2. Apoptosis NF-κB MAPK/ERK Pathway Immunology/Inflammation
  3. RIP kinase NF-κB p38 MAPK Interleukin Related
  4. RIPK2-IN-8

RIPK2-IN-8 是具有口服活性的高选择性的 RIPK2 抑制剂 (IC50 = 11 nM)。RIPK2-IN-8 对 RIPK2 的选择性高于 RIPK1 (IC50 > 30,000 nM)，对 RIPK3 有中度抑制作用 (IC50= 44.61 nM)。RIPK2-IN-8 通过抑制 NOD2-RIPK2 信号通路和炎症因子 IL-6 和 TNFα 的表达，发挥抗炎作用。RIPK2-IN-8 在急性肝损伤 (ALI) 模型中显示出抗炎和保肝作用，可用于 ALI 研究。

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RIPK2-IN-8

RIPK2-IN-8 Chemical Structure

CAS No. : 3036254-29-9

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RIPK2-IN-8 相关抗体

Top Publications Citing Use of Products

查看 RIP kinase 亚型特异性产品:

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RIPK1 RIPK2 RIPK3

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 p38 MAPK 亚型特异性产品:

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

查看 Interleukin Related 亚型特异性产品:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RIPK2-IN-8 is an orally active and highly selective RIPK2 inhibitor (IC50 = 11 nM). RIPK2-IN-8 is highly selective for RIPK2 over RIPK1 (IC50 > 30,000 nM) and has a moderate inhibitory effect on RIPK3 (IC50 = 44.61 nM). RIPK2-IN-8 inhibits the NOD2-RIPK2 signaling pathway and the expression of the inflammatory cytokines IL-6 and TNFα, thereby exerting anti-inflammatory effects. RIPK2-IN-8 has demonstrated anti-inflammatory and hepatoprotective effects in an acute liver injury (ALI) model and can be used in ALI research[1].

IC50 & Target[1]

RIPK2

11 nM (IC50)

RIPK3

44.61 nM (IC50)

IL-6

 

体外研究
(In Vitro)

RIPK2-IN-8 (Compound HY3) (0-10 μM，0.5-6 小时) 在 L18-MDP (HY-148690) 刺激的 THP-1 细胞中可延缓 NF-kB 和 MAPK 的活化，且不影响蛋白表达或细胞活力[1]。
RIPK2-IN-8 (1 μM) 对炎症相关激酶 (如 BTK、FLT3、JNK2α2、SAPK3、MSK1、MAPKAP-K2) 几乎没有抑制活性[1]。
RIPK2-IN-8 对 H9C2 细胞具有较弱的细胞毒性 (IC50 > 40 μM)[1]。
RIPK2-IN-8 在 Muramyl dipeptide (MDP) (HY-127090) 刺激的 THP-1 细胞中抑制 IL-8 的产生，IC50 为 29 nM[1]。

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

RIPK2-IN-8 相关抗体:

Western Blot Analysis[1]

Cell Line: THP-1 cells were stimulated with L18-MDP
Concentration: 0 μM, 0.001 μM, 0.003 μM, 0.01 μM, 0.03 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM
Incubation Time: 0.5 h, 6 h
Result: Delayed phosphorylation of p65, p38, and JNK. At 1 μM, did not alter the total levels of p65, p38, JNK, and β-actin.
Did not affect phosphorylation of RIPK3 or MLKL, key markers of necroptotic signaling.
体内研究
(In Vivo)

RIPK2-IN-8 (Compound HY3) (7.5-30 mg/kg，口服，一次) 在 MDP 诱导的腹膜炎小鼠模型中抑制 RIPK2 激酶活性，从而阻断下游炎症信号的激活，并进一步影响细胞因子 IL-6 的合成和释放[1]。
RIPK2-IN-8 (5-20 mg/kg，口服，一次) 在 Acetaminophen (APAP) (HY-66005) 诱导的 ALI 模型中通过抑制炎症细胞因子的表达发挥保肝作用，从而降低血清炎症标志物水平，减轻肝损伤[1]。

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

Animal Model: MDP-induced (100 μg, i.p.) peritonitis mice (Female C57BL/6 at 8 weeks of age) model[1]
Dosage: 7.5 mg/kg, 15 mg/kg, 30 mg/kg
Administration: p.o., once
Result: Reduced IL-6 levels, with IL-6 levels dropping to 23.9 pg/mL at 30 mg/kg, comparable to the RIPK2-positive compound GSK2983559 (HY-112038A).
Animal Model: APAP-induced (500 mg/kg, i.p.) ALI mice (Female C57BL/6 at 8 weeks of age) model[1]
Dosage: 5 mg/kg, 10 mg/kg, 20 mg/kg
Administration: p.o., once
Result: Reduced ALT and AST levels, particularly in the high-dose group, where ALT and AST levels decreased to 202 and 275 U/L, respectively.
Reduced serum and mRNA levels of IL-6 and TNFα.
分子量

453.56

Formula

C22H20FN5OS2
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

RIPK2-IN-8 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:

RIPK2-IN-83036254-29-9RIP kinaseNF-κBp38 MAPKInterleukin RelatedReceptor-interacting protein kinasesRIPKNuclear factor-κBNuclear factor-kappaBILInhibitorH9C2 cellsTHP-1 cellsALIMDP-induced peritonitisC57BL/6 miceAcute liver injuryinhibitorinhibit

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