2. Apoptosis MAPK/ERK Pathway
  3. RIP kinase Mixed Lineage Kinase Apoptosis
  4. WJH-C19

WJH-C19 是一种具备口服活性的 RIPK1 抑制剂，其 IC50 为 5.7 nM。WJH-C19 可抑制 RIPK1/RIPK3/MLKL 信号轴，阻断 RIPK1 磷酸化，抑制下游 RIPK3 和 MLKL 的磷酸化，破坏坏死小体的形成，在多种细胞系中展现出坏死性凋亡 (Apoptosis) 保护作用。WJH-C19 在小鼠结肠炎模型中通过调节坏死性凋亡通路改善炎症性肠病症状。WJH-C19 改善类风湿性关节炎小鼠模型的炎症和骨破坏。WJH-C19 可用于炎症性肠病、类风湿性关节炎的相关研究。

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WJH-C19

WJH-C19 Chemical Structure

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WJH-C19 相关抗体

Top Publications Citing Use of Products

查看 RIP kinase 亚型特异性产品:

查看所有亚型
RIPK1 RIPK2 RIPK3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

WJH-C19 is an orally active RIPK1 inhibitor with an IC50 of 5.7 nM. WJH-C19 inhibits the RIPK1/RIPK3/MLKL signaling axis, blocks RIPK1 phosphorylation, suppresses the phosphorylation of downstream RIPK3 and MLKL, disrupts necrosome formation, and exhibits protective effects against necroptosis (Apoptosis) in multiple cell lines. WJH-C19 ameliorates symptoms of inflammatory bowel disease in a mouse colitis model by regulating the necroptosis pathway. WJH-C19 alleviates inflammation and bone destruction in a mouse model of rheumatoid arthritis. WJH-C19 is applicable to research related to inflammatory bowel disease and rheumatoid arthritis[1].

IC50 & Target[1]

RIPK1

5.7 nM (IC50)

RIPK3

 

体外研究
(In Vitro)

WJH-C19 (Compound 10e12) (25 h) 在多种细胞系中展现出强效的浓度依赖性坏死性凋亡保护作用，其 EC50 值分别为 L929 细胞 0.28 nM、HT22 细胞 4.0 nM、HT29 细胞 1.6 nM 以及 U937 细胞 2.0 nM；且该化合物可剂量依赖性地减少坏死性凋亡的 L929 细胞[1]。
WJH-C19 可强效抑制 RIPK1 激酶活性，其 IC50 为 5.7 nM[1]。
WJH-C19 (0.5-50 nM) 可浓度依赖性地抑制 L929 细胞中 TNFα/z-VAD-FMK (HY-16658BG) (TZ)诱导的 RIPK1、RIPK3 和 MLKL 的磷酸化，以及 HT29 细胞中 mTNFα/Smac mimetic/z-VAD-FMK (TSZ) 诱导的磷酸化，从而阻断坏死小体的形成和下游的坏死性凋亡信号通路[1]。

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

WJH-C19 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route CL Vss T1/2 AUC0-t Tmax Cmax AUC0-∞ MRT0-∞ Bioavailability
Mice[1] 1 mg/kg i.v. 0.11 L/h/kg 0.93 L/kg 5.89 h 8914.61 ng·h/mL 0.083 h 10495 ng/mL 9205.63 ng·h/mL 4.77 h /
Mice[1] 10 mg/kg p.o. / / 6.54 h 10906.26 ng·h/mL 6 h 1051 ng/mL 11864.51 ng·h/mL / 12.89 %
体内研究
(In Vivo)

WJH-C19 (1.25-2.5 mg/kg; p.o.; daily; 7 days) 可强效改善 DSS (HY-116282C) 诱导的雌性 C57BL/6 小鼠结肠炎，实现 47.5% 的体重恢复、42.9% 的 DAI 降低，并能强效抑制 RIPK1/RIPK3/MLKL 信号轴[1]。
WJH-C19 (10-20 mg/kg; p.o.; daily; 14 days) 可强效改善雌性 C57BL/6 小鼠中由 CFA (HY-153808) 诱导的类风湿性关节炎，减轻足爪肿胀、关节炎症与骨破坏，并抑制 RIPK1/RIPK3/MLKL 信号轴[1]。

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

Animal Model: C57BL/6 (female, 10-12 weeks old, ~28 g, DSS-induced colitis)[1]
Dosage: 2.5 mg/kg; 1.25 mg/kg
Administration: p.o.; daily; 7 days
Result: Achieved 47.5% body weight recovery, 42.9% disease activity index (DAI) reduction, and 60.5% colon length recovery at 2.5 mg/kg.
Achieved 33.2% body weight recovery, 32.1% DAI reduction, and 35.1% colon length recovery at 1.25 mg/kg.
Reduced proinflammatory cytokine levels (IL-1β, IL-6, TNFα) and increased anti-inflammatory cytokine IL-10 levels in colon tissue at both doses.
Inhibited phosphorylation of RIPK1, RIPK3, and MLKL in colonic proteins at both doses, with the high dose showing the most robust inhibition.
Reduced mucosal damage, maintained intact glandular architecture, and restored zonula occludens-1 (ZO-1) and Occludin expression at both doses, with the high-dose group exhibiting near-normal morphology.
Animal Model: C57BL/6 (female, 8 weeks old, CFA-induced rheumatoid arthritis)[1]
Dosage: 20 mg/kg; 10 mg/kg
Administration: p.o.; daily; 14 days
Result: Reduced paw swelling percentage, ankle joint temperature, and arthritis index scores in a dose-dependent manner at both doses, with efficacy comparable or superior to celecoxib.
Reduced osteophyte formation and reversed bone destructive changes, including improvements in bone mineral density (BMD), cortical BMD, trabecular number (Tb.N), connectivity density (Conn.D), bone volume (BV), cortical volume (CV), trabecular separation (Tb.Sp), pore number (Po.N), cortical area (Ct.Ar), and cortical thickness (Ct.Th) at both doses, with the high dose showing the most pronounced improvement.
Reduced inflammatory cell infiltration, synovial hyperplasia, and cartilage erosion at both doses, with the high-dose group achieving histological scores approaching normal levels.
Reduced the M1/M2 macrophage ratio in spleens in a dose-dependent manner at both doses, shifting toward the anti-inflammatory M2 phenotype.
Suppressed expression of phosphorylated RIPK1, RIPK3, and MLKL in ankle joints at both doses, with the high dose showing the strongest inhibition.
分子量

516.01

Formula

C27H22ClN5O2S
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

WJH-C19 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:

WJH-C19RIP kinaseMixed Lineage KinaseApoptosisReceptor-interacting protein kinasesRIPKMLKsRIPK1 inhibitorL929 cellsHT22 cellsHT29cellsU937 cellsinflammatory bowel diseaserheumatoid arthritisC57BL/6 mice
Inhibitorinhibitorinhibit

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