1. PROTAC Anti-infection Metabolic Enzyme/Protease
  2. PROTACs Parasite Dihydrofolate reductase (DHFR)
  3. BION106

BION106 是一种二氢叶酸还原酶胸苷酸合成酶 (DHFR-TS) PROTAC 降解剂。BION106 具有极强的抗疟活性,对恶性疟原虫的 Ki 值为 2.68 nM,毒性为 0.2 μM;对哺乳动物细胞的 Ki 值大于 100 μM,毒性为 44.2 μM。BION106 可用于抗疟原虫研究 (粉色:DHFR-TS 配体 (HY-15676);蓝色:Idasanutlin 配体 (HY-153007);黑色:连接子 (HY-W021401))。

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BION106

BION106 Chemical Structure

CAS No. : 3077918-44-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BION106 is a dihydrofolate reductasethymidylate synthase (DHFR-TS) PROTAC degrader. BION106 exhibits extremely strong anti-malarial activity with a Ki and toxicity of 2.68 nM and 0.2 μM against Plasmodium falciparum, and > 100 μM and 44.2 μM in mammalian cells. BION106 can be used for the study of antimalarial parasites (Pink: DHFR-TS ligand (HY-15676); Blue: Idasanutlin ligand (HY-153007); Black: Linker (HY-W021401))[1].

体外研究
(In Vitro)

BION106 (10 μM,30-240 分钟) 能快速有效地降解 Plasmodium falciparum 中二氢叶酸还原酶-胸苷酸合成酶,表明其能快速形成有效的三元复合物并启动降解过程[1]
BION106 (0.4-50 μM,4 小时) 能以浓度依赖的方式显著降低 Plasmodium falciparum 中二氢叶酸还原酶-胸苷酸合成酶的含量[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

1133.12

Formula

C57H69Cl2F2N9O9

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
BION106
目录号:
HY-178728
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