2. Cell Cycle/DNA Damage Apoptosis
  3. DNA/RNA Synthesis Apoptosis
  4. O6-Benzylguanine

O6-Benzylguanine, a guanine analog, is the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase (MGMT/AGT) inhibitor. O6-Benzylguanine acts as an AGT substrate, which transfers its benzyl group to the AGT cysteine residue, thereby irreversibly inactivating AGT and preventing DNA repair. O6-Benzylguanine induces tumor cell apoptosis. Antineoplastic activity.

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O6-Benzylguanine Chemical Structure

O6-Benzylguanine Chemical Structure

CAS No. : 19916-73-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 30 In-stock
Solution
10 mM * 1 mL in DMSO USD 30 In-stock
Solid
5 mg USD 20 In-stock
10 mg USD 26 In-stock
25 mg USD 51 In-stock
50 mg USD 79 In-stock
100 mg USD 129 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

O6-Benzylguanine Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE O6-Benzylguanine

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  • Purity & Documentation

  • References

  • Customer Review

Description

O6-Benzylguanine, a guanine analog, is the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase (MGMT/AGT) inhibitor. O6-Benzylguanine acts as an AGT substrate, which transfers its benzyl group to the AGT cysteine residue, thereby irreversibly inactivating AGT and preventing DNA repair. O6-Benzylguanine induces tumor cell apoptosis. Antineoplastic activity[1][2].

In Vitro

The L3.6pl cells are relatively sensitive to O6-Benzylguanine (24-72 hours) in a dose- and time-dependent manner. The IC50 is 50 μg (at 48 hours)[2].
O6-Benzylguanine (50 μg; 48 hours) modulates p53 downstream target protein expression, induces apoptosis, and decreases cell proliferation[2].
O6-Benzylguanine (50 μg; 48 hours) significantly decreases the MGMT transcriptional activity in L3.6pl[2].

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

O6-Benzylguanine Related Antibodies

Western Blot Analysis[2]

Cell Line: L3.6pl and PANC1 cells
Concentration: 50 μg
Incubation Time: 48 hours
Result: Expressions of O6 methyl guanine DNA methyl transferase (MGMT), cyclin B1, cyclin B2, cyclin A, p53, and ki-67 were decreased, whereas p21 was increased. The levels of cyto C and caspase 9 were increased, whereas the levels of PARP1 protein were decreased.

RT-PCR[2]

Cell Line: L3.6pl cells
Concentration: 50 μg
Incubation Time: 48 hours
Result: Decreased the MGMT transcriptional activity in L3.6pl.
In Vivo

O6-Benzylguanine (100 μg; i.p.; daily for 35 days) inhibits pancreatic cancer cell growth and increases pancreatic cell sensitivity to Gemcitabine (100 mg/kg)[2].
O6-Benzylguanine inhibits pancreatic cancer cell proliferation and induces tumor cell apoptosis in vivo[2].

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

Animal Model: Male athymic nude mice (NCI-nu) (bearing human pancreatic cancer L3.6pl cells)[2]
Dosage: 100 μg
Administration: i.p; daily for 35 days
Result: Significantly decreased median tumor volume and weight.
Molecular Weight

241.25

Formula

C12H11N5O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC(N=C1OCC2=CC=CC=C2)=NC3=C1NC=N3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

RT, protect from light
Solvent & Solubility
In Vitro: 

DMSO : 110 mg/mL (455.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.1451 mL 20.7254 mL 41.4508 mL
5 mM 0.8290 mL 4.1451 mL 8.2902 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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.75 mg/mL (11.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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% Corn Oil

    Solubility: ≥ 2.75 mg/mL (11.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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: 99.84%

COA (249 KB) HNMR (126 KB) RP-HPLC (248 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
DMSO 1 mM 4.1451 mL 20.7254 mL 41.4508 mL 103.6269 mL
5 mM 0.8290 mL 4.1451 mL 8.2902 mL 20.7254 mL
10 mM 0.4145 mL 2.0725 mL 4.1451 mL 10.3627 mL
15 mM 0.2763 mL 1.3817 mL 2.7634 mL 6.9085 mL
20 mM 0.2073 mL 1.0363 mL 2.0725 mL 5.1813 mL
25 mM 0.1658 mL 0.8290 mL 1.6580 mL 4.1451 mL
30 mM 0.1382 mL 0.6908 mL 1.3817 mL 3.4542 mL
40 mM 0.1036 mL 0.5181 mL 1.0363 mL 2.5907 mL
50 mM 0.0829 mL 0.4145 mL 0.8290 mL 2.0725 mL
60 mM 0.0691 mL 0.3454 mL 0.6908 mL 1.7271 mL
80 mM 0.0518 mL 0.2591 mL 0.5181 mL 1.2953 mL
100 mM 0.0415 mL 0.2073 mL 0.4145 mL 1.0363 mL
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O6-Benzylguanine 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:

O6-Benzylguanine19916-73-5DNA/RNA SynthesisApoptosisguanineanalogantineoplasticp53cyclinAPARP1p21transcriptionalpancreaticcancerInhibitorinhibitorinhibit

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