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

CPI-455 是一種特異性的泛 KDM5 抑制劑，對(duì) KDM5A 的 IC50 為 10 nM，CPI-455 介導(dǎo) KDM5 抑制，提高 H3K4me3 的整體水平，并減少多腫瘤細(xì)胞系模型中耐藥的持久癌細(xì)胞的數(shù)量。

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CPI-455 Chemical Structure

CPI-455 Chemical Structure

CAS No. : 1628208-23-0

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規(guī)格 價(jià)格 是否有貨 數(shù)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   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

Other Forms of CPI-455:

查看 Histone Demethylase 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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

 

細(xì)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]
體外研究
(In Vitro)

CPI-455 介導(dǎo) KDM5 抑制，提高 H3K4 三甲基化 (H3K4me3) 的總體水平，并減少使用標(biāo)準(zhǔn)化療或靶向藥物處理的多種癌細(xì)胞系模型中的 DTP 數(shù)量[1]。
CPI-455，對(duì)目標(biāo) KDM5 蛋白具有高親和力。在 24 小時(shí)內(nèi)，在暴露于兩種活性化合物 CPI-455 和 CPI-766 中的任何一種后，觀察到 H3K4me3 以劑量依賴性方式增加。KDM5 Inhibitor CPI0455 在 3 種管腔乳腺癌細(xì)胞系 MCF-7、T-47 和 EFM-19 中的 IC50 計(jì)算值分別為 35.4、26.19 和 16.13 μM[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

在小鼠中雙重阻斷 B7-H4 和 KDM5B (CPI-455，50/70 mg/kg，腹腔注射，每日) 可引發(fā)保護(hù)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 號(hào)
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 31.25 mg/mL (112.28 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 98.95%

參考文獻(xiàn)

CPI-455 相關(guān)分類

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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.

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產(chǎn)品名稱：
CPI-455
目錄號(hào)：
HY-100421
需求量：