1. Metabolic Enzyme/Protease
    Apoptosis
  2. Glutaminase
    Apoptosis
  3. GLS1 Inhibitor-6

GLS1 Inhibitor-6 

Cat. No.: HY-151434
Handling Instructions

GLS1 Inhibitor-6 (Compound 24y) is an orally active, potent and selective glutaminase 1 (GLS1) inhibitor (IC50=68 nM), shows 220-fold selectivity for GLS2. GLS1 Inhibitor-6 shows good anti-tumor activity, antitumor cell proliferation activity and induces apoptosis.

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

GLS1 Inhibitor-6 Chemical Structure

GLS1 Inhibitor-6 Chemical Structure

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Description

GLS1 Inhibitor-6 (Compound 24y) is an orally active, potent and selective glutaminase 1 (GLS1) inhibitor (IC50=68 nM), shows 220-fold selectivity for GLS2. GLS1 Inhibitor-6 shows good anti-tumor activity, antitumor cell proliferation activity and induces apoptosis[1].

IC50 & Target

IC50: 68 nM (GLS1)[1]

In Vitro

GLS1 Inhibitor-6 (0-10 μM) inhibts cancer cell growth[1].
GLS1 Inhibitor-6 (1-10 μM, 48 h) can induce A549 cell apoptosis[1].
GLS1 Inhibitor-6 (50-800 nM, 48 h) can induce cell cycle arrest in the G1 phase[1].

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

Cell Viability Assay[1]

Cell Line: A549 and HCT116 cell
Concentration: 0-10 μM
Incubation Time:
Result: Inhibited A549 and HCT116 cell growth with IC50s of 0.57 and 0.42 μM, respectively.

Apoptosis Analysis[1]

Cell Line: A549 cell
Concentration: 1, 5, and 10 μM
Incubation Time: 48 h
Result: Showed the population of apoptotic cells to 84% at the concentration of 10 μM.

Cell Cycle Analysis[1]

Cell Line: A549 cell
Concentration: 50, 100, 200, 400 and 800 nM
Incubation Time: 48 h
Result: Resulted in G1 phase cell cycle arrest in a dose-dependent manner, and decreased proportion of cells in the S phase.
In Vivo

GLS1 Inhibitor-6 (oral gavage; 100 mg/kg; once daily; 28 d) treatment inhibits tumor growth in the preclinical mouse models[1].

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

Animal Model: Rats[1]
Dosage: 3 mg/kg
Administration: I.V. and P.O.; 3 mg/kg; once
Result: 1.19 The pharmacokinetic parameters of GLS1 Inhibitor-5 (compound 24y)[1].
Parameters I.V. P.O.
t1/2 (h) 9.9 19.8
CL (L/h/kg) 6.1 33.4
Cmax ng/mL 699.1 41.3
AUC0–t (ng·h/mL) 2092.3 251.6
F% 12.4
Animal Model: Human non-small cell lung A549 xenograft tumor model, GLS1 high-expression HCT116 xenograft tumor model[1]
Dosage: 100 mg/kg
Administration: Oral gavage; 100 mg/kg; once daily; 28 days
Result: Showed 40.9% tumor growth inhibition in A549 model, and showed 42% tumor growth inhibition in HCT116 model.
Molecular Weight

660.91

Formula

C37H52N6O3S

SMILES

O=C(NCC1CCN(CCCCCC)CC1)C2=CC=CC(COCCC3CCN(C4=NN=C(NC(CC5=CC=CC=C5)=O)S4)CC3)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Product Name:
GLS1 Inhibitor-6
Cat. No.:
HY-151434
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