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首页-小分子抑制剂&激动剂-Apoptosis-RIP kinase-Zharp2-1
Zharp2-1

Chemical Structure : Zharp2-1

CAS No.: 2772600-18-5

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Zharp2-1 (Zharp 2-1)

货号: PC-21082Not For Human Use, Lab Use Only.

Zharp2-1 is a novel potent, selective RIPK2 inhibitor with IC50 of 38.5 nM in ADP-Glo kinase assay, effectively blocks RIPK2 kinase function and NOD-mediated NF-κB/MAPK activation.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Zharp2-1 is a novel potent, selective RIPK2 inhibitor with IC50 of 38.5 nM in ADP-Glo kinase assay, effectively blocks RIPK2 kinase function and NOD-mediated NF-κB/MAPK activation.
Zharp2-1 has a high affinity to RIPK2 (Kd=3.1 nM) in binding assay.
Zharp2-1 shows no significant binding to RIPK1 with Kd of >30,000 nM or RIPK3 with Kd of 710 nM, does not affect the kinase activity of RIPK1 and RIPK3 even at 1 μM.
Zharp2-1 efficiently inhibits pro-inflammatory cytokine IL-8 in THP-1 cells with an IC50 of 6.4 nM stimulated by L18-MDP and an IC50 of 16.4 nM stimulated by MDP.
Zharp2-1 blocks cellular NOD-mediated activation of MAPK/NF-κB signaling pathway.
Zharp2-1 significantly inhibits MDP-induced cytokine release in PBMCs, with an IC50 of 0.8 nM for IL-8, 8.7 nM for IL-6 and 11.9 nM for TNF-α, exerts a higher efficacy compared to GSK2983559 (Cat# PC-73178).
Zharp2-1 (15 mg/kg, once daily by oral gavage for 6 day) significantly alleviates inflammatory bowel disease in rat model of colitis induced by dinitrobenzene sulfonic acid (DNBS).

物理化学性质&存储条件

分子量 383.41
分子式 C19H18N3O2PS
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

O=P(C)(C)C1=C(OC)C=C2N=CC=C(NC3=CC=C(SC=N4)C4=C3)C2=C1

参考文献

1. Yujun Lai, et al. Biochem Pharmacol. 2023 Aug;214:115647.

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