货号:A1967108 同义名: JADA82 trihydrochloride;PCK82 trihydrochloride
JQKD82 trihydrochloride是一种细胞通透性和选择性 KDM5 抑制剂,能够增加 H3K4me3 水平,展现了在多发性骨髓瘤研究中的应用潜力,可用于表观遗传学的相关研究。
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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 |
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ORY-1001 |
+++
LSD1, IC50: 20 nM |
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SP-2509 |
++++
LSD1, IC50: 13 nM |
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GSK2879552 2HCl |
+
LSD1, Ki: 1.7 μM |
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T-3775440 HCl |
++++
LSD1, IC50: 2.1 nM |
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GSK-LSD1 2HCl |
+++
LSD1, IC50: 16 nM |
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Pulrodemstat benzenesulfonate | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
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 |
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PFI-90 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
ML324 |
+
JMJD2, IC50: 920 nM |
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NCGC00244536 |
++++
KDM4, IC50: 10 nM |
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KDM4D-IN-1 |
++
KDM4D, IC50: 0.41 μM |
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GSK467 |
++++
KDM5B, Ki: 10 nM |
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GSK-J1 |
+++
JMJD3, IC50: 60 nM |
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(Z)-JIB-04 |
++
JMJD2E, IC50: 340 nM JMJD2A, IC50: 1100 nM |
++
JARID1A, IC50: 230 nM |
++
JMJD3, IC50: 855 nM |
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CPI-455 |
++++
KDM5A, IC50: 10 nM |
++++
KDM5, IC50: 10 nM |
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JIB-04 |
++
JMJD2E, IC50: 435 nM JMJD2D, IC50: 290 nM |
++
JARID1A, IC50: 230 nM |
++
JMJD3, IC50: 855 nM |
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GSK-J4 HCl |
+++
JMJD3, IC50: 60 nM |
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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。 |
描述 | JQKD82 trihydrochloride, also known as JADA82, is a selective KDM5 inhibitor that permeates cells. It enhances H3K4me3 levels and is applicable in multiple myeloma research [1]. |
体内研究 | JQKD82 trihydrochloride (50-75 mg/kg twice daily for 3 weeks) demonstrates anti-multiple myeloma activity [1]. JQKD82 trihydrochloride elevates H3K4me3 levels and significantly reduces MYC immunostaining in vivo[1]. |
体外研究 | 0.3 μM JQKD82 trihydrochloride for 24 hours induces a global increase in H3K4me3 levels in MM.1S cells [1]. JQKD82 trihydrochloride exhibits dose- and time-dependent growth inhibition with an IC50 of 0.42 μM in MM.1S cells, when administered at concentrations ranging from 0.1 to 10 μM over 5 days [1]. JQKD82 trihydrochloride (1 μM) induces G1 cell-cycle arrest within 48 hours in MM.1S and MOLP-8 cells [1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.64mL 0.33mL 0.16mL |
8.20mL 1.64mL 0.82mL |
16.39mL 3.28mL 1.64mL |
CAS号 | 2863676-87-1 |
分子式 | C27H43Cl3N4O5 |
分子量 | 610.013 |
别名 | JADA82 trihydrochloride;PCK82 trihydrochloride |
运输 | 蓝冰 |
存储条件 |
粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 50 mg/mL(81.97 mM),配合低频超声助溶,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 |