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  1. Cell Cycle/DNA Damage Apoptosis
  2. NEKs Apoptosis
  3. INH6

INH6是有效的Nek2/Hec1抑制劑;抑制HeLa細胞生長的IC50值為2.4 μM。

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INH6 Chemical Structure

INH6 Chemical Structure

CAS No. : 1001753-24-7

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥550
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5 mg ¥312
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10 mg ¥500
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25 mg ¥1100
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50 mg ¥1800
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100 mg ¥3400
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Customer Review

查看 NEKs 亞型特異性產(chǎn)品:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

INH6 is a potent Nek2/Hec1 inhibitor; inhibits the growth of HeLa cells with an IC50 of 2.4 μM.

IC50 & Target

NEK2

 

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
HeLa IC50
2.4 μM
Compound: 6
Cytotoxicity against human HeLa cells after 4 days by XTT assay
Cytotoxicity against human HeLa cells after 4 days by XTT assay
[PMID: 19243176]
HeLa IC50
3.6 μM
Compound: 2
Antiproliferative activity against human HeLa cells assessed as cell viability after 96 hrs by CellTiter96 assay
Antiproliferative activity against human HeLa cells assessed as cell viability after 96 hrs by CellTiter96 assay
[PMID: 24773549]
K562 IC50
2.5 μM
Compound: 6
Cytotoxicity against human K562 cells after 4 days by XTT assay
Cytotoxicity against human K562 cells after 4 days by XTT assay
[PMID: 19243176]
K562 IC50
3.2 μM
Compound: 2
Antiproliferative activity against human K562 cells assessed as cell viability after 96 hrs by CellTiter96 assay
Antiproliferative activity against human K562 cells assessed as cell viability after 96 hrs by CellTiter96 assay
[PMID: 24773549]
MDA-MB-231 IC50
1.7 μM
Compound: 6
Cytotoxicity against human MDA-MB-231 cells after 4 days XTT assay
Cytotoxicity against human MDA-MB-231 cells after 4 days XTT assay
[PMID: 19243176]
MDA-MB-231 IC50
3.2 μM
Compound: 2
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 96 hrs by CellTiter96 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 96 hrs by CellTiter96 assay
[PMID: 24773549]
MDA-MB-468 IC50
2.1 μM
Compound: 6
Cytotoxicity against human MDA-MB-468 cells after 4 days by XTT assay
Cytotoxicity against human MDA-MB-468 cells after 4 days by XTT assay
[PMID: 19243176]
MDA-MB-468 IC50
2.2 μM
Compound: 2
Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability after 96 hrs by CellTiter96 assay
Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability after 96 hrs by CellTiter96 assay
[PMID: 24773549]
體外研究
(In Vitro)

小分子 INH (Nek2/Hec1 抑制劑) 靶向有絲分裂途徑中的 Hec1 及其調(diào)節(jié)因子 Nek2,經(jīng)鑒定可使由蛋白質(zhì)降解介導(dǎo)的 Hec1/Nek2 功能失活,隨后導(dǎo)致染色體錯誤分離和細胞死亡。INH6 處理的細胞表現(xiàn)出增加的具有多極紡錘體配置的有絲分裂群體。在用 INH6 處理表達染色體標記蛋白 H2B-GFP 的 HeLa 細胞后,檢測到染色體錯位率增加。INH6 處理的細胞表現(xiàn)出垂死細胞的進行性形態(tài)學(xué)變化特征 (例如,膜起泡),這通過使用 FACS 分析的細胞周期分析進一步證實。大約 20% 的 INH6 處理細胞在處理后 72 小時發(fā)生凋亡[1]

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

分子量

322.42

Formula

C19H18N2OS

CAS 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
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)
細胞實驗: 

DMSO 中的溶解度 : 50 mg/mL (155.08 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 3.1015 mL 15.5077 mL 31.0154 mL
5 mM 0.6203 mL 3.1015 mL 6.2031 mL
查看完整儲備液配制表

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

  • 摩爾計算器

  • 稀釋計算器

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

動物實驗:

請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用;
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

    請依序添加每種溶劑: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.75 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,此方案實驗周期在半個月以上的動物實驗酌情使用。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中,混合均勻。

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動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。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,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,請謹慎選擇該方案。
請確保第一步儲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
參考文獻
Cell Assay
[1]

Standard XTT assays with a four-day drug treatment procedure were performed to measure the dose-dependent cytotoxicity of INH analogs in cultured cells. Triplicate sets were measured and compiled for final data presentation. Cells were plated on 96-well dishes one day before the drug treatment, followed by drug treatment (2.5 μM INH6) on day 2 and XTT assay on day 5 after drug addition. The absorption at 595 nm was measured with a plate reader and converted to cell survival percentages in comparison to mock treated groups[1].

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

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1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 3.1015 mL 15.5077 mL 31.0154 mL 77.5386 mL
5 mM 0.6203 mL 3.1015 mL 6.2031 mL 15.5077 mL
10 mM 0.3102 mL 1.5508 mL 3.1015 mL 7.7539 mL
15 mM 0.2068 mL 1.0338 mL 2.0677 mL 5.1692 mL
20 mM 0.1551 mL 0.7754 mL 1.5508 mL 3.8769 mL
25 mM 0.1241 mL 0.6203 mL 1.2406 mL 3.1015 mL
30 mM 0.1034 mL 0.5169 mL 1.0338 mL 2.5846 mL
40 mM 0.0775 mL 0.3877 mL 0.7754 mL 1.9385 mL
50 mM 0.0620 mL 0.3102 mL 0.6203 mL 1.5508 mL
60 mM 0.0517 mL 0.2585 mL 0.5169 mL 1.2923 mL
80 mM 0.0388 mL 0.1938 mL 0.3877 mL 0.9692 mL
100 mM 0.0310 mL 0.1551 mL 0.3102 mL 0.7754 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:
INH6
目錄號:
HY-100541
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