TL4-12

Research use only, not for human use.

TL4-12 is a specific MAP4K2/GCK inhibitor that inhibits IKZF1 and BCL-6.TL4-12 inhibits MM cell proliferation and induces apoptosis, and can be used in the study of multiple myeloma (MM).

TL4-12 is a selective MAP4K2/GCK inhibitor, dose-dependently downregulates IKZF1 and BCL-6 and leads to MM cell proliferation inhibition (IC50=37 nM) accompanied by induction of apoptosis. TL4-12 can be used to overcome immunomodulatory agent resistance in multiple myeloma (MM).

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.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.TL4-12 dose-dependently increases Annexin-V positive cell from 6% (dimethyl sulfoxide) to 13% (1 μM) and 22% (3 μM), respectively.TL4-12 induces apoptosis and cell-cycle arrest in the G0/G1 phase in MM.1S, RPMI-8226, RPMI-8226 cells.

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Others

Other Targets

Immunology/Inflammation related | BCL | Apoptosis

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1620820-12-3

500.52

C25H27F3N6O2

>98% (HPLC)

In Vitro:?DMSO : 8.33 mg/mL (16.64 mM; Ultrasonic (<60°C)

O=C(NC=1C=C(C=C(C1)C(F)(F)F)N2CCN(C)CC2)C3=CC=C(C(OC4=NC=NC(=C4)NC)=C3)C

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(-20℃)

With Ice Pack

≥ 2 years