKZF1 and BCL-6 and leads to MM cell proliferation inhibition (IC₅₀=37 nM) accompanied by induction ofapoptosis. TL4-12 can be used to overcome immunomodulatory drug resistance in multiple myeloma (MM)^[1].

TL4 12 (0-5 μM; 4 days) shows antiproliferation activity with anIC₅₀value of 37 nM for MM cells, and withIC₅₀s 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].

500.52

C₂₅H₂₇F₃N₆O₂

1620820-12-3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.