| Description |
VY-3-135 is an orally active, selective acetyl-CoA synthetase 2 (ACSS2) inhibitor with an IC50 value of 44 nM. VY-3-135 displayes no inhibitory activity towards recombinant human ACSS1 or ACSS3. VY-3-135 potently inhibits ACSS2 dependent fatty acid metabolism but has no effect on gene expression in tumors. VY-3-135 inhibits triple negative breast cancer (TNBC) tumor growth in mouse ACSS2high but not ACSS2low tumors models[1].
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| Related Catalog |
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| In Vitro |
VY-3-135 (0.1, 1 μM; for 24 hours) blocks acetate dependent labeling of palmitate by 13C2-acetate in ACSS2low A7C11 and ACSS2high Brpkp110 cells[1].
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| In Vivo |
VY-3-135 (100 mg/kg/day; PO; 30 days) represses MDA-MB-468 (ACSS2high) tumor growth but is mostly ineffective at blocking WHIM12 (ACSS2low) growth[1].
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| References |
[1]. Katelyn D Miller, et al. Targeting ACSS2 with a Transition-State Mimetic Inhibits Triple-Negative Breast Cancer Growth. Cancer Res. 2021 Mar 1;81(5):1252-1264.
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