CPI-455 HCl is an inhibitor of KDM5. It can elevate global levels of H3K4 trimethylation (H3K4me3) and decrease the number of DTPs in multiple cancer cell line models.
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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 | CPI-455 Hydrochloride is the hydrochloride form of CPI-455. CPI-455 is a specific KDM5 inhibitor with IC50 value of 10nM for inhibition of full-length KDM5A in enzymatic assays. CPI-455-mediated KDM5 inhibition resulted in a dose-dependent increase in global H3K4me3 in HeLa cells. Also it induced a time-dependent increase in H3K4me3 that was detected only after 2 or more days of treatment. The elevation of H3K4 trimethylation mediated by this inhibition of KDM5 by CPI-455 decreased the number of drug-tolerant state in multiple cancer cell line models treated with standard chemotherapy or targeted agents[2]. |
作用机制 | The nitrile of CPI-455 makes a single interaction with the active-site metal ion of KDM5. The position occupied by CPI-455 completely overlaps the binding site of 2-OG, demonstrating a competitive mode of action.[1] |
Dose | Mice: 50 mg/kg, 70 mg/kg[2] (i.p.) |
Administration | i.p. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.18mL 0.64mL 0.32mL |
15.88mL 3.18mL 1.59mL |
31.77mL 6.35mL 3.18mL |
CAS号 | 2095432-28-1 |
分子式 | C16H15ClN4O |
分子量 | 314.769 |
别名 | CPI-455 HCl |
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 | |
动物实验配方 |
IP 2% DMSO+water 2 mg/mL clear PO 0.5% CMC-Na 45 mg/mL suspension |