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Purity: ≥98%
GSK'872 (also known as GSK2399872A, GSK872, or GSK-872) is a novel, potent and selective RIPK3 (receptor interacting protein kinase-3) inhibitor. With an IC50 value of 1.8 nM, it has a strong affinity for the RIP3 kinase domain and inhibits kinase activity with an IC50 of 1.3 nM. Toll-like receptor 3 (TLR3)-induced necroptosis in mouse cells is inhibited by GSK'872. Additionally, GSK'872 prevents death brought on by TLR3 or DAI, two necroptosis pathways not dependent on RIP1. Primary hepatocytes receive substantial protection after pretreatment with GSK'872. However, primary hepatocytes are not given any protection by RIPK1 inhibition (by Nec1).
| Targets |
RIP3K (IC50 = 1.3 nM)
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| ln Vitro |
When assayed at 1 μM, GSK'872 fails to inhibit most of 300 human protein kinases tested. 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 fold 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. It causes the activation of caspase, which is followed by apoptotic cell death[1].
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| ln Vivo |
GSK'872 treatment significantly reduces HIF-1 expression in comparison to no treatment after ischemia injury in vivo[3].
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| Enzyme Assay |
GSK872 (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 |
RIP3 kinase inhibitors GSK'843 or GSK'872 are used to treat 3T3-SA cells at the indicated concentrations for 18 hours after TNF treatment in the presence of Z-VAD-fmk in vehicle control (DMSO) or other treatments.
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| References |
| Molecular Formula |
C19H17N3O2S2
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|---|---|
| Molecular Weight |
383.49
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| Exact Mass |
383.0762
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| Elemental Analysis |
C, 59.51; H, 4.47; N, 10.96; O, 8.34; S, 16.72
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| CAS # |
1346546-69-7
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| Related CAS # |
GSK-872 hydrochloride;2703752-81-0
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| Appearance |
Solid powder
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| SMILES |
CC(C)S(=O)(=O)C1=CC2=C(C=CN=C2C=C1)NC3=CC4=C(C=C3)SC=N4
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| InChi Key |
ZCDBTQNFAPKACC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H17N3O2S2/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)
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| Chemical Name |
N-(6-propan-2-ylsulfonylquinolin-4-yl)-1,3-benzothiazol-5-amine
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| Synonyms |
GSK2399872A; GSK872; GSK-872; GSK 872; GSK2399872-A; GSK2399872 A; GSK-2399872A; GSK-2399872 A
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| HS Tariff Code |
2934.99.9001
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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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.42 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6076 mL | 13.0381 mL | 26.0763 mL | |
| 5 mM | 0.5215 mL | 2.6076 mL | 5.2153 mL | |
| 10 mM | 0.2608 mL | 1.3038 mL | 2.6076 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05804123 | Recruiting | Drug: Cefotaxime Drug: Ciprofloxacin |
Upper Respiratory Tract Infections |
Anabio R&D | October 28, 2021 | Not Applicable |
Products are for research use only; We do not sell to patients
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