1. Metabolic Enzyme/Protease
  2. Glutaminase
  3. 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 Chemical Structure

GLS1 Inhibitor-1 Chemical Structure

CAS No. : 1832646-52-2

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Based on 1 publication(s) in Google Scholar

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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
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.
SMILES

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

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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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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.

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GLS1 Inhibitor-1
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HY-136704
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