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  2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis
  4. 5,6-Dichlorobenzimidazole riboside

5,6-Dichlorobenzimidazole riboside  (Synonyms: DRB)

目錄號(hào): HY-14392 純度: 99.89%
COA 產(chǎn)品使用指南 技術(shù)支持

5,6-Dichlorobenzimidazole riboside (DRB) 是一種核苷類(lèi)似物，可抑制幾種羧基末端結(jié)構(gòu)域激酶，包括酪蛋白激酶 II 和細(xì)胞周期依賴(lài)性激酶。5,6-Dichlorobenzimidazole riboside 有抗腫瘤活性。5,6-Dichlorobenzimidazole riboside 可誘導(dǎo)細(xì)胞凋亡。

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5,6-Dichlorobenzimidazole riboside Chemical Structure

5,6-Dichlorobenzimidazole riboside Chemical Structure

CAS No. : 53-85-0

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥330
In-stock
5 mg ￥300
In-stock
10 mg ￥450
In-stock
25 mg ￥900
In-stock
50 mg ￥1350
In-stock
100 mg ￥2000
In-stock
200 mg   詢(xún)價(jià)  
500 mg   詢(xún)價(jià)  

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Customer Review

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

5,6-Dichlorobenzimidazole riboside (DRB) is a nucleoside analog that inhibits several carboxyl-terminal domain kinases, including casein kinase II and cell cycle-dependent kinases (CDK). 5, 6-dichlorobenzimidazole riboside has antitumor activity. 5, 6-dichlorobenzimidazole riboside can induce apoptosis[1][2][3][4][5][6][7].

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
BSC-1 IC50
30 μM
Compound: 1f
Antiviral activity against HSV-1 (herpes simplex virus), determined by ELISA in quadruplicate wells using BSC-1 cells
Antiviral activity against HSV-1 (herpes simplex virus), determined by ELISA in quadruplicate wells using BSC-1 cells
[PMID: 10882370]
HCT-116 GI50
25 μM
Compound: DRB
Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay
Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay
[PMID: 22225635]
HFF IC50
24 μM
Compound: DRB
Cytotoxicity produced in human foreskin fibroblasts (HFF) cells was estimated by visual scoring of cells unaffected by virus infection in the plaque-reduction assay.
Cytotoxicity produced in human foreskin fibroblasts (HFF) cells was estimated by visual scoring of cells unaffected by virus infection in the plaque-reduction assay.
[PMID: 8784445]
HFF IC50
42 μM
Compound: DRB
Compound was tested for antiviral activity against human cytomegalovirus (HCMV) by plaque reduction assay using HFF cells
Compound was tested for antiviral activity against human cytomegalovirus (HCMV) by plaque reduction assay using HFF cells
[PMID: 10882375]
HFF IC50
42 μM
Compound: 1f
Antiviral activity against towne strain HCMV was determined by plaque reduction assay in duplicate wells using HFF cells
Antiviral activity against towne strain HCMV was determined by plaque reduction assay in duplicate wells using HFF cells
[PMID: 10882370]
Huh-7 EC50
34.1 μM
Compound: DRB
Antiviral activity against HCV 1b con1 in dual-reporter HCV replicon Huh7 cells by measuring hRLuc reporter activity after 72 hrs
Antiviral activity against HCV 1b con1 in dual-reporter HCV replicon Huh7 cells by measuring hRLuc reporter activity after 72 hrs
[PMID: 17060518]
Huh-7 CC50
40.4 μM
Compound: DRB
Cytotoxicity against dual-reporter HCV replicon Huh7 cells by measuring XTT end points after 72 hrs
Cytotoxicity against dual-reporter HCV replicon Huh7 cells by measuring XTT end points after 72 hrs
[PMID: 17060518]
Huh-7 CC50
60.7 μM
Compound: DRB
Cytotoxicity against dual-reporter HCV replicon Huh7 cells by measuring FLuc reporter activity after 72 hrs
Cytotoxicity against dual-reporter HCV replicon Huh7 cells by measuring FLuc reporter activity after 72 hrs
[PMID: 17060518]
LP-1 IC50
29.81 μM
Compound: DRB
Cytotoxicity against human LP-1 cells after 72 hrs by alamar blue assay
Cytotoxicity against human LP-1 cells after 72 hrs by alamar blue assay
[PMID: 15958589]
MCF7 GI50
36 μM
Compound: DRB
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
[PMID: 22225635]
NCI-H929 IC50
20.13 μM
Compound: DRB
Cytotoxicity against human NCI-H929 cells after 72 hrs by alamar blue assay
Cytotoxicity against human NCI-H929 cells after 72 hrs by alamar blue assay
[PMID: 15958589]
OPM-2 IC50
29.52 μM
Compound: DRB
Cytotoxicity against human OPM2 cells after 72 hrs by alamar blue assay
Cytotoxicity against human OPM2 cells after 72 hrs by alamar blue assay
[PMID: 15958589]
RPMI-8226 IC50
46.79 μM
Compound: DRB
Cytotoxicity against human RPM18226 cells after 72 hrs by alamar blue assay
Cytotoxicity against human RPM18226 cells after 72 hrs by alamar blue assay
[PMID: 15958589]
U-266 IC50
41.02 μM
Compound: DRB
Cytotoxicity against human U266 cells after 72 hrs by alamar blue assay
Cytotoxicity against human U266 cells after 72 hrs by alamar blue assay
[PMID: 15958589]
體外研究
(In Vitro)

5,6-Dichlorobenzimidazole riboside (10-80 μg/mL, 72 h) 通過(guò)阻斷 RNA 合成誘導(dǎo)人結(jié)腸癌細(xì)胞 p53 依賴(lài)性凋亡[5]。
5,6-Dichlorobenzimidazole riboside (10-100 μM, 72 h) 通過(guò)調(diào)控 Mcl-1 和 BclxL 誘導(dǎo)人 MCF-7 乳腺癌細(xì)胞凋亡。并以時(shí)間和劑量依賴(lài)的方式激活半胱天冬酶家族成員[6]。

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

Western Blot Analysis[5]

Cell Line: LS174T, HT29, SW48
Concentration: 80 μg/mL
Incubation Time: 24 h
Result: Decreased incorporation of [5,6-3H] uridine and increased level of p53 protein.

Cell Viability Assay[6]

Cell Line: MCF-7, T-47D
Concentration: 10, 50, 75,100 μM
Incubation Time: 72 h
Result: Inhibited cell-growth in a dose-dependent manner.
Resulted in a higher early apoptotic population (5.7 ± 1.1 vs. 2 ± 0.4%) and late apoptotic population (15.9 ± 2.4 vs. 7.7 ± 0.9%) at a concentration of 75 μM.

Western Blot Analysis[6]

Cell Line: MCF-7
Concentration: 75 μM
Incubation Time: 0.5, 2, 6, 10 h
Result: Reduced Mcl-1 protein levels in a time-dependent manner and increased the level of p53 after 6 h.
體內(nèi)研究
(In Vivo)

5,6-Dichlorobenzimidazole riboside (2.0-3.0 mg/0.25 mL 水, 腹腔注射,一天兩次連續(xù) 5 天) 對(duì)小鼠 PR8 型流感病毒增殖無(wú)抑制作用[7]。

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

319.14

Formula

C12H12Cl2N2O4
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
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 100 mg/mL (313.34 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(kāi)封的 DMSO)

DMF 中的溶解度 : 100 mg/mL (313.34 mM; 超聲助溶)

Ethanol 中的溶解度 : 7.69 mg/mL (24.10 mM; 超聲助溶)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 3.1334 mL 15.6671 mL 31.3342 mL
5 mM 0.6267 mL 3.1334 mL 6.2668 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, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)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 (7.83 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。
  • 方案 二

    請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.83 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 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
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(guò)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(guò) 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(guò)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(guò)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: 99.95%

參考文獻(xiàn)

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, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO / DMF 1 mM 3.1334 mL 15.6671 mL 31.3342 mL 78.3355 mL
5 mM 0.6267 mL 3.1334 mL 6.2668 mL 15.6671 mL
10 mM 0.3133 mL 1.5667 mL 3.1334 mL 7.8336 mL
15 mM 0.2089 mL 1.0445 mL 2.0889 mL 5.2224 mL
20 mM 0.1567 mL 0.7834 mL 1.5667 mL 3.9168 mL
DMSO / DMF 25 mM 0.1253 mL 0.6267 mL 1.2534 mL 3.1334 mL
30 mM 0.1044 mL 0.5222 mL 1.0445 mL 2.6112 mL
40 mM 0.0783 mL 0.3917 mL 0.7834 mL 1.9584 mL
50 mM 0.0627 mL 0.3133 mL 0.6267 mL 1.5667 mL
60 mM 0.0522 mL 0.2611 mL 0.5222 mL 1.3056 mL
80 mM 0.0392 mL 0.1958 mL 0.3917 mL 0.9792 mL
100 mM 0.0313 mL 0.1567 mL 0.3133 mL 0.7834 mL
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  • 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(chēng)：
5,6-Dichlorobenzimidazole riboside
目錄號(hào)：
HY-14392
需求量：