| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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GSK-872 hydrochloride (GSK'872; GSK2399872A; GSK872; GSK-872) is a novel, potent and selective RIPK3 (receptor interacting protein kinase-3) inhibitor with anticancer and anti-inflammatory effects. It inhibits kinase activity with an IC50 of 1.3 nM and has a high binding affinity to the RIP3 kinase domain at a value of 1.8 nM. Toll-like receptor 3 (TLR3)-induced necroptosis is inhibited by GSK'872 in mouse cells. Additionally, GSK'872 blocks the RIP1-independent necroptosis pathways of TLR3- or DAI-induced death. Primary hepatocytes benefit significantly from pretreatment with GSK'872. Nec1's inhibition of RIPK1 does not, however, give primary hepatocytes any added protection.
| Targets |
RIPK3
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|---|---|---|
| ln Vitro |
GSK-872 fails to inhibit the majority of the 300 human protein kinases tested when measured at 1 μM.Direct tests show that it is unable to inhibit RIP1 kinase. In HT-29 cells, GSK-872 inhibits TNF-induced necroptosis in a concentration-dependent manner. In comparison to cell-free biochemical assays, the IC50 is 100–1000 times higher in cell-based assays. In primary human neutrophils isolated from whole blood, GSK-872 also inhibits necroptosis. GSK-872 blocks two RIP1-independent pathways of necroptosis, TLR3- or DAI-induced death. Caspase activation is brought on by it, and apoptotic cell death follows.
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| ln Vivo |
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| Enzyme Assay |
GSK-872 (also known as GSK2399872A, GSK872, or GSK-872) is a potent and selective RIPK3 (receptor interacting protein kinase-3) inhibitor. It has a high binding affinity to the RIP3 kinase domain with IC50 value of 1.8 nM, and it inhibits the kinase activity with an IC50 of 1.3 nM.
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| Cell Assay |
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.
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| Animal Protocol |
Eight weeks old Sprague-Dawley male rats with 300-320 g body weight (rat SAH model)[3]
25 mM/6 μL Syringe pump (intracerebroventricular) at 30 min after SAH |
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| References |
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| Molecular Formula |
C19H18CLN3O2S2
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|---|---|
| Molecular Weight |
419.95
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| CAS # |
2703752-81-0
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| Related CAS # |
GSK-872;1346546-69-7
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| Appearance |
Solid
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| SMILES |
CC(C)S(=O)(=O)C1=CC2=C(C=CN=C2C=C1)NC3=CC4=C(C=C3)SC=N4.Cl
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| InChi Key |
VKCVPZFWFZKUJY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H17N3O2S2.ClH/c1-12(2)26(23,24)14-4-5-16-15(10-14)17(7-8-20-16)22-13-3-6-19-18(9-13)21-11-25-19;/h3-12H,1-2H3,(H,20,22);1H
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| Chemical Name |
N-(6-propan-2-ylsulfonylquinolin-4-yl)-1,3-benzothiazol-5-amine;hydrochloride
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| Synonyms |
GSK-872 hydrochloride
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~10 mg/mL (~23.8 mM)
H2O: ~2.5 mg/mL (~6.0 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.21 mg/mL (0.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 2.1 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3812 mL | 11.9062 mL | 23.8124 mL | |
| 5 mM | 0.4762 mL | 2.3812 mL | 4.7625 mL | |
| 10 mM | 0.2381 mL | 1.1906 mL | 2.3812 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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