YL-602
YL-602 is an orally active Hippo pathway activator. YL-602 activates the Hippo pathway via MST1/2, with downstream pathway activation. YL-602 inhibits YAP and CTGF expression in cells irrespective of cell density and serum presence. YL-602 induces tumor cell apoptosis and inhibits colony formation. YL-602 suppresses tumor growth in mice. YL-602 can be used for the research of cancer, such as breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 3081701-84-7
- Formula: C17H11NO4
- Molecular Weight:293.27
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Storage:
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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Biological Activity
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Chemical Information
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- References
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Biological Activity
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MST1 |
MST2 |
YL-602 (0.01-100 μM; 24 h) potently inhibits CTGF promoter activity in A549-CTGF cells with an EC50 of 0.474 μM[1].
YL-602 (0.62-10 μM; 24 h) activates the Hippo pathway in BxPC-3 and A549-CTGF cells by increasing phosphorylation of MST1/2, LATS1, and MOB1, reducing nuclear YAP localization, and decreasing total YAP and CTGF protein levels, without altering YAP/TAZ transcription[1].
YL-602 (1.25-20 μM; 12-14 days) potently inhibits colony formation in BxPC-3, MIA PaCa-2, SMMC-7721, MDA-MB-231, and 4T1 cancer cells in a dose-dependent manner, but does not inhibit HT-29 cell colony formation at ≤10 μM[1].
YL-602 (2.5-20 μM; 5 days) induces dose-dependent apoptosis in BxPC-3 and MDA-MB-231 cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BxPC-3 cells, A549-CTGF cells
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Concentration:0.62, 1.25, 2.5. 5, 10 μM
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Incubation Time:24 h
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Result:Reduced nuclear YAP levels in BxPC-3 cells in a dose-dependent manner without altering YAP/TAZ mRNA levels.
Dose-dependently increased phosphorylation of MST1/2 (Thr183/Thr180), LATS1 (Thr1079), and MOB1 (Thr35) in both BxPC-3 and A549-CTGF cells, while leaving total MST1, LATS1, and MOB1 protein levels unchanged.
Reduced total YAP and CTGF protein levels in BxPC-3 cells.
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Cell Line:BxPC-3, MIA PaCa-2, SMMC-7721, MDA-MB-231, 4T1, HT-29 cancer cells
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Concentration:1.25, 2.5. 5, 10, 20 μM
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Incubation Time:12-14 days
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Result:Dose-dependently inhibited colony formation in BxPC-3, MIA PaCa-2, SMMC-7721, MDA-MB-231, and 4T1 cells.
Achieved near-complete inhibition at 20 μM in BxPC-3 and SMMC-7721 cells.
Showed no significant inhibition in HT-29 cells at ≤10 μM.
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Cell Line:BxPC-3, MDA-MB-231 cancer cells
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Concentration:2.5. 5, 10, 20 μM
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Incubation Time:5 days
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Result:Induced early apoptosis in BxPC-3 cells in a dose-dependent manner and late apoptosis at 10-20 μM.
Induced apoptosis at 20 μM in MDA-MB-231 cells.
YL-602 (50 mg/kg; p.o.) significantly inhibits BXPC-3 pancreatic carcinoma tumor growth in nude mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c (female, 6 weeks old, 4T1 murine mammary carcinoma cells injected subcutaneously)[1]
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Dosage:25 mg/kg; 50 mg/kg; 100 mg/kg
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Administration:p.o.; daily; 21 days
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Result:Reduced tumor volume and tumor weight in a dose-dependent manner.
Significantly decreased mean tumor weight at 100 mg/kg relative to vehicle control.
Increased phosphorylation levels of MST1/2, LATS1, and MOB1 in tumor tissues compared to vehicle control.
Decreased YAP protein levels in tumor tissues compared to vehicle control.
Caused no significant body weight loss or histopathological changes in heart, liver, spleen, lung, or kidney.
Chemical Information
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CAS No. 3081701-84-7
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Molecular Weight 293.27
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Formula C17H11NO4
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SMILES
C12=C3OCOC3=CC=C1C=C(C4=CC5=C(OCO5)C=C4)N=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YL-602 Related Classifications
HY-186148 Related Classifications
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