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CPI-455盐酸 /CPI-455 hydrochloride {[allProObj[0].p_purity_real_show]}

货号:A301323 同义名: CPI-455 HCl Ambeed 开学季,买赠积分,赢豪礼

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.

CPI-455 hydrochloride 化学结构 CAS号:2095432-28-1
CPI-455 hydrochloride 化学结构
CAS号:2095432-28-1
CPI-455 hydrochloride 3D分子结构
CAS号:2095432-28-1
CPI-455 hydrochloride 化学结构 CAS号:2095432-28-1
CPI-455 hydrochloride 3D分子结构 CAS号:2095432-28-1
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CPI-455 hydrochloride 纯度/质量文件 产品仅供科研

货号:A301323 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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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。

CPI-455 hydrochloride 生物活性

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]

CPI-455 hydrochloride 动物研究

Dose Mice: 50 mg/kg, 70 mg/kg[2] (i.p.)
Administration i.p.

CPI-455 hydrochloride 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 hydrochloride 实验方案

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

CPI-455 hydrochloride 技术信息

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

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