2. Apoptosis MAPK/ERK Pathway
  3. RIP kinase Mixed Lineage Kinase Necroptosis
  4. RIPK1-IN-34

RIPK1-IN-34 是一种选择性、可穿透血脑屏障的 RIPK1 抑制剂 (IC50 = 126.70 nM)，对 RIPK3 几乎没有抑制作用 (IC50 ＞ 10, 000 nM)。RIPK1-IN-34 通过抑制坏死性凋亡 (necroptosis) 通路中 RIPK1、RIPK3 和混合谱系激酶结构域样假激酶 (MLKL) 的磷酸化，发挥显著的神经保护作用。RIPK1-IN-34 在大鼠大脑中动脉闭塞 (MCAO) 模型中显示出神经保护作用。RIPK1-IN-34 可用于急性缺血性卒中 (AIS) 的治疗研究。

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RIPK1-IN-34

RIPK1-IN-34 Chemical Structure

CAS No. : 3065634-19-4

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RIPK1-IN-34 相关抗体

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查看 RIP kinase 亚型特异性产品:

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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

RIPK1-IN-34 is a selective, brain-penetrant RIPK1 inhibitor (IC50 = 126.70 nM) with almost no inhibitory effect on RIPK3 (IC50 ＞ 10, 000 nM). RIPK1-IN-34 offers substantial neuroprotection by inhibiting the phosphorylation of RIPK1, RIPK3, and mixed lineage kinase domain-like pseudokinase (MLKL) within the necroptosis pathway. RIPK1-IN-34 shows the neuroprotective effect in a rat middle cerebral artery occlusion (MCAO) model. RIPK1-IN-34 can be used for the study of anti-acute ischemic stroke (AIS)[1].

IC50 & Target

RIPK1

126.7 nM (IC50)

体外研究
(In Vitro)

RIPK1-IN-34 (Compound 9b) 显著降低 HT-29 (EC50 = 71.61 nM) 和 HT-22 (EC50 = 38.45 nM) 细胞中 TNF-α (T)、Smac 模拟物 SM-164 (HY-15989) (S) 和 Z-VAD-FMK (HY-16658B) (Z) 诱导的细胞凋亡[1]。
RIPK1-IN-34 (0.78-400 nM，24 小时) 可有效拮抗 TSZ 诱导的 HT-29、U937、L929 和 HT-22 细胞的凋亡，使其接近未处理对照组的状态[1]。
RIPK1-IN-34 (1、10、100 nM，4.5 小时) 可有效保护 L929 细胞免于坏死性凋亡[1]。
RIPK1-IN-34 (0-1000 nM, 4.5 小时) 以剂量依赖的方式抑制 L929 细胞中 RIPK1、RIPK3 和 MLKL 的磷酸化[1]。

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

RIPK1-IN-34 相关抗体:

Apoptosis Analysis[1]

Cell Line: L929 cells
Concentration: 1 nM, 10 nM, 100 nM
Incubation Time: After pre-incubation with the compound for 30 minutes, cells were treated with TSZ for 4 hours
Result: Effectively protected the cells from necroptosis in L929 cells.

Western Blot Analysis[1]

Cell Line: L929 cells
Concentration: 0 nM, 10 nM, 100 nM, 1000 nM
Incubation Time: After pre-incubation with the compound for 30 minutes, cells were treated with TSZ for 4 hours
Result: Decreased the intensities of p-RIPK1 and p-RIPK3 bands in response to increasing concentrations.
Curtailed the enhancement of MLKL phosphorylation.
体内研究
(In Vivo)

RIPK1-IN-34 (Compound 9b) (0.5-4.5 mg/kg，静脉注射，两次) 剂量依赖性地改善 SD 大鼠的神经功能，减少脑梗死体积，并抑制炎症和氧化应激，证明其具有显著的神经保护作用[1]。
RIPK1-IN-34 (78.4-160 mg/kg，腹腔注射，两次腹腔注射，间隔一小时) 在 C57BL/6 小鼠中测试的剂量下不会引起急性毒性，其 LD50 超过 160 mg/kg，表明其具有很高的安全性[1]。

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

Animal Model: SPF grade male SD rats (180-200 g) were used to construct a middle cerebral occlusion model[1].
Dosage: 0.5 mg/kg, 1.5 mg/kg, 4.5 mg/kg
Administration: I.v., administered intravenously once 0.5 hours before modeling, and again after reperfusion, for a total of two administrations
Result: Significantly improved neurological outcomes 24 h post-operation, with reductions in scores exhibiting a dose-dependent trend: low dose (5.20), medium dose (5.09), and high dose (3.82).
Significantly reduced infarct volumes across all treatment groups in a dose-responsive manner: low dose (20.60), medium dose (18.32), and high dose (16.51).
Diminished MDA, TNF-α, and IL-1β levels while slightly increasing SOD levels.
Animal Model: SPF grade male C57BL/6 mice (aged 6-8 weeks, weighing 18-22 g)[1].
Dosage: 160 mg/kg, 112 mg/kg, 78.4 mg/kg
Administration: I.p., two intraperitoneal injections, one hour apart
Result: No abnormal behaviors or deaths were observed, and the body weight of mice in all groups steadily increased over 7 days with no significant differences.
分子量

491.54

Formula

C28H25N7O2
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

RIPK1-IN-34 相关分类

  • 摩尔计算器

  • 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:

RIPK1-IN-343065634-19-4RIP kinaseMixed Lineage KinaseNecroptosisReceptor-interacting protein kinasesRIPKMLKsRIPK1 inhibitorQuinazoline coreNeuroprotectantsAnti acute ischemic strokeInhibitorinhibitorinhibit

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