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MM-102 TFA

CAS No. : 1883545-52-5

MCE 站：MM-102 TFA

产品活性：MM-102 TFA (HMTase Inhibitor IX TFA) 是一种有效的 WDR5/MLL 相互作用抑制剂, WDR5 结合检测中, IC₅₀ =2.4 nM, K_i< 1 nM。

研究领域：Epigenetics

作用靶点：Histone Methyltransferase

In Vitro: MM-102 (HMTase Inhibitor IX) inhibits MLL1 methyltransferase activity and MLL-1-induced HoxA9 and Meis-1 gene expression in leukemia cells expressing the MLL1-AF9 fusion gene. Also inhibits cell growth and induces apoptosis in leukemia cells harbouring MLL1 fusion proteins.
MM-102 (TFA), with the highest binding affinities to WDR5, also show the most potent inhibitory activity in the HMT assay withIC₅₀=0.4-0.9 μM.
MM-102 (HMTase Inhibitor IX) dose-dependently inhibits cell growth in the MV4;11 and KOPN8 leukemia cell lines, which carry MLL1-AF4 and MLL1-ENL fusion proteins, respectively.
MM-102 (HMTase Inhibitor IX) has IC₅₀=25 μM in both cell lines and completely inhibits cell growth in these cell lines at 75 μM.
MM-102 (HMTase Inhibitor IX) effectively and selectively inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins and has minimal effect in leukemia cells with wild-type MLL1 protein.

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