2. Epigenetics
  3. Histone Demethylase
  4. CPI-455

CPI-455 是一种特异性的泛 KDM5 抑制剂，对 KDM5A 的 IC50 为 10 nM，CPI-455 介导 KDM5 抑制，提高 H3K4me3 的整体水平，并减少多肿瘤细胞系模型中耐药的持久癌细胞的数量。

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CPI-455 Chemical Structure

CPI-455 Chemical Structure

CAS No. : 1628208-23-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1387
In-stock
1 mg ￥453
In-stock
5 mg ￥855
In-stock
10 mg ￥1410
In-stock
25 mg ￥2650
In-stock
50 mg ￥4240
In-stock
100 mg ￥6000
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of CPI-455:

CPI-455 相关抗体

Top Publications Citing Use of Products

查看 Histone Demethylase 亚型特异性产品:

查看所有亚型
KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents[1].

IC50 & Target

KDM5

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 GI50
> 50 μM
Compound: 3; CPI-455
Growth inhibition of human A549 cells after 72 hrs by Alamar blue staining based fluorescence assay
Growth inhibition of human A549 cells after 72 hrs by Alamar blue staining based fluorescence assay
[PMID: 30745098]
MKN-45 IC50
23.79 μM
Compound: CPI-455
Antiproliferative activity against human MKN-45 cells assessed as reduction in cell proliferation measured after 6 days by MTS assay
Antiproliferative activity against human MKN-45 cells assessed as reduction in cell proliferation measured after 6 days by MTS assay
[PMID: 32155529]
MKN-45 IC50
30.33 μM
Compound: CPI-455
Antiproliferative activity against human MKN-45 cells assessed as reduction in cell proliferation measured after 4 days by MTS assay
Antiproliferative activity against human MKN-45 cells assessed as reduction in cell proliferation measured after 4 days by MTS assay
[PMID: 32155529]
Sf9 IC50
14300 nM
Compound: 3; CPI-455
Inhibition of human C-terminal FLAG-tagged KDM6B (1043 to end residues) expressed in baculovirus infected Sf9 insect cells using H3(21-44)-K27(Me3)-GK(Biotin)/2-OG as substrate measured after 1 hr by Alphalisa assay
Inhibition of human C-terminal FLAG-tagged KDM6B (1043 to end residues) expressed in baculovirus infected Sf9 insect cells using H3(21-44)-K27(Me3)-GK(Biotin)/2-OG as substrate measured after 1 hr by Alphalisa assay
[PMID: 30745098]
Sf9 IC50
3010 nM
Compound: 3; CPI-455
Inhibition of full-length human N-terminal FLAG/His-tagged KDM5C (2 to 1560 residues) expressed in baculovirus infected Sf9 insect cells using H3(1-21)K4(Me3)-GGK(Biotin)/2-OG as substrate measured after 1 hr by Alphalisa assay
Inhibition of full-length human N-terminal FLAG/His-tagged KDM5C (2 to 1560 residues) expressed in baculovirus infected Sf9 insect cells using H3(1-21)K4(Me3)-GGK(Biotin)/2-OG as substrate measured after 1 hr by Alphalisa assay
[PMID: 30745098]
Sf9 IC50
337 nM
Compound: 3; CPI-455
Inhibition of human N-terminal FLAG/His-tagged KDM5B (2 to 751 residues) expressed in baculovirus infected Sf9 insect cells using H3(1-21)K4(Me3)-GGK(Biotin)/2-OG as substrate measured after 1 hr by Alphalisa assay
Inhibition of human N-terminal FLAG/His-tagged KDM5B (2 to 751 residues) expressed in baculovirus infected Sf9 insect cells using H3(1-21)K4(Me3)-GGK(Biotin)/2-OG as substrate measured after 1 hr by Alphalisa assay
[PMID: 30745098]
Sf9 IC50
506 nM
Compound: 3; CPI-455
Inhibition of human C-terminal FLAG-tagged KDM5A (1 to 1090 residues) expressed in baculovirus infected Sf9 insect cells using H3(1-21)K4(Me3)-GGK(Biotin)/2-OG as substrate measured after 1 hr by Alphalisa assay
Inhibition of human C-terminal FLAG-tagged KDM5A (1 to 1090 residues) expressed in baculovirus infected Sf9 insect cells using H3(1-21)K4(Me3)-GGK(Biotin)/2-OG as substrate measured after 1 hr by Alphalisa assay
[PMID: 30745098]
体外研究
(In Vitro)

CPI-455 介导 KDM5 抑制，提高 H3K4 三甲基化 (H3K4me3) 的总体水平，并减少使用标准化疗或靶向药物处理的多种癌细胞系模型中的 DTP 数量[1]。
CPI-455，对目标 KDM5 蛋白具有高亲和力。在 24 小时内，在暴露于两种活性化合物 CPI-455 和 CPI-766 中的任何一种后，观察到 H3K4me3 以剂量依赖性方式增加。KDM5 Inhibitor CPI0455 在 3 种管腔乳腺癌细胞系 MCF-7、T-47 和 EFM-19 中的 IC50 计算值分别为 35.4、26.19 和 16.13 μM[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

CPI-455 相关抗体:
体内研究
(In Vivo)

在小鼠中双重阻断 B7-H4 和 KDM5B (CPI-455，50/70 mg/kg，腹腔注射，每日) 可引发保护性免疫[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six-week-old male C57BL/6 mice (One- to 2-mm fragments of P. gingivalis–positive PDXs were implanted subcutaneously into the flank region of humanized mice.)
Dosage: 50 mg/kg or 70 mg/kg (combined with anti–B7-H4).
Administration: IP, daily, 14-28 days.
Result: Histopathology analysis revealed no inflammation in either group at 2 weeks in response to the primary infection. However, at 8 weeks after inoculation, mice receiving monotherapy exhibited mild inflammation, whereas the combined treatment presented with heavy to severe inflammation, which persisted at 12 and 16 weeks after challenge.
Treatment with CPI-455 to selectively target H3K4-specific JmjC demethylases increased CXCL11, CXCL9, and CXCL10 following infection, with maximum levels observed 48 hours after infection.
分子量

278.31

Formula

C16H14N4O
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 31.25 mg/mL (112.28 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.5931 mL 17.9656 mL 35.9312 mL
5 mM 0.7186 mL 3.5931 mL 7.1862 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.98 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 98.95%

COA (200 KB) HNMR (180 KB) LCMS (117 KB)

产品使用指南 (1538 KB)
参考文献

CPI-455 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.5931 mL 17.9656 mL 35.9312 mL 89.8279 mL
5 mM 0.7186 mL 3.5931 mL 7.1862 mL 17.9656 mL
10 mM 0.3593 mL 1.7966 mL 3.5931 mL 8.9828 mL
15 mM 0.2395 mL 1.1977 mL 2.3954 mL 5.9885 mL
20 mM 0.1797 mL 0.8983 mL 1.7966 mL 4.4914 mL
25 mM 0.1437 mL 0.7186 mL 1.4372 mL 3.5931 mL
30 mM 0.1198 mL 0.5989 mL 1.1977 mL 2.9943 mL
40 mM 0.0898 mL 0.4491 mL 0.8983 mL 2.2457 mL
50 mM 0.0719 mL 0.3593 mL 0.7186 mL 1.7966 mL
60 mM 0.0599 mL 0.2994 mL 0.5989 mL 1.4971 mL
80 mM 0.0449 mL 0.2246 mL 0.4491 mL 1.1228 mL
100 mM 0.0359 mL 0.1797 mL 0.3593 mL 0.8983 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CPI-4551628208-23-0CPI455CPI 455Histone DemethylaseInhibitorinhibitorinhibit

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目录号：
HY-100421
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