2. Stem Cell/Wnt Apoptosis
  3. Hippo (MST) YAP Apoptosis
  4. YL-602

YL-602 是一种具有口服活性的 Hippo 通路激活剂。YL-602 通过 MST1/2 激活 Hippo 通路，并引发下游通路激活。YL-602 可抑制细胞中 YAP 和 CTGF 的表达，且该作用不受细胞密度和血清存在与否的影响。YL-602 可诱导肿瘤细胞凋亡 (apoptosis) 并抑制集落形成。YL-602 可抑制小鼠体内的肿瘤生长。YL-602 可用于癌症相关研究，例如乳腺癌。

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YL-602

YL-602 Chemical Structure

CAS No. : 3081701-84-7

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YL-602 相关抗体

Top Publications Citing Use of Products

查看 Hippo (MST) 亚型特异性产品:

查看所有亚型
MST1 MST2 MST3 MST4

查看 YAP 亚型特异性产品:

查看所有亚型
YAP/TAZ YAP/TAZ-TEAD TEAD YAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

YL-602 (0.01-100 μM; 24 h) 可强效抑制 A549-CTGF 细胞中 CTGF 启动子的活性，其 EC50 为 0.474 μM[1]。
YL-602 (0.62-10 μM; 24 h) 可通过提高 MST1/2、LATS1 和 MOB1 的磷酸化水平、减少 YAP 的核定位并降低总 YAP 和 CTGF 蛋白水平，激活 BxPC-3 和 A549-CTGF 细胞中的 Hippo 通路，且不改变 YAP/TAZ 的转录水平[1]。
YL-602 (1.25-20 μM; 12-14 days) 可强效且呈剂量依赖性地抑制 BxPC-3、MIA PaCa-2、SMMC-7721、MDA-MB-231 和 4T1 癌细胞的集落形成，但 ≤10 μM 时对 HT-29 细胞的集落形成无抑制作用[1]。
YL-602 (2.5-20 μM; 5 days) 可在 BxPC-3 和 MDA-MB-231 癌细胞中诱导剂量依赖性凋亡[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

YL-602 相关抗体:

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.
体内研究
(In Vivo)

YL-602 (25-100 mg/kg；口服；每日一次；连续 21 天) 可通过激活 Hippo 通路显著抑制 Balb/c 小鼠体内 4T1 乳腺癌的肿瘤生长[1]。
YL-602 (50 mg/kg；口服) 可显著抑制裸鼠体内 BXPC-3 胰腺癌肿瘤的生长[1]。

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.
分子量

293.27

Formula

C17H11NO4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

YL-602 相关分类

  • 摩尔计算器

  • 稀释计算器

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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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