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CPI-455 {[allProObj[0].p_purity_real_show]}

货号:A145136

CPI-455 is a selective inhibitor of KDM5 demethylases and can reduce survival of drug-tolerant cancer cells.

CPI-455 化学结构 CAS号:1628208-23-0
CPI-455 化学结构
CAS号:1628208-23-0
CPI-455 3D分子结构
CAS号:1628208-23-0
CPI-455 化学结构 CAS号:1628208-23-0
CPI-455 3D分子结构 CAS号:1628208-23-0
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CPI-455 纯度/质量文件 产品仅供科研

货号:A145136 标准纯度: {[allProObj[0].p_purity_real_show]}
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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

++

KDM4C, IC50: 0.6 μM

KDM4E, IC50: 2.3 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 ++

JMJD2A, IC50: 1100 nM

JMJD2E, IC50: 340 nM

++

JARID1A, IC50: 230 nM

++

JMJD3, IC50: 855 nM

97%
CPI-455 ++++

KDM5A, IC50: 10 nM

++++

KDM5, IC50: 10 nM

98%
JIB-04 ++

JMJD2D, IC50: 290 nM

JMJD2E, IC50: 435 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。

CPI-455 生物活性

靶点
  • KDM6

    KDM5, IC50:10 nM

  • KDM5

    KDM5, IC50:10 nM

  • KDM5

    KDM5A, IC50:10 nM

描述 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.[2]

CPI-455 参考文献

[1]Vinogradova M, Gehling VS, et al. An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells. Nat Chem Biol. 2016 Jul;12(7):531-8.

[2]Vinogradova M, Gehling VS, Gustafson A, Arora S, Tindell CA, Wilson C, Williamson KE, Guler GD, Gangurde P, Manieri W, Busby J, Flynn EM, Lan F, Kim HJ, Odate S, Cochran AG, Liu Y, Wongchenko M, Yang Y, Cheung TK, Maile TM, Lau T, Costa M, Hegde GV, Jackson E, Pitti R, Arnott D, Bailey C, Bellon S, Cummings RT, Albrecht BK, Harmange JC, Kiefer JR, Trojer P, Classon M. An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells. Nat Chem Biol. 2016 Jul;12(7):531-8. doi: 10.1038/nchembio.2085. Epub 2016 May 23. PMID: 27214401.

CPI-455 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.59mL

0.72mL

0.36mL

17.97mL

3.59mL

1.80mL

35.93mL

7.19mL

3.59mL

CPI-455 技术信息

CAS号1628208-23-0
分子式C16H14N4O
分子量 278.309
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 Sealed in dry,Room Temperature

溶解度

DMSO: 35 mg/mL(125.76 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
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