2-Guanidinobezimidazole
Based on 1 Customer Validation
2-Guanidinobezimidazole (2GBI) is a NLRP3 agonist with a KD of 1.29 μM and a selective state-dependent HVCN1 blocker. 2-Guanidinobezimidazole directly binds NLRP3’s LRR domain, enhances NLRP3-ASC and NLRP3-NEK7 interactions, and drives NLRP3 inflammasome activation. 2-Guanidinobezimidazole can be used for the research of LLC lung carcinoma, B16F10 melanoma and ischemic stroke.
For research use only. We do not sell to patients.
- Purity: 95.74%
- CAS No.: 5418-95-1
- Formula: C8H9N5
- Molecular Weight:175.19
-
Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
All Vasopressin Receptor Isoforms
More
Biological Activity
|
NLRP3 |
2-Guanidinobezimidazole rapidly inhibits proton conduction in wild-type human Hv1 channels expressed in Xenopus laevis oocytes via open-channel block, with fast binding and unbinding kinetics, and does not interact with closed channel states[2].
2-Guanidinobezimidazole interacts with human Hv1 mutant channels (D112E, F150A) expressed in Xenopus laevis oocytes via a binding site comprising residues D112 and F150, with mutations at these sites altering the fast open-channel block kinetics[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
2-Guanidinobezimidazole (20 mg/kg; i.p.; every other day) overcomes anti-PD-1 resistance and exerts synergistic anti-tumor effects in LLC tumor-bearing C57BL/6J mice[1].
2-Guanidinobezimidazole (20 mg/kg; i.p.; every other day) significantly inhibits B16F10 melanoma growth in C57BL/6J mice[1].
2-Guanidinobezimidazole (20 mg/kg; i.p.; every other day) activates inflammasomes, inhibits tumor growth, and enhances anti-tumor immunity in a NLRP3-dependent manner in LLC tumor-bearing mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6J (8-12 weeks old; subcutaneously injected with 1.5 × 106 LLC cells)[1]
-
Dosage:20 mg/kg
-
Administration:i.p.; every other day
-
Result:Increased tumor tissue IL-1β levels to ~2500 pg/mL/100 mg (n=7,8) and IL-18 levels to ~1500 pg/mL/100 mg (n=6).
Increased the proportion of caspase-1+ macrophages to 33.9% (n=6), caspase-1+ DCs to 32.8% (n=5), and caspase-1+ neutrophils to 20.7% (n=5) in tumors.
Reduced LLC tumor volume to ~300 mm3 at day 30 (n=6) and tumor weight to ~0.5 g (n=6).
Increased tumor-infiltrating CD4+ T cell counts to ~15 × 105 (n=7) and CD8+ T cell counts to ~8 × 105 (n=7).
Increased the percentage of IFN-γ+ CD8+ T cells to 17.5% (n=7).
Increased migratory DC counts to ~6 × 103 (n=5) and increased CD40 MFI to ~1400 and CD86 MFI to ~1600 on DCs in tumor-draining lymph nodes (n=5).\nReduced LLC tumor volume to ~400 mm3 at day 30 when administered alone.
Further reduced tumor volume to ~200 mm3 at day 30 (n=5,6) when combined with anti-PD-1, overcoming anti-PD-1 resistance.
-
Animal Model:C57BL/6J (8-12 weeks old; subcutaneously injected with 1.5 × 106 B16F10 cells)[1]
-
Dosage:20 mg/kg
-
Administration:i.p.; every other day
-
Result:Significantly inhibited B16F10 tumor growth.
-
Animal Model:C57BL/6J (8-12 weeks old, specific pathogen-free; wild-type and Nlrp3-/-)[1]
-
Dosage:20 mg/kg
-
Administration:i.p.; every other day
-
Result:Increased tumor IL-1β levels to ~4000 pg/mL/100 mg (n=5) and IL-18 levels to ~1800 pg/mL/100 mg (n=5), and increased caspase-1+ macrophage proportion to 26.9% (n=5) in WT mice; these effects were abolished in Nlrp3-/- mice.
Reduced WT mouse tumor volume to ~200 mm3 at day 26 (n=5) and tumor weight to ~0.5 g (n=5); no such effect was observed in Nlrp3-/- mice.
Increased tumor-infiltrating CD4+ T cell counts to ~25 × 105 (n=5) and CD8+ T cell counts to ~20 × 105 (n=5), and increased IFN-γ+ CD8+ T cell percentage to 22.9% (n=5) in WT mice; none of these effects were observed in Nlrp3-/- mice.
Chemical Information
-
CAS No. 5418-95-1
-
Appearance Solid
-
Molecular Weight 175.19
-
Formula C8H9N5
-
Color White to light yellow
-
SMILES
N/C(N)=N/C1=NC2=CC=CC=C2N1
-
Synonyms
2GBI
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 250 mg/mL (1427.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (11.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (11.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
-
Data Sheet (279 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
[1]. Liu X, et al. A small molecule directly targets NLRP3 to promote inflammasome activation and antitumor immunity. Cell Death Dis. 2025;16(1):252. Published 2025 Apr 4. [Content Brief]
[2]. Zhao C, et al. A novel Hv1 inhibitor reveals a new mechanism of inhibition of a voltage-sensing domain. J Gen Physiol. 2021;153(9):e202012833. [Content Brief]
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 (protect from light). 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 | 5.7081 mL | 28.5404 mL | 57.0809 mL | 142.7022 mL |
| 5 mM | 1.1416 mL | 5.7081 mL | 11.4162 mL | 28.5404 mL | |
| 10 mM | 0.5708 mL | 2.8540 mL | 5.7081 mL | 14.2702 mL | |
| 15 mM | 0.3805 mL | 1.9027 mL | 3.8054 mL | 9.5135 mL | |
| 20 mM | 0.2854 mL | 1.4270 mL | 2.8540 mL | 7.1351 mL | |
| 25 mM | 0.2283 mL | 1.1416 mL | 2.2832 mL | 5.7081 mL | |
| 30 mM | 0.1903 mL | 0.9513 mL | 1.9027 mL | 4.7567 mL | |
| 40 mM | 0.1427 mL | 0.7135 mL | 1.4270 mL | 3.5676 mL | |
| 50 mM | 0.1142 mL | 0.5708 mL | 1.1416 mL | 2.8540 mL | |
| 60 mM | 0.0951 mL | 0.4757 mL | 0.9513 mL | 2.3784 mL | |
| 80 mM | 0.0714 mL | 0.3568 mL | 0.7135 mL | 1.7838 mL | |
| 100 mM | 0.0571 mL | 0.2854 mL | 0.5708 mL | 1.4270 mL |
2-Guanidinobezimidazole Related Classifications
HY-W158030 Related Classifications
Powered by Bioz