2. Epigenetics Immunology/Inflammation GPCR/G Protein Metabolic Enzyme/Protease
  3. Epigenetic Reader Domain CXCR MMP
  4. Snail IN-1

Snail IN-1 是一种口服有效的 Snail 抑制剂，其靶标 Ka 为 0.36 μM。Snail IN-1 可破坏 Snail-CBP 相互作用，通过降低乙酰化和增加多泛素化水平加速 Snail 蛋白降解，且不改变其他 EMT 转录因子。Snail IN-1 可减轻动脉粥样硬化斑块负荷、调控炎症及斑块稳定性相关因子、下调 CCL5、CXCL10、MMP2 和 MMP9，同时上调 α-平滑肌肌动蛋白。Snail IN-1 具有抗炎及斑块稳定活性，可用于动脉粥样硬化的研究。

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Snail IN-1

Snail IN-1 Chemical Structure

CAS No. : 3083216-69-4

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Snail IN-1 相关抗体

Top Publications Citing Use of Products

查看 CXCR 亚型特异性产品:

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CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

查看 MMP 亚型特异性产品:

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Snail IN-1 is an orally active Snail inhibitor with a Ka of 0.36 μM.Snail IN-1 disrupts Snail-CBP interaction, accelerates Snail protein degradation, reduces Snail acetylation, increases Snail polyubiquitination, and selectively downregulates Snail protein without altering other EMT transcription factors.Snail IN-1 reduces atherosclerotic plaque burden, modulates inflammation and plaque stability factors, downregulates CCL5, CXCL10, MMP2, and MMP9, and upregulates α-smooth muscle actin.Snail IN-1 exerts anti-inflammatory and plaque-stabilizing properties.Snail IN-1 can be used for the research of atherosclerosis[1].

IC50 & Target

CXCR2

 

MMP-9

 

MMP-10

 

Recombinant Snail Protein

0.36 μM (Ki)

体外研究
(In Vitro)

Snail IN-1 (compound S29) (0.1-10 μM; 48 h) 可在体外以浓度依赖的方式强效下调 HUVECs 中的 Snail 蛋白水平，且不改变 Snail 的 mRNA 水平，提示其调控作用发生在转录后阶段[1]。
Snail IN-1 (5-60 μM; 48 h) 在浓度高达 60 μM、孵育 48 h 后，对 HUVECs 无明显细胞毒性[1]。
Snail IN-1 (5 μM; 0-240 min) 可加速 HUVECs 中 Snail 蛋白的降解，降低其稳定性[1]。
Snail IN-1 (2.5-20 μM; 48 h) 可特异性下调 HUVEC 中的 Snail 蛋白水平，而不影响其他 EMT 转录因子 (Zeb1、Slug、Twist) 的蛋白或 mRNA 水平[1]。
Snail IN-1 (5 μM; 24 h) 通过破坏 Snail 与 CBP 的相互作用、降低 Snail 乙酰化水平并增加人脐静脉内皮细胞 (HUVECs) 中 Snail 的多聚泛素化来促进 Snail 降解[1]。
Snail IN-1 (2.5 μM; 24 h) 可显著下调 TNF-α 刺激的 HUVECs 中促动脉粥样硬化因子 (CCL5、CXCL10、MMP-9、MMP-2) 的 mRNA 水平[1]。
Snail IN-1 (1.25-5 μM; 24 h) 以浓度依赖的方式抑制 TNF-α 刺激的 HUVEC 中 CCL5 和 CXCL10 蛋白的表达[1]。
Snail IN-1 (2.5 μM; 24 h) 可通过改变经 TNF-α 刺激的 HUVEC 的分泌谱来损伤单核细胞的募集[1]。

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

Snail IN-1 相关抗体:

Western Blot Analysis[1]

Cell Line: human umbilical vein endothelial cells (HUVECs)
Concentration: 0.1, 1.25, 2.5, 5, 10 μM
Incubation Time: 48 h
Result: Reduced Snail protein levels (normalized to β-actin) to 0.27 relative to vehicle control at 10 μM.
Significantly reduced Snail protein levels at 0.1, 1.25, 2.5, and 5 μM.
Showed no significant changes in Snail mRNA levels across all tested concentrations.

Cell Cytotoxicity Assay[1]

Cell Line: human umbilical vein endothelial cells (HUVECs)
Concentration: 5, 10, 20, 40, 60 μM
Incubation Time: 48 h
Result: Showed no significant reduction in HUVEC viability, with cell viability remaining above 90% relative to vehicle control across all tested concentrations.

Western Blot Analysis[1]

Cell Line: human umbilical vein endothelial cells (HUVECs)
Concentration: 5 μM; with cycloheximid (CHX)
Incubation Time: 0, 30, 60, 120, 240 min
Result: Increased the degradation rate of Snail protein compared to vehicle-treated cells.
Lowered relative Snail protein levels at all time points after CHX addition, with a more pronounced decrease over time.

Western Blot Analysis[1]

Cell Line: human umbilical vein endothelial cells (HUVECs)
Concentration: 5 μM; 2.5, 5, 10, 20 μM
Incubation Time: 48 h
Result: Potently reduced Snail protein levels at 5 μM, but had no appreciable effect on the abundance of Zeb1, Slug, or Twist protein.
Showed no significant changes in mRNA levels of Zeb1, Slug, Twist, or Snail across tested concentrations.

Cell Migration Assay[1]

Cell Line: TNF-α-stimulated human umbilical vein endothelial cells (HUVECs); THP-1 monocytes
Concentration: 2.5 μM
Incubation Time: 24 h
Result: Resulted in a significant reduction in THP-1 monocyte migration when using conditioned medium from Snail IN-1-treated HUVECs compared to medium from control cells.
体内研究
(In Vivo)

Snail IN-1 (25-50 mg/kg; 灌胃; 每日; 4 周) 在高脂饮食喂养的 ApoE-/- 小鼠中发挥剂量依赖性抗动脉粥样硬化作用，通过降低炎性趋化因子 (CCL5、CXCL10) 和基质降解酶 (MMP2、MMP9) 减少斑块负荷，同时增加斑块稳定因子 (胶原蛋白、α-SMA)[1]。
Snail IN-1 (2000 mg/kg; 灌胃; 单剂量) 对 C57BL/6 小鼠具有良好的耐受性，不会造成急性器官损伤或功能紊乱[1]。

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

Animal Model: ApoE-/- mice (high-fat diet-induced atherosclerotic model; treated for 4 weeks post-modeling)[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: i.g.; daily; 4 weeks
Result: Reduced aortic plaque area to 11.33% at 25 mg/kg and a lower unspecified value at 50 mg/kg relative to control.
Reduced intraplaque CCL5 area to ~2% (from control ~15%) and CXCL10 area to ~1.5% (from control ~5%) at 50 mg/kg.
Increased collagen area in plaques to ~45% (from control ~40%) and α-SMA area to ~10% (from control ~3%) at 50 mg/kg.
Reduced intraplaque MMP2 area by 64.2% and MMP9 area by 60% relative to control at 50 mg/kg.
Animal Model: C57BL/6 mice[1]
Dosage: 2000 mg/kg
Administration: i.g.; single dose
Result: Showed no adverse effects, changes in body weight, or organ weight abnormalities.
Exhibited normal tissue architecture with no pathological alterations in heart, liver, spleen, lung, kidney, and brain via histopathological analysis.
Demonstrated serum levels of hepatic injury markers (ALT, AST), renal function markers (BUN, Scr), and metabolic indicators (Glu, LAC) comparable to vehicle control with no statistically significant differences.
分子量

409.50

Formula

C21H23N5O2S
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

Snail IN-1 相关分类

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  • 稀释计算器

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  • 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:

Snail IN-13083216-69-4Snail IN1Snail IN 1Epigenetic Reader DomainCXCRMMPCXC chemokine receptorsC-X-C motif chemokine receptorsMatrix metalloproteinasesCBPα-smooth muscle actinMMP9MMP2atherosclerosisSnailCXCL10HUVECsEMT transcription factorsCCL5Inhibitorinhibitorinhibit

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