Glutaminase-IN-1
Based on 1 publication(s) in Google Scholar
Glutaminase-IN-1 (CB839 derivative), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM. Glutaminase-IN-1 (CB839 derivative) shows improved cellular uptake and antitumor activity.
For research use only. We do not sell to patients.
- Purity: 98.09%
- CAS No.: 2247127-79-1
- Formula: C26H24F3N7O3Se
- Molecular Weight:618.47
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Glutaminase-IN-1
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Biological Activity
IC50: 1 nM (KGA)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.017 μM
Compound: CPD20
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Antiproliferative activity against human A549 cells after 5 days by EZMTT reagent-based assay
Antiproliferative activity against human A549 cells after 5 days by EZMTT reagent-based assay
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[PMID: 30543285] |
| CAKI-1 | IC50 |
0.019 μM
Compound: CPD20
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Antiproliferative activity against human Caki1 cells after 5 days by EZMTT reagent-based assay
Antiproliferative activity against human Caki1 cells after 5 days by EZMTT reagent-based assay
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[PMID: 30543285] |
| H22 | IC50 |
6.78 μM
Compound: CPD20
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Antiproliferative activity against mouse H22 cells after 5 days by EZMTT reagent-based assay
Antiproliferative activity against mouse H22 cells after 5 days by EZMTT reagent-based assay
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[PMID: 30543285] |
| HCT-116 | IC50 |
0.009 μM
Compound: CPD20
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Antiproliferative activity against human HCT116 cells after 5 days by EZMTT reagent-based assay
Antiproliferative activity against human HCT116 cells after 5 days by EZMTT reagent-based assay
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[PMID: 30543285] |
Glutaminase-IN-1 (CPD20), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM. Glutaminase-IN-1 shows improved cellular uptake and antitumor activity. The IC50 values of Glutaminase-IN-1 are 17 nM, 6.78 μM, 19 nM and 9 nM in A549, H2, Caki-1 and HCT116 cell lines, respectively. Glutaminase-IN-1 has better KGA inhibitory activity than the corresponding BPTES and CB839[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2247127-79-1
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Appearance Solid
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Molecular Weight 618.47
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Formula C26H24F3N7O3Se
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Color Light yellow to yellow
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SMILES
O=C(NC1=NN=C(CCCCC2=NN=C(NC(CC3=CC=CC(OC(F)(F)F)=C3)=O)C=C2)[Se]1)CC4=NC=CC=C4
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Synonyms
CB839 derivative
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Mol Oncol
HRD1 inhibits fatty acid oxidation and tumorigenesis by ubiquitinating CPT2 in triple-negative breast cancer. [Abstract]2021 Feb;15(2):642-656. PMID: 33207079
Solvent & Solubility
DMSO : 25 mg/mL (40.42 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 1.44 mg/mL (2.33 mM); Clear solution
This protocol yields a clear solution of ≥ 1.44 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.4 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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
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
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Data Sheet (269 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6169 mL | 8.0845 mL | 16.1689 mL | 40.4223 mL |
| 5 mM | 0.3234 mL | 1.6169 mL | 3.2338 mL | 8.0845 mL | |
| 10 mM | 0.1617 mL | 0.8084 mL | 1.6169 mL | 4.0422 mL | |
| 15 mM | 0.1078 mL | 0.5390 mL | 1.0779 mL | 2.6948 mL | |
| 20 mM | 0.0808 mL | 0.4042 mL | 0.8084 mL | 2.0211 mL | |
| 25 mM | 0.0647 mL | 0.3234 mL | 0.6468 mL | 1.6169 mL | |
| 30 mM | 0.0539 mL | 0.2695 mL | 0.5390 mL | 1.3474 mL | |
| 40 mM | 0.0404 mL | 0.2021 mL | 0.4042 mL | 1.0106 mL |
Glutaminase-IN-1 Related Classifications
HY-114334 Related Classifications
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