2. Metabolic Enzyme/Protease Apoptosis
  3. Glutaminase Apoptosis
  4. LWG-301

LWG-301 is an allosteric inhibitor of Glutaminase 1 (GLS1) with an IC50 value of 7 nM. LWG-301 significantly block glutamine metabolism, increases intracellular ROS, thus induces apoptosis. LWG-301 exhibits moderate antitumor effects in HCT116 xenograft model.

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LWG-301 Chemical Structure

LWG-301 Chemical Structure

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LWG-301 Related Antibodies

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Description

LWG-301 is an allosteric inhibitor of Glutaminase 1 (GLS1) with an IC50 value of 7 nM. LWG-301 significantly block glutamine metabolism, increases intracellular ROS, thus induces apoptosis. LWG-301 exhibits moderate antitumor effects in HCT116 xenograft model[1].

In Vitro

LWG-301 (compound 41a) inhibits HCT116 cancer cells growth with an IC50 value of 61 nM[1].
LWG-301 has great metabolic stability in human liver microsomes with T1/2=108 min, CL=32 μL/min/mg[1].
LWG-301 (10 μM; 6 h) interacts with GLS1 protein in a dose- and time-dependent manner[1].
LWG-301 (0.03-3 μM; 14 d) inhibits the colony formation of HCT116 cells in a concentration-dependent manner[1].
LWG-301 (0.2 μM, 1 μM, 5 μM; 24 h) blocks the metabolism of glutamine thus results a decrease of glutamate, glutathione, and fumaric acid[1].
LWG-301 (1-10 μM; 24 h) induces ROS production and (0.1-10 μM; 24 h) induces apoptosis in HCT116 cells[1].

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

LWG-301 Related Antibodies

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.001, 0.01, 0.1, 1, and 10 μM
Incubation Time: 10, 30, 60, 180, 240 min
Result: Showed the interaction with GLS1 in a dose- and time-dependent manner.

Immunofluorescence[1]

Cell Line: HCT116 cells
Concentration: 1, 5, and 10 μM
Incubation Time: 6 hours
Result: Induced ROS production in HCT116 cells.

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.1, 0.3, 1, 3, and 10 μM
Incubation Time: 24 hours
Result: Induced apoptosis in HCT116 cells
In Vivo

LWG-301 (compound 41a) (100 mg/kg; i.p.; once daily for 20 d) shows anti-tumor activity without in HCT116 xenograft tumor model in mice[1].

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

Animal Model: HCT116 tumor-bearing nude mice[1]
Dosage: 100 mg/kg;
Administration: Intraperitoneal injection; once a day for 20 days;
Result: Reduced tumor growth, resulting in 38.9% tumor growth inhibition.
Showed little toxicity on main organ.
Molecular Weight

566.72

Formula

C28H38N8O3S
SMILES

CCCCOC1=CC=CC(CC(NC2=NN=C(C=C2)N3CCC(CC3)NC4=NN=C(S4)NC(CCCC)=O)=O)=C1
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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LWG-301 Related Classifications

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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:

LWG-301LWG301LWG 301GlutaminaseApoptosisInhibitorinhibitorinhibit

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