YTB53
YTB53 is a MNK1 and MNK2 inhibitor with IC50s of 37 nM and 9 nM, respectively. YTB53 inhibits PDGFRα, TRKB and FLT3 in leukemia cells. YTB53 induces cell cycle arrest, apoptosis, pyroptosis, and mitochondrial dysfunction. YTB53 exhibits antiangiogenic effects. YTB53 can be used for the study of acute myeloid leukemia (AML).
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- 分子式: C18H13N3O2
- 分子量:303.31
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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]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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MNK1 37 nM (IC50) |
MNK2 9 nM (IC50) |
FLT3 0.47 nM (IC50) |
PDGFRα |
TrkB |
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Cell Line
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Type | Value | Description | References |
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| MV4-11 | IC50 |
2 nM
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Inhibits cell growth of MV4-11 cells for 72 h.
Inhibits cell growth of MV4-11 cells for 72 h.
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42223949 |
YTB53 (copmound 31) (72 h) inhibits cell growth of MV4-11 cells with an IC50 of 2 nM[1].
YTB53 (1 μM; 2 h) inhibits eIF4E phosphorylation at Ser209 in HEK293T cells[1].
YTB53 (1 μM) exhibits strong inhibitory activity against PDGFRα (98.88%) and TRKB (97.43%). YTB53 inhibits FLT3 with an IC50 of 0.470 nM[1].
YTB53 (0.1-10 μM; 24 h) inhibits eIF4E phosphorylation at Ser209 in MV4-11 cells[1].
YTB53 (0.05-0.2 μM; 24 h) induces cell cycle arrest in MV4-11 cells[1].
YTB53 (0.05-0.2 μM; 48 h) induces cell apoptosis and pyroptosis in MV4-11 cells[1].
YTB53 (0.05-0.2 μM; 24 h) effectively triggeres a substantial increase in ROS generation and a concurrent decrease in mitochondrial membrane potential[1].
YTB53 (0.05-0.2 μM; 0-24 h) exerts a dual antiangiogenic action, suppressing both endothelial morphogenesis and migration in human umbilical vein endothelial cells (HUVECs)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells
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Concentration:1 μM
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Incubation Time:2 h
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Result:Demonstrated the most potent activity, nearly completely abolishing p-eIF4E levels at 1 μM.
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Cell Line:MV4-11 cells
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Concentration:0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM
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Incubation Time:24 h
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Result:Completely inhibited the expression of p-eIF4E even at a low concentration of 0.3 μM, while a concentration of 0.1 μM exhibited partial inhibition.
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Cell Line:MV4-11 cells
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Concentration:0.05 μM, 0.1 μM, 0.2 μM
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Incubation Time:24 h
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Result:Showed a 24 h treatment induced a concentration-dependent arrest at the G0/G1 phase.
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Cell Line:MV4-11 cells
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Concentration:0.05 μM, 0.1 μM, 0.2 μM
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Incubation Time:24 h
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Result:Inhibited cyclin E-CDK2 activity.
Pronounced downregulation of cyclin B1 and its kinase partner CDC2 (CDK1) disables the core engine required for G2/M progression.
Increased the phosphorylated p53 (p-p53) protein levels.
Decreased the total p53 protein levels.
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Cell Line:MV4-11 cells
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Concentration:0.05 μM, 0.1 μM, 0.2 μM
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Incubation Time:48 h
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Result:Led to a dose-dependent increase in the proportion of cells undergoing apoptosis.
Revealed a coordinated downregulation of the antiapoptotic proteins Bcl-2 and Bcl-XL, alongside a reduction in the pro-apoptotic protein Bax-a change.
Decreased the inactive forms of caspase-8, caspase-9, and caspase-3.
The levels of both full-length and cleaved PARP remained largely unchanged.
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Cell Line:MV4-11 cells
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Concentration:0.05 μM, 0.1 μM, 0.2 μM
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Incubation Time:24 h
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Result:Led to significantly elevated levels of lactate dehydrogenase (LDH) and the pro-inflammatory cytokine IL-18.
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Cell Line:MV4-11 cells
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Concentration:0.05 μM, 0.1 μM, 0.2 μM
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Incubation Time:24 h
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Result:Showed a significant increase in NLRP3 (NOD-like receptor protein 3) protein levels.
Decreased the level of full-length GSDMD (Gasdermin D).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nude mice received a 200 μL subcutaneous injection into the right axillary containing a 1:1 (v/v) mixture of human acute myeloid leukemia MV4-11 cells and Matrigel[1].
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Dosage:10 mg/kg, 20 mg/kg, 40 mg/kg
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Administration:s.c.; once a day; 14 days
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Result:Significantly inhibited tumor growth in a dose-dependent manner.
H&E staining revealed no evidence of inflammatory infiltrates, fibrosis, or architectural disruption in these tissues.
Did not significantly suppress ki-67 expression at low and medium doses (10 and 20 mg/kg) but markedly reduced its levels at the highest dose (40 mg/kg).
Significantly downregulated the expression of p-eIF4E, p53, caspase-9, and Bcl-2.
Elicited a strong inflammatory response at lower doses. However, as the dose increased, the level of inflammation decreased markedly.
化学情報
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分子量 303.31
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分子式 C18H13N3O2
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SMILES
O=C(N)C1=CC=C(C=C1)C2=CN=C(O2)C3=CC4=CC=CC=C4N3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
YTB53 関連分類
HY-184431 関連分類
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