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

5,6-Dichlorobenzimidazole riboside  (Synonyms: DRB)

Cat. No.: HY-14392 Purity: 99.90%
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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.

For research use only. We do not sell to patients.

5,6-Dichlorobenzimidazole riboside Chemical Structure

5,6-Dichlorobenzimidazole riboside Chemical Structure

CAS No. : 53-85-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 33 In-stock
Solution
10 mM * 1 mL in DMSO USD 33 In-stock
Solid
5 mg USD 30 In-stock
10 mg USD 45 In-stock
25 mg USD 90 In-stock
50 mg USD 135 In-stock
100 mg USD 200 In-stock
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Based on 3 publication(s) in Google Scholar

5,6-Dichlorobenzimidazole riboside Related Antibodies

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

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  • Purity & Documentation

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Description

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].

In Vitro

5,6-Dichlorobenzimidazole riboside (10-80 μg/mL, 72 h) induces p53-dependent apoptosis of human colon cancer cells by blocking RNA synthesis[5].
5,6-Dichlorobenzimidazole riboside (10-100 μM, 72 h) induces apoptosis of human MCF-7 breast cancer cells by regulating Mcl-1 and BclxL. And activates members of the caspase family in a time - and dose-dependent manner[6].

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

5,6-Dichlorobenzimidazole riboside Related Antibodies

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.
In Vivo

5,6-Dichlorobenzimidazole riboside (2.0-3.0 mg/0.25 mL water,  intraperitoneally injected twice a day for 5 days) does not inhibit the multiplication of the PR8 strain of influenza virus in mice[7].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

319.14

Formula

C12H12Cl2N2O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC[C@@H]1[C@@H](O)[C@@H](O)[C@H](N2C3=CC(Cl)=C(Cl)C=C3N=C2)O1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMF : 100 mg/mL (313.34 mM; Need ultrasonic)

DMSO : 100 mg/mL (313.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 7.69 mg/mL (24.10 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.83 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.83 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.95%

COA (253 KB) HNMR (273 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol / DMF / DMSO 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
DMF / DMSO 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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5,6-Dichlorobenzimidazole riboside Related Classifications

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:

5,6-Dichlorobenzimidazole riboside53-85-0DRBCDKApoptosisCyclin dependent kinaseInhibitorAntitumorLS174TMCF-7RNA synthesisinhibitorinhibit

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