2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. XW-17

XW-17 是一种 PARP14 抑制剂，其 IC50 为 3.03 nM，对其他 PARP 家族成员具有选择性。XW-17 可抑制 PARP14 介导的单 ADP 核糖基化，结合并稳定内源性 PARP14 蛋白。XW-17 可减轻特应性皮炎样小鼠模型的皮肤损伤，并降低 IL-4、IL-13、IgE 和 IL-17A 的表达。XW-17 可用于特应性皮炎的研究。

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XW-17

XW-17 Chemical Structure

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XW-17 相关抗体

Top Publications Citing Use of Products

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

XW-17 is a PARP14 inhibitor with an IC50 of 3.03 nM and selectivity over other PARP family members.XW-17 suppresses PARP14-mediated mono-ADP-ribosylation, engages and stabilizes endogenous PARP14 protein.XW-17 attenuates skin lesions and decreases expression of IL-4, IL-13, IgE, and IL-17A in an atopic dermatitis-like mouse model.XW-17 can be used for the research of atopic dermatitis[1].

IC50 & Target

PARP14

 

体外研究
(In Vitro)

XW-17 (孵育 1 小时) 可强效且选择性地抑制纯化的 PARP14 酶活性，其 IC50 为 3.03 nM，对 PARP1 的选择性指数超过 9900[1]。
XW-17 在大鼠血浆、小鼠肝微粒体、大鼠肝微粒体和人肝微粒体中均表现出优异的代谢稳定性，所有受试体系中的 T1/2 值均大于 240 min[1]。
XW-17 (5 μM; 2 h) 在 MDCK 和 Caco-2 细胞模型中表现出良好的膜通透性和低外排性，其 Papp A→B 值分别为 16.32 × 10-6 cm/s 和 20.49 × 10-6 cm/s[1]。
XW-17 (0.001-3 μM; unspecified duration) 可结合并稳定 IFN-γ 刺激的 CFPAC-1 细胞中的内源性 PARP14，其 EC50 为 59.5 nM[1]。
XW-17 (0.01-1 μM; 6 h pretreatment, 24 h IFN-γ stimulation) 可在 IFN-γ 刺激的 CFPAC-1 和 RAW264.7 细胞中以浓度依赖的方式强效抑制 PARP14 介导的 MARylation[1]。
XW-17 (up to at least 30 μM; 72 h) 对 MCF-10A 和 AML-12 细胞无显著细胞毒性，其 IC50 值大于 30 μM[1]。
XW-17 (5-30 μM) 具有较低的 hERG 钾通道抑制活性，在 5 μM 时抑制率为 3.15%，在 30 μM 时抑制率为 5.56%，提示其心脏毒性风险较低[1]。

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

XW-17 相关抗体:

Western Blot Analysis[1]

Cell Line: CFPAC-1 cells
Concentration: 0.001-3 μM
Incubation Time: unspecified duration (IFN-γ stimulation)
Result: Induced a concentration-dependent upregulation of PARP14 protein expression, confirming target binding and stabilization, with an EC50 of 59.5 nM.

Western Blot Analysis[1]

Cell Line: CFPAC-1 cells, RAW264.7 cells
Concentration: 0.01-1 μM
Incubation Time: 6 h pretreatment; 24 h IFN-γ stimulation
Result: Reduced intracellular MARylation signals in a concentration-dependent manner in both cell lines, indicating inhibition of endogenous PARP14 catalytic activity.

Cell Cytotoxicity Assay[1]

Cell Line: MCF-10A human mammary epithelial cells, AML-12 mouse hepatocytes
Concentration: up to at least 30 μM
Incubation Time: 72 h
Result: Did not exhibit significant cytotoxicity, with IC50 values exceeding 30 μM in both cell lines.
体内研究
(In Vivo)

XW-17 (腹腔注射，25-100 mg/kg，每日 2 次，持续 11 天) 可剂量依赖性地改善 DNCB 诱导的雄性 BALB/c 小鼠特应性皮炎，其中 100 mg/kg 腹腔注射、每日 2 次的剂量对皮炎评分、组织病理学损伤及 Th2/Th17 相关炎症介质的降低效果最为显著，优于阳性对照药物 RBN-3143 和 Upadacitinib[1]。

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

Animal Model: BALB/c (male, 18−22 g, DNCB-induced atopic dermatitis)[1]
Dosage: 25 mg/kg; 50 mg/kg; 100 mg/kg
Administration: i.p.; twice daily; 11 days
Result: Significantly reduced dermatitis score compared to model group at 25 mg/kg (P < 0.05), 50 mg/kg (P < 0.01), and 100 mg/kg (P < 0.001).
Achieved lower dermatitis score than positive controls RBN-3143 and Upadacitinib at 100 mg/kg.
Dose-dependently reduced histopathological abnormalities in dorsal skin, with 100 mg/kg dose achieving lowest histological score and outperforming Upadacitinib.
Significantly reduced protein levels of IL-4, IL-13, IL-17A in skin homogenates and serum IgE at 50 mg/kg and 100 mg/kg, with most pronounced inhibition at 100 mg/kg.
Dose-dependently suppressed mRNA levels of IL-31, TSLP, and GATA3 in dorsal skin.
Showed no significant effect on Th1 pathway-related cytokines (TNF-α, IL-6, IL-1β) at any dose.
Caused no significant body weight loss or histological abnormalities in major organs (heart, liver, spleen, lung, kidney).
分子量

452.55

Formula

C24H32N6O3
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

XW-17 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:

XW-17XW17XW 17PARPpoly ADP ribose polymerasemono-ADP-ribosylationIL-17AIL-13atopic dermatitisCaco-2IL-4CFPAC-1PARP14MDCKIgEInhibitorinhibitorinhibit

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