2. JAK/STAT Signaling Stem Cell/Wnt Apoptosis
  3. STAT Apoptosis
  4. YZ-35

YZ-35 是一种 STAT3 抑制剂，其 Ki 值为 0.38 μM。YZ-35 以高亲和力直接结合 STAT3，其解离常数 (Kd) 为190 nM。YZ-35能直接抑制 STAT3 的双重磷酸化 (Tyr705 和 Ser727 位点)。YZ-35 可抑制乳腺癌细胞系的菌落形成、细胞迁移，并诱导细胞凋亡 (apoptosis)。YZ-35 选择性地抑制乳腺癌干细胞 (BCSC) 的自我更新能力。YZ-35 在乳腺癌干细胞异种移植模型中抑制肿瘤生长。YZ-35 可用于乳腺癌研究。

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YZ-35

YZ-35 Chemical Structure

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YZ-35 相关抗体

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STAT3 STAT5 STAT6 STAT1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

YZ-35 is a STAT3 inhibitor, with a Ki value of 0.38 μM. YZ-35 binds directly to STAT3 with high affinity, exhibiting a dissociation constant (Kd) of 190 nM. YZ-35 directly attenuates the dual phosphorylation of STAT3 (Tyr705 and Ser727). YZ-35 suppresses colony formation, cellular migration, and induces apoptosis in breast cancer cell lines (BCSC). YZ-35 selectively suppresses BCSC self-renewal. YZ-35 inhibits tumor growth in the BCSC xenograft models. YZ-35 can be used for the study of breast cancer[1].

体外研究
(In Vitro)

YZ-35 (0.1-100 μM, 48 h) 对 MDA-MB-231 细胞 (IC50 = 0.63 μM), MCF-7 细胞 (IC50 = 0.32 μM) 和 MCF-10A 细胞 (IC50 = 34.34 μM) 显示出抑制效力[1]。
YZ-35 (0-4 μM, 0-48 h) 通过直接减弱 STAT3 的双重磷酸化 (Tyr705 和 Ser727)，在 MDA-MB-231 和 MCF-7 细胞中表现出强效的抗乳腺癌功效[1]。
YZ-35 (0-6 μM, 24-48 h) 抑制 MDA-MB-231 和 MCF-7 细胞的集落形成、细胞迁移并诱导细胞凋亡[1]。
YZ-35 (2.5-10 μM, 48 h) 降低 MDA-MB-231 和 MCF-7 细胞的肿瘤干性[1]。

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

YZ-35 相关抗体:

Cell Viability Assay[1]

Cell Line: MDA-MB-231 cells, MCF-7 cells and MCF-10A cells
Concentration: 0.1-100 μM
Incubation Time: 48 h
Result: Demonstrated inhibitory potency against MDA-MB-231 cells (IC50 = 0.63 μM), MCF-7 cells (IC50 = 0.32 μM) and MCF-10A cells (IC50 = 34.34 μM).

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells and MCF-7 cells
Concentration: 0, 1, 2, 3, 4 μM
Incubation Time: 0, 12, 24, 36, 48 h
Result: Exhibited concentration- and time-dependent suppression of the phosphorylation of STAT3 at both Tyr705 and Ser727 residues in MDA-MB-231 and MCF-7 cell lines, while maintaining total STAT3 protein levels.
Showed no effect on the expression levels of STAT1 and STAT5 or their phosphorylation.
Did not impact the phosphorylation of JAK2, Src, and ERK.
inhibited the expression of critical apoptosis-related proteins, including Cyclin D1, BCL2, BCL-xL, and Survivin, in a concentration-dependent manner.

Cell Migration Assay [1]

Cell Line: MDA-MB-231 cells and MCF-7 cells
Concentration: 0, 1, 2, 3 μM
Incubation Time: 24 h
Result: Decreased the migration of MDA-MB-231 cells by 99%.
Reduced the migration in MCF-7 cells by 72.97%.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells and MCF-7 cells
Concentration: 0, 1, 2, 4, 6 μM
Incubation Time: 48 h
Result: Induced programmed cell apoptosis in a concentration-dependent manner, with differential responses observed between BRCA subtypes: predominantly late-stage apoptosis in MDA-MB-231 cells, while promoting both earlyand late-phase apoptotic events in MCF-7 cells.

Immunofluorescence[1]

Cell Line: MDA-MB-231 cells and MCF-7 cells
Concentration: 0, 1, 2, 3 μM
Incubation Time: 48 h
Result: Induced programmed cell death of BRCA, notably manifesting as pronounced chromatin condensation and nuclear fragmentation, with the most substantial apoptotic phenotype observed at 3 μM concentration.
体内研究
(In Vivo)

YZ-35 (5-10 mg/kg，静脉给药，每日一次，持续 21 天) 抑制 BCSC 异种移植模型中的肿瘤生长[1]。

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

Animal Model: 1 × 107 MDA-MB-21 cells were resuspended with 100 μL saline and injected into the left flank of 5-week-old female BALB/c-nude mice[1]
Dosage: 5, 10 mg/kg
Administration: i.v. once daily for 21 days
Result: Inhibited tumor growth (the TGI of high (10 mg/kg) and low (5 mg/kg) groups were 89.98 and 74.13%, respectively).
Inhibited STAT3 phosphorylation and significantly reduced FOXM1 and AURKA expression.
Augmented the proportion of apoptotic cells while concurrently diminishing Ki67-positive proliferating cell populations in tumor tissues relative to vehicle controls.
Showed no significant toxicity was observed in major organs including the heart, liver, spleen, lung, and kidney.
分子量

512.58

Formula

C29H24N2O5S
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

YZ-35 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:

YZ-35YZ35YZ 35STATApoptosisSTAT3MDA-MB-231 cellsMCF-7 cellsMCF-10A cellsbreast cancerInhibitorinhibitorinhibit

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