ChemicalBook > CAS DataBase List > GSK872

GSK872

Product Name
GSK872
CAS No.
1346546-69-7
Chemical Name
GSK872
Synonyms
GSK872;CS-2489;GSK2399872A;GSK'872 (GSK2399872A);GSK-872;GSK 872;GSK872;GSK' 872 (GSK2399872A);GSK'872;GSK872;GSK2399872A;N-(6-(Isopropylsulfonyl)quinolin-4-yl)benzo[d]thiazol-5-amine;N-5-benzothiazolyl-6-[(1-methylethyl)sulfonyl]-4-Quinolinamine;N-(6-propan-2-ylsulfonylquinolin-4-yl)-1,3-benzothiazol-5-amine
CBNumber
CB03165850
Molecular Formula
C19H17N3O2S2
Formula Weight
383.49
MOL File
1346546-69-7.mol
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GSK872 Property

Boiling point:
625.7±55.0 °C(Predicted)
Density 
1.395±0.06 g/cm3(Predicted)
storage temp. 
Keep in dark place,Inert atmosphere,Room temperature
solubility 
Soluble in DMSO (up to at least 25 mg/ml)
pka
5.53±0.49(Predicted)
form 
solid
color 
Off-White or pale yellow
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
23300
Product name
GSK872
Purity
≥98%
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
23300
Product name
GSK872
Purity
≥98%
Packaging
5mg
Price
$116
Updated
2024/03/01
Cayman Chemical
Product number
23300
Product name
GSK872
Purity
≥98%
Packaging
10mg
Price
$214
Updated
2024/03/01
Tocris
Product number
6492
Product name
GSK'872
Purity
≥98%(HPLC)
Packaging
10
Price
$169
Updated
2021/12/16
Tocris
Product number
6492
Product name
GSK'872
Purity
≥98%(HPLC)
Packaging
50
Price
$710
Updated
2021/12/16
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GSK872 Chemical Properties,Usage,Production

Description

GSK 872 (CAS 1346546-69-7) is a potent (IC50 = 1.8nM domain binding; IC50 = 1.3 nM kinase activity) and selective inhibitor of receptor interacting protein 3 (RIP3).1 It is able to prevent necroptosis, virus-induced necrosis, and TLR3-induced necrosis.1,2 GSK872 can induce Caspase8-mediated apoptosis at higher concentrations (e.g.3 μM).2

Uses

GSK''872 is a potent and selective receptor activating protein kinase 3 (RIP3) inhibitor (IC50 = 1.3 nM). Exhibits >1000-fold selectivity for RIP3 over a panel of 300 other kinases including RIP1. Inhibits TNF-induced cell death in 3T3-SA cells and TLR3-induced necrosis in fibroblasts in vitro. Blocks necroptosis of primary human neutrophils from whole blood. Also induces apoptosis at higher concentrations (3 - 10 μM).

Biological Activity

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.

storage

-20°C

References

1)?Kaiser et al. (2013) Toll-like receptor 3-mediated necrosis via TRIF, RIP3, and MLKL; J. Biol. Chem.?288 31279 2)?Mandal et al. (2014) RIP3 induces apoptosis independent of pro-necrotic kinase activity; Mol. Cell 56 481

GSK872 Preparation Products And Raw materials

Raw materials

Preparation Products

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1346546-69-7, GSK872Related Search:


  • GSK872
  • N-5-benzothiazolyl-6-[(1-methylethyl)sulfonyl]-4-Quinolinamine
  • N-(6-(Isopropylsulfonyl)quinolin-4-yl)benzo[d]thiazol-5-amine HCl salt
  • N-(6-propan-2-ylsulfonylquinolin-4-yl)-1,3-benzothiazol-5-amine
  • CS-2489
  • GSK-872;GSK 872;GSK872
  • GSK2399872A
  • GSK'872;GSK872;GSK2399872A
  • GSK'872 (GSK2399872A)
  • 4-Quinolinamine, N-5-benzothiazolyl-6-[(1-methylethyl)sulfonyl]-
  • N-(6-(Isopropylsulfonyl)quinolin-4-yl)benzo[d]thiazol-5-amine HCL SALT // GSK-872 HCL
  • N-(6-(Isopropylsulfonyl)quinolin-4-yl)benzo[d]thiazol-5-amine
  • translocation,GSK-872,neurological,HMGB1,Receptor-interacting protein kinases,brain,GSK 872,cytoplasmic,deficits,Inhibitor,edema,inhibit,RIPK,RIP kinase
  • GSK' 872 (GSK2399872A)
  • 1346546-69-7