2. Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB MAPK/ERK Pathway
  3. Ferroptosis Necroptosis RIP kinase Reactive Oxygen Species (ROS) Mixed Lineage Kinase
  4. Zharp1-163

Zharp1-163 是铁死亡 (ferroptosis) 和坏死性凋亡 (necroptosis) 的双重抑制剂。Zharp1-163 通过降低活性氧 (ROS) 水平有效阻断铁死亡，并通过强效且选择性地靶向 RIPK1 激酶活性来抑制坏死性凋亡(KD = 240 nM; IC50 = 406.1 nM)。Zharp1-163 抑制坏死性凋亡刺激引起的 RIPK1、RIPK3 和 MLKL 的细胞活化。Zharp1-163 显著减轻 TNF-α (HY-P1875) 诱导的全身炎症综合征，包括预防 TNF-α 诱导的小鼠死亡和体温过低。Zharp1-163 显著减轻 Cisplatin (HY-17394) 和缺血再灌注诱导的模型中与坏死性凋亡和铁死亡相关的急性肾损伤。Zharp1-163 可用于研究与细胞死亡通路相关的疾病，例如肾脏疾病。

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Zharp1-163

Zharp1-163 Chemical Structure

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Zharp1-163 相关抗体

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RIPK1 RIPK2 RIPK3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Zharp1-163 is a dual inhibitor of ferroptosis and necroptosis. Zharp1-163 effectively blocks ferroptosis by reducing reactive oxygen species (ROS) levels and inhibits necroptosis by potently and selectively targeting RIPK1 kinase activity (KD = 240 nM; IC50 = 406.1 nM). Zharp1-163 inhibits the cellular activation of RIPK1, RIPK3 and MLKL in response to necroptotic stimulation. Zharp1-163 markedly attenuates TNF-α (HY-P1875)-induced systemic inflammatory syndrome, including the prevention of TNF-α-induced mortality and hypothermia in mice. Zharp1-163 significantly alleviates acute kidney injury associated with both necroptosis and ferroptosis in models induced by Cisplatin (HY-17394) and ischemia-reperfusion. Zharp1-163 can be used for the study of diseases associated with cell death pathways, such as kidney disease[1].

IC50 & Target

RIPK1

240 nM (Kd)

RIPK1

406.1 nM (IC50)

RIPK3

 

体外研究
(In Vitro)

Zharp1-163 (0.01-10 μM，18 小时) 显著抑制 Erastin (HY-15763) 或 RSL3 (HY-100218A) 诱导的 HT-1080 细胞 (EC50 = 0.95 μM；EC50 = 1.33 μM) 和小鼠胚胎成纤维细胞 (MEF) (EC50 = 1.93 μM；EC50 = 1.39 μM) 中的铁死亡[1]。
Zharp1-163 (0.01-10 μM，14-18 小时) 阻断 TNF-α、Smac 模拟物和 Z-VAD (HY-164388) 诱导的 HT-29 细胞 (EC50 = 0.1 μM) 和 MEF (EC50 = 0.11 μM) 中的坏死性凋亡[1]。
Zharp1-163 (0.01-10 μM，14 小时) 能有效抑制小鼠成纤维细胞 L929 中 TNFα 和 Z-VAD 诱导的坏死性凋亡[1]。
Zharp1-163 (0.3-3 μM，26 小时) 能抑制 TNFα 联合 Smac 模拟物诱导的 MEF 细胞凋亡[1]。
Zharp1-163 (0.3-3 μM，8 小时) 对 THP-1 细胞的细胞焦亡无影响[1]。
Zharp1-163 (10 μM，7 小时) 能显著降低铁死亡过程中脂质 ROS 的产生，并降低 RSL3 诱导的 HT-1080 细胞中 CHAC1 和 PTGS2 的表达[1]。
Zharp1-163 (0.1-3 μM，10 小时) 可消除人 HT-29 细胞中 RIPK1、RIPK3 和 MLKL 的磷酸化，并阻断 MEF 细胞中 RIPK1、RIPK3 和 MLKL 的磷酸化[1]。
Zharp1-163 (0.3-3 μM，10 小时) 可抑制 HT-29 细胞中 RIPK3 斑点的形成和 MLKL 的寡聚化[1]。

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

Zharp1-163 相关抗体:

Cell Viability Assay[1]

Cell Line: HT-1080 cells and MEFs.
Concentration: 0.01 μM, 0.1 μM, 1 μM, 10 μM
Incubation Time: Pretreated 2 h and then treated with Erastin or RSL3 for 16 h
Result: Significantly inhibited Erastin- or RSL3-induced ferroptosis in HT-1080 cells and MEFs.

Cell Viability Assay[1]

Cell Line: HT-1080 cells and MEFs.
Concentration: 0.01 μM, 0.1 μM, 1 μM
Incubation Time: Pretreated 2 h, followed by treatment with TNF-α (T) (40 ng/mL), Smac mimetic (S) (100 nM), Z-VAD (Z) (20 μM) for 12-16 h
Result: Blocked TNF-α, Smac mimetic, and Z-VAD-induced necroptosis in HT-29 cells (EC50 = 0.1 μM), in MEFs (EC50 = 0.11 μM).

Cell Viability Assay[1]

Cell Line: Mouse fibroblast L929 cells
Concentration: 0.01 μM, 0.1 μM, 1 μM
Incubation Time: 2 h, followed by treatment with T (40 ng/mL) and Z (20 μM) for 12 h
Result: Blocked TNF-α, Z-VAD-induced necroptosis in mouse fibroblast L929 cells (EC50 = 0.08 μM).

Apoptosis Analysis[1]

Cell Line: MEFs
Concentration: 0.3 μM, 1 μM, 3 μM
Incubation Time: 2 h before treatment with T (40 ng/mL) and S (100 nM) for 24 h
Result: Inhibited apoptosis induced by TNFα plus Smac mimetic in MEFs.

Real Time qPCR[1]

Cell Line: HT-1080 cells
Concentration: 10 μM
Incubation Time: 2 h, followed by induction with RSL3 for 5 h
Result: Significantly reduced the induction of both CHAC1 and PTGS2 in response to RSL3.

Western Blot Analysis[1]

Cell Line: HT-29 cells, MEFs
Concentration: 0.1 μM, 0.3 μM, 1 μM, 3 μM
Incubation Time: 2 h, followed by treatment with T (40 ng/mL), S (100 nM) and Z (20 μM) for 8 h
Result: Eliminated the phosphorylation of RIPK1, RIPK3, and MLKL in human HT-29 cells.
Blocked the phosphorylation of RIPK1, RIPK3, and MLKL in MEFs.

Immunofluorescence[1]

Cell Line: HT-29 cells stably expressing Flag-tagged RIPK3
Concentration: 0.3 μM, 1 μM, 3 μM
Incubation Time: Before the addition of T (40 ng/mL), S (100 nM), and Z (20 μM) for an additional 8 h, HT-29 cells stably expressing Flag-tagged RIPK3 were preincubated with the specified compounds for 2 h
Result: Prevented the generation of RIPK3 puncta.
体内研究
(In Vivo)

Zharp1-163 (5 mg/kg，腹腔注射，一次) 是一种有有效的 RIPK1 抑制剂，可显著保护 C57BL/6 小鼠免受 TNF 诱导的 SIRS 的影响[1]。
Zharp1-163 (5 mg/kg，腹腔注射，一次) 显著减轻了 C57BL/6 小鼠中 Cisplatin 和缺血再灌注诱发的模型中与坏死性凋亡和铁死亡相关的急性肾损伤[1]。

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

Animal Model: C57BL/6 mice injected TNF[1].
Dosage: 5 mg/kg
Administration: I.p., pretreated with 30 min prior to challenge
Result: Significantly protected mice from TNF-α-induced lethality and reduced TNF-α-induced temperature loss in these mice.
Significantly ameliorated the production of proinflammatory cytokines, including IL-6.
Induced damage to the cecum and colon.
Animal Model: Cisplatin-induced acute kidney injury in C57BL/6 mice[1].
Dosage: 5 mg/kg
Administration: I.p., pretreated with 30 min prior to challenge
Result: Significantly inhibited cisplatin-induced body weight loss.
Mitigated mild inflammation and tubular epithelial cell damage.
Decreased the serum creatinine and blood urea nitrogen (BUN) levels in the context of Cisplatin-induced kidney injury.
Animal Model: The left renal artery of C57BL/6 mice pretreated for 2 h was isolated and clamped for 45 min via a nontraumatic artery clamp following right nephrectomy. Reperfusion was subsequently performed[1].
Dosage: 5 mg/kg
Administration: I.p., 2 h
Result: Significantly inhibited the levels of creatinine and BUN in mouse serum.
分子量

393.44

Formula

C21H23N5O3
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

Zharp1-163 相关分类

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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:

Zharp1-163FerroptosisNecroptosisRIP kinaseReactive Oxygen Species (ROS)Mixed Lineage KinaseReceptor-interacting protein kinasesRIPKMLKsDual inhibitorRIPK1 kinaseInhibitorinhibitorinhibit

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