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产品名称 | KDM1 ↓ ↑ | KDM2 ↓ ↑ | KDM3 ↓ ↑ | KDM4 ↓ ↑ | KDM5 ↓ ↑ | KDM6 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
OG-L002 |
+++
LSD1, IC50: 20 nM |
99%+ | |||||||||||||||||
ORY-1001 |
+++
LSD1, IC50: 20 nM |
98% | |||||||||||||||||
SP-2509 |
++++
LSD1, IC50: 13 nM |
98+% | |||||||||||||||||
GSK2879552 2HCl |
+
LSD1, Ki: 1.7 μM |
99%+ | |||||||||||||||||
T-3775440 HCl |
++++
LSD1, IC50: 2.1 nM |
99% | |||||||||||||||||
GSK-LSD1 2HCl |
+++
LSD1, IC50: 16 nM |
98% | |||||||||||||||||
Pulrodemstat benzenesulfonate | ✔ | 99%+ | |||||||||||||||||
IOX1 |
+
KDM2A, IC50: 1.8 μM |
+++
KDM3A, IC50: 0.1 μM |
++
KDM4E, IC50: 2.3 μM KDM4C, IC50: 0.6 μM |
+
KDM5C, IC50: 19 μM |
+
KDM6B, IC50: 1.6 μM |
99% | |||||||||||||
PFI-90 | ✔ | 99%+ | |||||||||||||||||
ML324 |
+
JMJD2, IC50: 920 nM |
99%+ | |||||||||||||||||
NCGC00244536 |
++++
KDM4, IC50: 10 nM |
95% | |||||||||||||||||
KDM4D-IN-1 |
++
KDM4D, IC50: 0.41 μM |
99%+ | |||||||||||||||||
GSK467 |
++++
KDM5B, Ki: 10 nM |
98% | |||||||||||||||||
GSK-J1 |
+++
JMJD3, IC50: 60 nM |
99%+ | |||||||||||||||||
(Z)-JIB-04 |
++
JMJD2E, IC50: 340 nM JMJD2A, IC50: 1100 nM |
++
JARID1A, IC50: 230 nM |
++
JMJD3, IC50: 855 nM |
97% | |||||||||||||||
CPI-455 |
++++
KDM5A, IC50: 10 nM |
++++
KDM5, IC50: 10 nM |
98% | ||||||||||||||||
JIB-04 |
++
JMJD2E, IC50: 435 nM JMJD2D, IC50: 290 nM |
++
JARID1A, IC50: 230 nM |
++
JMJD3, IC50: 855 nM |
98% | |||||||||||||||
GSK-J4 HCl |
+++
JMJD3, IC50: 60 nM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | The histone H3K9 demethylase LSD1 plays a critical role in the regulation of herpes simplex virus (HSV) infection. OG-L002 is a selective inhibitor of LSD1 with an IC50 value of 0.02μM. It is also a potent inhibitor of monoamine oxidases (MAO) with IC50 values of 1.38μM and 0.72μM for MAO-A and MAO-B, respectively. OG-L002 inhibited viral immediate-early gene expression in HeLa and HFF cells with IC50 values of ~10µM and ~3µM, respectively. Treatment of Hela cells with 50µM OG-L002 for 24 hours reduced viral yields compared with the DMSO-treated controls. Also in Hela cells, pretreatment with 50µM OG-L002 for 4 hours increased the levels of total histone H3 and H3K9-me2 (20- to 30-fold) associated with viral immediate-early gene promoters. Treatment with OG-L002 (10 - 50µM) for 48 hours repressed viral reactivation in trigeminal ganglia isolated from HSV-infected mice. In BALB/c mice, pretreatment with OG-L002 (6 - 40mg/kg/day) for one week reduced the levels of detectable viral genomes in the ganglia at both 3- and 5-day post-infection. The administration of mice with OG-L002 at a dose of 20mg/kg/day reduced viral genome accumulation at 3-, 5-, and 10-day post-infection[2]. |
作用机制 | OG-L002 is a potent LSD1 inhibitor that blocks HSV lytic replication and reactivation from latency[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
4.44mL 0.89mL 0.44mL |
22.19mL 4.44mL 2.22mL |
44.39mL 8.88mL 4.44mL |
CAS号 | 1357302-64-7 |
分子式 | C15H15NO |
分子量 | 225.286 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,2-8°C |
溶解度 |
DMSO: 105 mg/mL(466.07 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |