2. Metabolic Enzyme/Protease
  3. Glutaminase
  4. GLS1 Inhibitor-1

GLS1 Inhibitor-1 (Compound 27) is an orally active inhibitor for glutaminase 1 (GLS1) with an IC50 of 0.021 μM. GLS1 Inhibitor-1 inhibits the proliferation of PC-3 with an IC50 of 0.3 nM. GLS1 Inhibitor-1 exhibits antitumor efficacy against NCI-H1703 with GI50 of 0.011 μM. GLS1 Inhibitor-1 exhibits moderate pharmacokinetic characteristics.

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GLS1 Inhibitor-1

GLS1 Inhibitor-1 Chemical Structure

CAS No. : 1832646-52-2

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Based on 1 publication(s) in Google Scholar

GLS1 Inhibitor-1 Related Antibodies

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Description

GLS1 Inhibitor-1 (Compound 27) is an orally active inhibitor for glutaminase 1 (GLS1) with an IC50 of 0.021 μM. GLS1 Inhibitor-1 inhibits the proliferation of PC-3 with an IC50 of 0.3 nM. GLS1 Inhibitor-1 exhibits antitumor efficacy against NCI-H1703 with GI50 of 0.011 μM. GLS1 Inhibitor-1 exhibits moderate pharmacokinetic characteristics[1].

IC50 & Target

IC50: 0.021 μM (GLS1)
Cellular Effect
Cell Line Type Value Description References
A549 IC50
12.59 nM
Compound: 6a
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by Celltiter-glo assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by Celltiter-glo assay
[PMID: 37849538]
CHO IC50
> 33.3 μM
Compound: 27
Inhibition of human ERG expressed in CHO cells by Ionworks electrophysiology assay
Inhibition of human ERG expressed in CHO cells by Ionworks electrophysiology assay
[PMID: 31199640]
NCI-H1703 GI50
0.011 μM
Compound: 27
Antiproliferative activity against human NCI-H1703 cells assessed as reduction in cell growth after 5 days by SYTOX green staining-based assay
Antiproliferative activity against human NCI-H1703 cells assessed as reduction in cell growth after 5 days by SYTOX green staining-based assay
[PMID: 31199640]
Molecular Weight

411.48

Formula

C19H21N7O2S
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C([C@H](C1=CC=CC=C1)OC)NC2=NN=C(S2)N[C@H]3CN(C4=CC=CN=N4)CC3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (48.61 mM; Need ultrasonic and warming; 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 2.4303 mL 12.1513 mL 24.3025 mL
5 mM 0.4861 mL 2.4303 mL 4.8605 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.59%

SDS (252 KB)

COA (250 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 (sealed storage, away from moisture). 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 2.4303 mL 12.1513 mL 24.3025 mL 60.7563 mL
5 mM 0.4861 mL 2.4303 mL 4.8605 mL 12.1513 mL
10 mM 0.2430 mL 1.2151 mL 2.4303 mL 6.0756 mL
15 mM 0.1620 mL 0.8101 mL 1.6202 mL 4.0504 mL
20 mM 0.1215 mL 0.6076 mL 1.2151 mL 3.0378 mL
25 mM 0.0972 mL 0.4861 mL 0.9721 mL 2.4303 mL
30 mM 0.0810 mL 0.4050 mL 0.8101 mL 2.0252 mL
40 mM 0.0608 mL 0.3038 mL 0.6076 mL 1.5189 mL
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GLS1 Inhibitor-1 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:

GLS1 Inhibitor-11832646-52-2GlutaminaseSCID mousePC-3NCI-H1703orally activeWistar ratInhibitorinhibitorinhibit

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