1. Epigenetics
  2. Histone Demethylase
  3. LSD1-IN-49

LSD1-IN-49 是一种赖氨酸特异性去甲基化酶 1 (LSD1/KDM1A) 抑制剂,对人源靶点的 IC50 为 29 nM。LSD1-IN-49 可通过与 LSD1 的黄素腺嘌呤二核苷酸 (FAD) 辅因子形成加合物,不可逆地抑制 LSD1 的酶活性。LSD1-IN-49 可用作开发靶向 LSD1 的脑部 PET 显像剂的先导化合物。

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LSD1-IN-49

LSD1-IN-49 Chemical Structure

CAS No. : 1422533-70-7

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  • 生物活性

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生物活性

LSD1-IN-49 is a Lysine-specific demethylase 1 (LSD1/KDM1A) inhibitor with a human IC50 of 29 nM. LSD1-IN-49 irreversibly inhibits LSD1 enzyme activity by forming an adduct with the flavin adenine dinucleotide (FAD) cofactor of LSD1. LSD1-IN-49 can be used as a lead compound for the development of LSD1-targeted PET imaging agents for the brain[1].

IC50 & Target[1]

LSD1

29 nM (IC50)

体外研究
(In Vitro)

LSD1-IN-49 (compound (±)1) (孵育 15 分钟) 可强效抑制人源重组 LSD1/CoREST 酶,其 IC50 为 29 nM[1]
LSD1-IN-49 (1 μM; 1 h) 在表达人 MDR1 的 LLC-PK1 细胞中检测时,MDR1 外排率为 0.8[1]

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

分子量

382.50

Formula

C26H26N2O

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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产品名称:
LSD1-IN-49
目录号:
HY-186116
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