2. Stem Cell/Wnt Apoptosis
  3. Hippo (MST) YAP Apoptosis
  4. 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.

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YL-602

YL-602 Chemical Structure

CAS No. : 3081701-84-7

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YL-602 Related Antibodies

Top Publications Citing Use of Products

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MST1 MST2 MST3 MST4

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YAP/TAZ YAP/TAZ-TEAD TEAD YAP1

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Description

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[1].

IC50 & Target[1]

MST1

 

MST2

 

In Vitro

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.

YL-602 Related Antibodies

Western Blot Analysis[1]

Cell Line: BxPC-3 cells, A549-CTGF cells
Concentration: 0.62, 1.25, 2.5. 5, 10 μM
Incubation Time: 24 h
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.

Cell Proliferation Assay[1]

Cell Line: BxPC-3, MIA PaCa-2, SMMC-7721, MDA-MB-231, 4T1, HT-29 cancer cells
Concentration: 1.25, 2.5. 5, 10, 20 μM
Incubation Time: 12-14 days
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.

Apoptosis Analysis[1]

Cell Line: BxPC-3, MDA-MB-231 cancer cells
Concentration: 2.5. 5, 10, 20 μM
Incubation Time: 5 days
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.
In Vivo

YL-602 (25-100 mg/kg; p.o.; daily; 21 days) significantly inhibits 4T1 mammary carcinoma tumor growth in Balb/c mice by activating the Hippo pathway[1].
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.

Animal Model: Balb/c (female, 6 weeks old, 4T1 murine mammary carcinoma cells injected subcutaneously)[1]
Dosage: 25 mg/kg; 50 mg/kg; 100 mg/kg
Administration: p.o.; daily; 21 days
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.
Molecular Weight

293.27

Formula

C17H11NO4
CAS No.
SMILES

C12=C3OCOC3=CC=C1C=C(C4=CC5=C(OCO5)C=C4)N=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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YL-602 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

YL-6023081701-84-7YL602YL 602Hippo (MST)YAPApoptosisYes-associated proteinCTGFBxPC-3 cellsTAZbreast cancerHippo pathwayA549-CTGF cellspancreatic cancerliver cancerMST1/2Inhibitorinhibitorinhibit

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