Pulrodemstat
| CAS号 | 1821307-10-1 | 货号 | BCP44101 |
| 中文名 | Pulrodemstat | ||
| 英文名 | Pulrodemstat | ||
| 中文别名 | |||
| 英文别名 | CC-90011; CC 90011; CC90011; Pulrodemstatum; | ||
| 分子式 | C24H23F2N5O2 | 分子量 | 451.47 |
| 生物活性 | Pulrodemstat is an orally available inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity. Upon administration, pulrodemstat binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the di- and mono-methylated forms of lysine at position 4 of histone H3 (H3K4) to mono- and unmethylated H3K4, respectively. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor (remove hyphen) suppressor genes. This may lead to an inhibition of cell growth in LSD1-overexpressing tumor cells. In addition, LSD1 demethylates mono- or di-methylated H3K9 which increases gene expression of tumor promoting genes; inhibition of LSD1 promotes H3K9 methylation and decreases transcription of these genes. LSD1, an enzyme belonging to the flavin adenine dinucleotide (FAD)-dependent amine oxidase family that is overexpressed in certain tumor cells, plays a key role in tumor cell growth and survival. | ||
| 信号通路 | Epigenetics | ||
| 靶 点 | Histone Demethylase | ||
结构式
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