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MedKoo Cat#: 406953 | Name: GSK481
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

GSK481 is a Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitor (RIP1 inhibitor). The recent discovery of the role of receptor interacting protein 1 (RIP1) kinase in tumor necrosis factor (TNF)-mediated inflammation has led to its emergence as a highly promising target for the treatment of multiple inflammatory diseases.

Chemical Structure

GSK481
GSK481
CAS#1622849-58-4

Theoretical Analysis

MedKoo Cat#: 406953

Name: GSK481

CAS#: 1622849-58-4

Chemical Formula: C21H19N3O4

Exact Mass: 377.1376

Molecular Weight: 377.40

Elemental Analysis: C, 66.83; H, 5.07; N, 11.13; O, 16.96

Price and Availability

Size Price Availability Quantity
5mg USD 295.00 2 Weeks
10mg USD 450.00 2 Weeks
25mg USD 850.00 2 Weeks
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Related CAS #
No Data
Synonym
GSK481; GSK-481; GSK 481
IUPAC/Chemical Name
5-(phenylmethyl)-N-[(3S)-2,3,4,5-tetrahydro-5-methyl-4-oxo-1,5-benzoxazepin-3-yl]-3-isoxazolecarboxamide
InChi Key
KNOUWGGQMADIBV-KRWDZBQOSA-N
InChi Code
InChI=1S/C21H19N3O4/c1-24-18-9-5-6-10-19(18)27-13-17(21(24)26)22-20(25)16-12-15(28-23-16)11-14-7-3-2-4-8-14/h2-10,12,17H,11,13H2,1H3,(H,22,25)/t17-/m0/s1
SMILES Code
O=C(C1=NOC(CC2=CC=CC=C2)=C1)N[C@H]3COC4=CC=CC=C4N(C)C3=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
GSK481 is a highly potent, selective, and specific receptor interacting protein 1 (RIP1) kinase inhibitor with an IC50 of 1.3 nM, which inhibits Ser166 phosphorylation in wild-type human RIP1 (IC50=2.8 nM). GSK481 also exhibits excellent translation in the U937 cellular assay with an IC50 of 10 nM.
In vitro activity:
Pan-caspase blocker zVAD and RIP1 inhibitors GSK'481 or necrostatin-1 revealed interesting modulations of such sub-populations of Jurkat cells. Reference: Methods. 2018 Feb 1;134-135:56-66. https://pubmed.ncbi.nlm.nih.gov/29175336/
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMF 25.0 66.24
DMSO 46.7 123.65
Ethanol 30.0 79.49
Ethanol:PBS (pH 7.2) (1:10) 0.1 0.24
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 377.40 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Lee HL, Pike R, Chong MHA, Vossenkamper A, Warnes G. Simultaneous flow cytometric immunophenotyping of necroptosis, apoptosis and RIP1-dependent apoptosis. Methods. 2018 Feb 1;134-135:56-66. doi: 10.1016/j.ymeth.2017.10.013. Epub 2017 Nov 24. PMID: 29175336. 2. Harris PA, King BW, Bandyopadhyay D, Berger SB, Campobasso N, Capriotti CA, Cox JA, Dare L, Dong X, Finger JN, Grady LC, Hoffman SJ, Jeong JU, Kang J, Kasparcova V, Lakdawala AS, Lehr R, McNulty DE, Nagilla R, Ouellette MT, Pao CS, Rendina AR, Schaeffer MC, Summerfield JD, Swift BA, Totoritis RD, Ward P, Zhang A, Zhang D, Marquis RW, Bertin J, Gough PJ. 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. doi: 10.1021/acs.jmedchem.5b01898. Epub 2016 Feb 23. PMID: 26854747.
In vitro protocol:
1. Lee HL, Pike R, Chong MHA, Vossenkamper A, Warnes G. Simultaneous flow cytometric immunophenotyping of necroptosis, apoptosis and RIP1-dependent apoptosis. Methods. 2018 Feb 1;134-135:56-66. doi: 10.1016/j.ymeth.2017.10.013. Epub 2017 Nov 24. PMID: 29175336. 2. Harris PA, King BW, Bandyopadhyay D, Berger SB, Campobasso N, Capriotti CA, Cox JA, Dare L, Dong X, Finger JN, Grady LC, Hoffman SJ, Jeong JU, Kang J, Kasparcova V, Lakdawala AS, Lehr R, McNulty DE, Nagilla R, Ouellette MT, Pao CS, Rendina AR, Schaeffer MC, Summerfield JD, Swift BA, Totoritis RD, Ward P, Zhang A, Zhang D, Marquis RW, Bertin J, Gough PJ. 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. doi: 10.1021/acs.jmedchem.5b01898. Epub 2016 Feb 23. PMID: 26854747.
In vivo protocol:
TBD
Beal AM, Bertin J, Reilly MA. Use of RIP1 Kinase Small-Molecule Inhibitors in Studying Necroptosis. Methods Mol Biol. 2018;1857:109-124. doi: 10.1007/978-1-4939-8754-2_11. PMID: 30136235.