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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C10H17NO2
- 分子量:183.25
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
Histone Methyltransferase アイソフォーム固有の製品をすべて表示
More
生物活性
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.
-
Cell Line:ASK120067-resistant NCI-H1975 (67R) NSCLC cells
-
Concentration:2.5, 5 mM
-
Incubation Time:7-10 days
-
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.
-
Cell Line:ASK120067-resistant NCI-H1975 (67R) NSCLC cells
-
Concentration:5, 10 mM
-
Incubation Time:3 days
-
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c nude (4-week-old) subcutaneously injected with 67R cells[1]
-
Dosage:80; 120 mg/kg
-
Administration:p.o.; twice daily; 43 days
-
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.
化学情報
-
分子量 183.25
-
分子式 C10H17NO2
-
SMILES
O=C(O)C[C@]1(CN)[C@](C2)([H])CC[C@]2([H])C1
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
WQQ-345 関連分類
HY-169061 関連分類
Powered by Bioz