GSK872
- Product Name
- GSK872
- CAS No.
- 1346546-69-7
- Chemical Name
- GSK872
- Synonyms
- GSK872;CS-2489;GSK'872;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
- CBNumber
- CB03165850
- Molecular Formula
- C19H17N3O2S2
- Formula Weight
- 383.49
- MOL File
- 1346546-69-7.mol
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.
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..…
N-Bromosuccinimide Price
- Product number
- 23300
- Product name
- GSK872
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 23300
- Product name
- GSK872
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $116
- Updated
- 2024/03/01
- Product number
- 23300
- Product name
- GSK872
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $214
- Updated
- 2024/03/01
- Product number
- 6492
- Product name
- GSK'872
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $169
- Updated
- 2021/12/16
- Product number
- 6492
- Product name
- GSK'872
- Purity
- ≥98%(HPLC)
- Packaging
- 50
- Price
- $710
- Updated
- 2021/12/16
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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