| GSK481RIP1(Receptor Interacting Protein Kinase 1) inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
GSK481 Dilution Calculator
calculate
GSK481 Molarity Calculator
calculate
| Cas No. | 1622849-58-4 | SDF | Download SDF |
| Chemical Name | (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)isoxazole-3-carboxamide | ||
| Canonical SMILES | O=C(C1=NOC(CC2=CC=CC=C2)=C1)N[C@H]3COC4=CC=CC=C4N(C)C3=O | ||
| Formula | C21H19N3O4 | M.Wt | 377.39 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: 1.3 nM for RIP1
GSK481 is a receptor interacting protein kinase 1 (RIP1) inhibitor.
The role of RIP1 kinase in tumor necrosis factor mediated inflammation has resulted in its emergence as a promising target for the treatment of multiple inflammatory diseases.
In vitro: Previous study showed that GSK481 could not only trigger an increase in biochemical activity but also exhibit great translation in the U937 cellular assay with IC50 of 10 nM. Moreover, GSK481 also showed complete specificity for RIP1 kinase against all other tested kinases when profiled over both a P33 radiolabeled assay screen. In tight-binding ADP-Glo IC50 evaluation with increasing ATP concentration, GSK481 exhibited a shift to lower potency, which was corresponding to a competitive model. In addition, GSK481 was also found to be a potent inhibitor of S166 phosphorylation in wild-type human RIP1 but was ineffective at reducing S166 phosphorylation for wild-type mouse RIP1. GSK481 was also able to more potently inhibit Ser166 phosphorylation in all three tested mouse RIP1 mutants than in wild-type mouse [1].
In vivo: So far, there is no animal in vivo data reported for GSK481.
Clinical trial: Up to now, GSK481 is still in the preclinical development stage.
Reference:[1] Harris PA et al. DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors. J Med Chem, 2016 Mar 10, 59(5):2163-78.
