2. Protein Tyrosine Kinase/RTK Stem Cell/Wnt TGF-beta/Smad NF-κB Apoptosis Neuronal Signaling
  3. DYRK TGF-beta/Smad NF-κB Wnt β-catenin MDM-2/p53 Notch
  4. XRF-1021

XRF-1021 是一种口服有效的 HIPK2 抑制剂 (IC50 = 0.18 μM)。XRF-1021 可降低 TGF-β1 刺激的 NRK-49F 和 HK-2 细胞中纤维化标志物的表达，包括纤连蛋白、I 型胶原蛋白和 α-SMA。XRF-1021 可阻断 TGF-β, NF-κB, p53, Wnt/β-catenin 和 Notch 信号通路。XRF-1021 可减轻体内肾损伤和纤维化。XRF-1021 可用于慢性肾脏病的研究。

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XRF-1021

XRF-1021 Chemical Structure

CAS No. : 2968523-32-0

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XRF-1021 相关抗体

Top Publications Citing Use of Products

查看 DYRK 亚型特异性产品:

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DYRK1 DYRK2 DYRK3 DYRK4 HIPK PRP4

查看 NF-κB 亚型特异性产品:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

查看 Wnt 亚型特异性产品:

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Wnt1 Wnt3 Wnt5 Wnt7

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

XRF-1021 is an orally active HIPK2 inhibitor (IC50 = 0.18 μM). XRF-1021 reduces the expression of fibrotic markers in TGF-β1 stimulated NRK-49F and HK-2 cells, including Fibronectin, Collagen I and α-SMA. XRF-1021 blocks TGF-β, NF-κB, p53, Wnt/β-catenin, and Notch signaling. XRF-1021 reduces renal injury and fibrosis in vivo. XRF-1021 can be used for the research of chronic kidney disease[1].

IC50 & Target[1]

HIPK2

0.18 μM (IC50)

NF-κB

 

体外研究
(In Vitro)

XRF-1021 (3-100 μM, 48 h) 可抑制 TGF-β1 刺激的 NRK-49F 细胞增殖，IC50 值为 4.87 μM，表明其可能调节 HIPK2 介导的信号通路[1]。
XRF-1021 (100 μM, 24 h) 可直接与 HIPK2 结合，并表现出较高的结合稳定性 (RMSD 约为 0.1 Å，RMSF < 0.1 Å)[1]。
XRF-1021 (2.5-80 μM, 24 h) 在浓度为 2.5, 5 和 10 μM 时，对 HK-2 细胞的增殖或活力没有显著影响[1]。
XRF-1021 (2.5-10 μM, 24 h) 可抑制 HIPK2 及其下游信号通路，从而减轻 HK-2 细胞的纤维化[1]。
XRF-1021 (2.5-10 μM, 24 h) 可降低 NRK-49F 细胞中 HIPK2, FN 和 α-SMA 蛋白的表达[1]。

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

XRF-1021 相关抗体:

Western Blot Analysis[1]

Cell Line: TGF-β1-stimulated HK-2 cells
Concentration: 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Reduced the expression levels of these fibrotic markers, including FN, α-SMA, and HIPK2 protein expression in HK-2 cells dose-dependently.
Exhibited the most pronounced inhibitory effect at 10 μmol/L.

Western Blot Analysis[1]

Cell Line: TGF-β1-stimulated HK-2 cells
Concentration: 0, 10 μM
Incubation Time: 24 h
Result: Significantly attenuated the phosphorylation levels of both proteins, indicating effective suppression of the TGF-β and NF-κB pathways.
Effectively reversed these TGF-β1-induced increases, including Wnt/β-catenin pathway target genes (PAI-1, Axin2, and MMP7) and Notch pathway target genes (Hes1, Hey1, and Hey2).
体内研究
(In Vivo)

XRF-1021 (25-75 mg/kg, 口服) 通过抑制 HIPK2 及其下游通路，如 TGF-β, NF-κB, p53, Wnt/β-catenin和 Notch 通路，来抑制纤维化标志物的表达，从而减轻 Sprague-Dawley (SD) 大鼠 UUO 模型中的肾纤维化进展[1]。
XRF-1021 (25-100 mg/kg, 口服) 通过抑制 HIPK2 及其下游多个促纤维化信号通路，包括 TGF-β, NF-κB, p53, Wnt/β-catenin 和 Notch 通路，来减轻 C57BL/6J 小鼠腺嘌呤饮食模型中的肾小管损伤，减少间质纤维化并改善肾功能[1]。

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

Animal Model: Sprague-Dawley (SD) rats[1]
Dosage: 25, 50 and 75 mg/kg
Administration: oral administration (p.o.)
Result: Partially ameliorated these pathological changes in a dose-dependent manner, with the 75 mg/kg dose showing greater efficacy.
Relieved renal injury and renal fibrosis and diminished the expression levels of related renal fibrosis indicators.
Suppressed the protein expression of fibrotic markers (FN, Collagen I, α-SMA, Vimentin) and HIPK2.
Inhibited HIPK2-regulated p53 pathway, TGF-β/Smad3, NF-κB, Wnt/β-catenin and Notch pathways.
Animal Model: Male C57BL/6J mice (seven weeks)[1]
Dosage: 25, 50 and 100 mg/kg
Administration: oral administration (p.o.)
Result: Mitigated renal lesions and interstitial fibrosis in a dose-dependent manner, with the 100 mg/kg dose showing the most pronounced effect.
Reduced serum creatinine, blood urea nitrogen, and uric acid levels dose-dependently.
Downregulated the expression of HIPK2, collagen I, α-SMA, and vimentin in the kidneys of adenine-fed mice.
Reduced phosphorylation levels of Smad3, NF-κB and p53.
分子量

404.44

Formula

C21H21FN8
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

XRF-1021 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:

XRF-10212968523-32-0XRF1021XRF 1021DYRKTGF-beta/SmadNF-κBWntβ-cateninMDM-2/p53NotchDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseTransforming growth factor betaNuclear factor-κBNuclear factor-kappaBBeta cateninRenal fibrosisHIPK2Anti-fibrotic therapychronic kidney diseaseTGF-β1p53Wnt/β-cateninInhibitorinhibitorinhibit

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