TL4-12,1620820-12-3

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TL4-12

CAS No. : 1620820-12-3

MCE 国际站：TL4-12

产品活性：TL4-12 是一种选择性 MAP4K2/GCK 抑制剂，下调 IKZF1 和 BCL-6，并抑制 MM 细胞增殖 (IC₅₀=37 nM) 并诱导细胞凋亡。TL4-12 可用于克服多发性骨髓瘤 (MM) 中免疫调节剂的耐药性。

研究领域：MAPK/ERK Pathway  |  Apoptosis

作用靶点：MAP4K  |  Apoptosis

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.
.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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