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BTYNB

BTYNB (MDK6620) 是IMP1结合 c-Myc mRNA 的有效选择性抑制剂，IC50为 5 μM。它下调 β-TrCP1 mRNA 并减少NF-κB 的激活。它通过损害 IGF2 mRNA 结合蛋白 1 结合来破坏这种增强子功能，可用于癌症研究。

CAS号

304456-62-0

分子式

C12H9BrN2OS

主要靶点

c-Myc|NF-κB|Others

仅限科研使用

Cat No : CM04753

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Synonyms

MDK6620|BTYNB IMP1 Inhibitor

验证数据展示

  • CAS No.: 304456-62-0

    BTYNB
    CAS#: 304456-62-0

产品信息

BTYNB (MDK6620) is an inhibitor of the oncofetal mRNA-binding protein IMP1 (IC50 = 5 μM for IMP1 binding to c-Myc mRNA). MDK6620 downregulates β-TrCP1 mRNA and reduces activation of nuclear transcriptional factors-kappa B (NF-κB). It disrupts this enhancer function by impairing IGF2 mRNA-binding protein 1 (IGF2BP1)-RNA association

CAS号 304456-62-0
分子式 C12H9BrN2OS
主要靶点 c-Myc|NF-κB|Others
主要通路 其他|NF-κB信号通路|细胞周期
分子量 309.18
纯度 98.00%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 MDK6620|BTYNB IMP1 Inhibitor

靶点活性

IMP1 c-Myc mRNA internation:5 μM (IC50)

体外活性

In cells, BTYNB downregulates several mRNA transcripts regulated by IMP1.?BTYNB destabilizes c-Myc mRNA, resulting in downregulation of c-Myc mRNA and protein.?BTYNB downregulates β-TrCP1 mRNA and reduces activation of nuclear transcriptional factors-kappa B (NF-κB).?The oncogenic translation regulator, eEF2, emerged as a new IMP1 target mRNA, enabling BTYNB to inhibit tumor cell protein synthesis.?BTYNB potently inhibited proliferation of IMP1-containing ovarian cancer and melanoma cells with no effect in IMP1-negative cells.?Overexpression of IMP1 reversed BTYNB inhibition of cell proliferation.?BTYNB completely blocked anchorage-independent growth of melanoma and ovarian cancer cells in colony formation assays.?With its ability to target c-Myc and to inhibit proliferation of difficult-to-target melanomas and ovarian cancer cells, and with its unique mode of action, BTYNB is a promising small molecule for further therapeutic evaluation and mechanistic studies[1].

溶解度

DMSO:62 mg/mL (200.53 mM),Ethanol:4 mg/mL (12.94 mM)

参考文献

1.Mahapatra L ,  Andruska N ,  Mao C , et al. A Novel IMP1 Inhibitor, BTYNB, Targets c-Myc and Inhibits Melanoma and Ovarian Cancer Cell Proliferation[J]. Translational Oncology, 2017, 10(5):818-827.
2.Simon M ,  Nadine B ,  Bianca B , et al. The oncofetal RNA-binding protein IGF2BP1 is a druggable, post-transcriptional super-enhancer of E2F-driven gene expression in cancer[J]. Nucleic Acids Research, 2020(15):15.

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