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UNC1215

CAS No. : 1415800-43-9

MCE 站：UNC1215

产品活性：UNC1215 是选择性 L3MBTL3 甲基赖氨酸结构域的拮抗剂，IC₅₀ 为40 nM，K_d 为 120 nM。UNC1215 可用于恶性脑瘤的研究。

研究领域：Epigenetics  |  Apoptosis

作用靶点：Histone Methyltransferase  |  Apoptosis

In Vitro: UNC1215 binds L3MBTL3 with a _d of 120 nM, competitively displacing mono- or dimethyllysine-containing peptides, and is greater than 50-fold more potent toward L3MBTL3 than other members of the MBT family while also demonstrating selectivity against more than 200 other reader domains examined. X-ray crystallography identified a unique 2:2 polyvalent mode of interaction between UNC1215 and L3MBTL3. In cells, UNC1215 is nontoxic and directly binds L3MBTL3 via the Kme-binding pocket of the MBT domains. UNC1215 increases the cellular mobility of GFP-L3MBTL3 fusion proteins, and point mutants that disrupt the Kme-binding function of GFP-L3MBTL3 phenocopy the effects of UNC1215 on localization.

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