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| 5mg |
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| 25mg |
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| 100mg |
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Purity: ≥98%
GSK2983559 active metabolite, formerly known as RIPK2-IN-1, is an active metabolite of GSK2983559 which is a potent and selective inhibitor of receptor interacting protein-2 (RIP2) kinase.
| Targets |
RIP2 Kinase
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|---|---|
| ln Vitro |
GSK2983559 active metabolite is a novel prodrug of a quinazolyl amine that inhibits RIP2 kinase. RReceptor interacting protein-2 (RIP2) kinase, also known as CARD3, RICK, CARDIAK, or RIPK2, is a serine/threonine protein kinase belonging to the TKL family that participates in innate immune signaling. The N- and C-terminal caspase-recruitment domains (CARD) of RIP2 kinase are connected by an intermediate (IM) region. RIP2 kinase interacts with other CARD-containing proteins like NODI and NOD2 through its CARD domain. Cytoplasmic receptors called NODI and NOD2 are important for innate immune surveillance. They are activated by particular peptidoglycan motifs, including muramyl dipeptide and diaminopimelic acid (i.e., DAP), and recognize both gram positive and gram negative bacterial pathogens[1].
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| References |
| Molecular Formula |
C21H22N4O4S2
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|---|---|
| Molecular Weight |
458.55
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| Exact Mass |
458.1082
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| Elemental Analysis |
C, 55.01; H, 4.84; N, 12.22; O, 13.96; S, 13.98
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| CAS # |
1423186-80-4
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| Related CAS # |
GSK2983559 free acid;1579965-12-0;GSK2983559
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| Appearance |
Solid powder
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| SMILES |
CC(C)(C)S(=O)(=O)C1=C(C=C2C(=C1)C(=NC=N2)NC3=CC4=C(C=C3)SC=N4)OCCOP(=O)(O)O
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| InChi Key |
UHDOJINBFLDQJM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H22N4O4S2/c1-21(2,3)31(27,28)19-9-14-15(10-17(19)29-7-6-26)22-11-23-20(14)25-13-4-5-18-16(8-13)24-12-30-18/h4-5,8-12,26H,6-7H2,1-3H3,(H,22,23,25)
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| Chemical Name |
2-[4-(1,3-benzothiazol-5-ylamino)-6-tert-butylsulfonylquinazolin-7-yl]oxyethanol
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| Synonyms |
GSK2983559; GSK-2983559; GSK 2983559; RIPK2-IN-1; RIPK2 IN 1; RIPK2IN;1 RIPK2 inhibitor-1; RIPK2 inhibitor 1
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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) |
DMSO: ~25 mg/mL (~54.5 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.45 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.45 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1808 mL | 10.9039 mL | 21.8079 mL | |
| 5 mM | 0.4362 mL | 2.1808 mL | 4.3616 mL | |
| 10 mM | 0.2181 mL | 1.0904 mL | 2.1808 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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