GSK'872 (GSK2399872A) - 10mM in DMSO , CAS No.1346546-69-7

CAS: 1346546-69-7 Cat. No.: G409176 Peso molecular: 383.48

GRADE & PURITY 10mM in DMSO

Synonyms

4-​Quinolinamine, N-​5-​benzothiazolyl-​6-​[(1-​methylethyl)​sulfonyl]​-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

GSK'872 (GSK2399872A) GSK'872 (GSK2399872A) is a potent and selective RIP3 kinase inhibitor which binds RIP3 kinase domain with high affinity (IC50=1.8 nM) and inhibits kinase activity with IC50 of 1.3 nM. It has minimal cross-reactivity.
In vitro

When assayed at 1 μM, GSK\'872 fails to inhibit most of 300 human protein kinases tested. It fails to inhibit RIP1 kinase when tested directly. GSK\'872 blocks TNF-induced necroptosis in a concentration-dependent manner in HT-29 cells. In cell-based assays, there is a 100- to 1000-fold shift in the IC50 compared to the cell-free biochemical assays. GSK\'872 also blocks necroptosis in primary human neutrophils isolated from whole blood. GSK\'872 inhibits TLR3- or DAI-induced death, two RIP1-independent pathways of necroptosis. It induces caspase activation followed by apoptotic cell death.

In vivo

GSK\'872 treatment significantly decreases HIF-1α expression compared with no treatment after ischemia injury in vivo.
Cell Data

cell lines：

Concentrations：0.3, 1, 3 μM

Incubation Time：18 h

Powder Purity:≥99%

Specifications

Sinónimos

4-​Quinolinamine, N-​5-​benzothiazolyl-​6-​[(1-​methylethyl)​sulfonyl]​-

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

GSK\'872 (GSK2399872A) is a potent and selective RIP3 kinase inhibitor which binds RIP3 kinase domain with high affinity (IC50=1.8 nM) and inhibits kinase activity with IC50 of 1.3 nM. It has minimal cross-reactivity.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Tipo de acción

INHIBITOR

Nombres e identificadores

• Isómeros SMILES: CC(C)S(=O)(=O)C1=CC2=C(C=CN=C2C=C1)NC3=CC4=C(C=C3)SC=N4
• Peso molecular: 383.48
• Reaxy-Rn: 25153150
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=25153150&ln=

Referencias

1. Chenying Zeng, Linjian Chen, Jiajie Lin, Zipeng Xiao, Qingqiang Tu, Wenhui Yu, Weihao Zhang, Qibo Li, Yanfeng Wu, Zhongyu Xie, Ziji Zhang.  (2025)  Taraxasterol Alleviates Osteoporosis by Targeting PI3K/AKT/PPARγ Signaling Axis to Suppress Necroptosis and Reverse Osteogenic-Adipogenic Differentiation Imbalance in BMSCs.  PHYTOMEDICINE,      [PMID:41317432] [10.1016/j.phymed.2025.157277]