WQQ-345
WQQ-345 is an orally active BCAT1 inhibitor with an IC50 values of 10.8 mM. WQQ-345 reduces cellular α-KG levels, upregulating H3K27me3 expression, decreasing glycolytic enzyme expression, and impairing glycolysis activity. WQQ-345 reduces colony formation, suppresses growth of BCAT1-high TKI-resistant lung cancer cells. WQQ-345 exerts in vitro and in vivo antitumor activity. WQQ-345 can be used for the research of TKI-resistant non-small cell lung cancer and TKI-resistant lung cancer.
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- Fòrmula: C10H17NO2
- Peso molecular:183.25
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
In Vitro
WQQ-345 (2.5-5 mM; 7-10 days) dose-dependently inhibits colony formation of 67R NSCLC cells[1].
WQQ-345 (5-10 mM; 3 days) dose-dependently reduces intracellular α-KG levels, upregulates H3K27me3 protein expression, and downregulates PFKP and LDHA protein expression in 67R NSCLC cells after 3 days of treatment at 5 mM or 10 mM[1].
WQQ-345 (5 mM; 3 days) impairs glycolytic activity (lowered ECAR) in 67R NSCLC cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:ASK120067-resistant NCI-H1975 (67R) NSCLC cells
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Concentration:2.5, 5 mM
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Incubation Time:7-10 days
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Result:Dose-dependently reduced colony formation of 67R cells, with significant inhibition observed at both 2.5 mM and 5 mM.
Resulted in stronger growth inhibition when co-treated with 1 μM ASK120067 (HY-138751) than either monotherapy.
Lost growth-inhibitory effects in 67R cells with BCAT1 knockdown, confirming on-target activity.
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Cell Line:ASK120067-resistant NCI-H1975 (67R) NSCLC cells
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Concentration:5, 10 mM
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Incubation Time:3 days
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Result:Dose-dependently upregulated H3K27me3 protein expression in 67R cells.
Left BCAT1 protein expression unchanged in 67R cells.\n
Dose-dependently reduced protein levels of glycolytic enzymes PFKP and LDHA in 67R cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (4-week-old) subcutaneously injected with 67R cells[1]
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Dosage:80; 120 mg/kg
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Administration:p.o.; twice daily; 43 days
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Result:Achieved robust tumor regression at 120 mg/kg, with significantly smaller tumor volumes compared to vehicle control by day 43.
Increased H3K27me3 protein expression significantly in tumors treated with 120 mg/kg relative to vehicle control tumors.
Decreased protein levels of glycolytic enzymes PFKP, LDHA, and PKM1/2 significantly in tumors treated with 120 mg/kg relative to vehicle control tumors.
Chemical Information
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Peso molecular 183.25
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Fòrmula C10H17NO2
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SMILES
O=C(O)C[C@]1(CN)[C@](C2)([H])CC[C@]2([H])C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Zhang T, et al. Branched-chain amino acid transaminase 1 confers EGFR-TKI resistance through epigenetic glycolytic activation. Signal Transduct Target Ther. 2024;9(1):216. Published 2024 Aug 15. [Content Brief]
[2]. Luo W, et al. Design, Synthesis and Biological Activity Study of γ-Aminobutyric Acid (GABA) Derivatives Containing Bridged Bicyclic Skeletons as BCAT1 Inhibitors. Molecules. 2025;30(4):904. Published 2025 Feb 15. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
WQQ-345 Related Classifications
HY-169061 Related Classifications
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Keywords
- WQQ-345
- WQQ345
- WQQ 345
- Histone Methyltransferase
- Aminotransferases (Transaminases)
- Lactate Dehydrogenase
- Aminotransferases (Transaminases)
- LDH
- EGFR TKI-resistant NSCLC cells
- H3K27me3
- lung cancer
- non-small cell lung cancer
- BCAT1
- LDHA
- 67R NSCLC cells
- branched-chain amino acid catabolism
- PFKP
- NSCLC xenograft models
- Inhibitor
- inhibitor
- inhibit