GSK'872 (GSK2399872A)

Catalog No.S8465

For research use only.

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.

GSK'872 (GSK2399872A) Chemical Structure

CAS No. 1346546-69-7

Selleck's GSK'872 (GSK2399872A) has been cited by 47 publications

Purity & Quality Control

Choose Selective RIP kinase Inhibitors

Biological Activity

Description 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.
Targets
RIP3K [1]
(Cell-free assay)
1.3 nM
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[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
K562  M{XmcGZ2dmO2aX;uJIF{e2G7 MoraNUBp NX33NXlrT1ONJ{i3NkB{cWewaX\pZ4FvfGy7IHnubIljcXSnZDDj[YxtKGSnYYTo MnTHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MkeyNFkoRjJ7NUK3NlA6RC:jPh?=
HBE cells MoW3SpVv[3Srb36gZZN{[Xl? M3ntPFUh|ryP M1zMOmdUUyd6N{KgeJJm[XSvZX70JJNq\26rZnnjZY51dHlicnXkeYNm\CC2aHWgdIFzfGmldXzheIUhdWG2dHXyJEhRVSlvaX7keYNm\CCneIDy[ZN{cW:wIH;mJGlNPiCjbnSgTWw5KGG2IHLveIghdVKQQTDhcoQheHKxdHXpckBt\X[nbIO= NWrpN4t[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2NlE4PTNpPkK5OlIyPzV|PD;hQi=>
U251 M4HMZ2Z2dmO2aX;uJIF{e2G7 NGLKXVg2KM7:TR?= M4LVTlEhcA>? NFzuVWRm\m[nY4TpeoVtgSCmZXPy[YF{\WRiVGC0MY1m\GmjdHXkJIN6fG:2b4jpZ4l1gQ>? M2niclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyN{G3N|A6Lz5|MEexO|MxQTxxYU6=
U87MG MVnGeY5kfGmxbjDhd5NigQ>? M1TmUFUh|ryP NFjZZZcyKGh? NGDHT|lm\m[nY4TpeoVtgSCmZXPy[YF{\WRiVGC0MY1m\GmjdHXkJIN6fG:2b4jpZ4l1gQ>? MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODdzN{OwPUc,OzB5MUezNFk9N2F-
HT-22 MkfLSpVv[3Srb36gZZN{[Xl? M3rhdFAvOSxiMTDhcoQhOTEkgJpOwG0> NHKxSmo6KGh? NFLqNnV7XkGGLDDHV2vjiJl6N{KgZY5lKGOxbXLpcoF1cX[nIHnueIVzfmWwdHnvckBidGyndnnheIVlKG2xcoDoc4xw\2mlIHHseIVz[XSrb37zJIFv\CCjdITlcpVifGWmIHPlcIwh\GWjdHigbY5lfWOnZDDifUBwgHmpZX6t[4x2[2:|ZTDk[ZBzcX[jdHnvckBidmRicnXvfJlo\W6jdHnvci=> NHLxbGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEeyOFg6OSd-Mki3NlQ5QTF:L3G+
MPSC1 cells MX3D[YxtKH[rYXLpcIl1gSCjc4PhfS=> MYe2JO69VQ>? NVuxW3RXOiCq NUPhVoZreHKnLYTy[YF1dWWwdDDmc5IhOuLCiXige4l1cCCJU1unPFczKHCjcoTpZYxtgSC{ZY\ldpNm\CCFRESwUE1qdmS3Y3XkJJJm\HWldHnvcpMhcW5iY3XscEB3cWGkaXzpeJk> Mn2yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|MUO5NVUoRjJ4M{GzPVE2RC:jPh?=
Assay
Methods Test Index PMID
Western blot Rip1 / Rip3 / p-MLKL / MLKL 31214277
Growth inhibition assay Cell viability 24019532
In vivo GSK'872 treatment significantly decreases HIF-1α expression compared with no treatment after ischemia injury in vivo[3].

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: 3T3-SA cells
  • Concentrations: 0.3, 1, 3 μM
  • Incubation Time: 18 h
  • Method:

    Viability of 3T3-SA cells at 18 h after treatment with TNF in the presence of Z-VAD-fmk in vehicle control (DMSO) or treated with the indicated concentrations of RIP3 kinase inhibitors, GSK'843 or GSK'872 are assayed.

Animal Research:

[3]

  • Animal Models: C57BL/6 mice
  • Dosages: 1.9 mmol/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 383.49
Formula

C19H17N3O2S2

CAS No. 1346546-69-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)S(=O)(=O)C1=CC2=C(C=CN=C2C=C1)NC3=CC4=C(C=C3)SC=N4

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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