Cofttek holdings limited

S6 kinase&PKD-1

GSK2982772 (1622848-92-3)

GSK2982772 is a potent and selective receptor Interacting Protein 1 (RIP1) KinaseSpecific Clinical Candidate for the Treatment of Inflammatory Diseases.

Not Intended for Therapeutic Use. For research use only.

CAS: 1622848-92-3 Category

GSK2982772 (1622848-92-3) Description:

GSK2982772 is a potent and ATP competitive RIP1 inhibitor with an IC50 of 16 nM. GSK2982772 is a potent and selective receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate for the Treatment of Inflammatory Diseases. GSK2982772 is, currently in phase 2a clinical studies for psoriasis, rheumatoid arthritis, and ulcerative colitis. GSK2982772 potently binds to RIP1 with exquisite kinase specificity and has excellent activity in blocking many TNF-dependent cellular responses. RIP1 has emerged as an important upstream kinase that has been shown to regulate inflammation through both scaffolding and kinase specific functions.

GSK2982772 (1622848-92-3) Specifications:

Product Name GSK2982772
Synonym GSK2982772; GSK-2982772; GSK 2982772.
Chemical Name (S)-5-Benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b]-[1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide
Drug Class ATP competitive RIP1 inhibitor
Purity ≥98% (HPLC)
CAS Number 1622848-92-3
Molecular Formula  C20H19N5O3
Molecular Weight 377.404
Monoisotopic Mass 377.1488  g/mol
MDL number MFCD09953122
InChIKey LYPAFUINURXJSG-AWEZNQCLSA-N
InChi Code InChI=1S/C20H19N5O3/c1-25-15-9-5-6-10-16(15)28-12-14(20(25)27)21-19(26)18-22-17(23-24-18)11-13-7-3-2-4-8-13/h2-10,14H,11-12H2,1H3,(H,21,26)(H,22,23,24)/t14-/m0/s1
SMILES O=C(C1=NN=C(CC2=CC=CC=C2)N1)N[[email protected]@H]3C(N(C)C4=CC=CC=C4OC3)=O
Form Powder
Color Yellow
Solubility  Soluble in DMSO.
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application A  ATP competitive RIP1 inhibitor

 


RIDADR NONH for all modes of transport

References:

[1]. Weisel K, Scott NE, Tompson DJ, Votta BJ, Madhavan S, Povey K, Wolstenholme A, Simeoni M, Rudo T, Richards-Peterson L, Sahota T, Wang JG, Lich J, Finger J, Verticelli A, Reilly M, Gough PJ, Harris PA, Bertin J, Wang ML.

[2]. Finger JN, Brusq JM, Campobasso N, Cook MN, Deutsch J, Haag H, Harris PA, Jenkins EL, Joglekar D, Lich JD, Maguire S, Nagilla R, Rivera EJ, Sun H, Votta BJ, Bertin J, Gough PJ. Pharmacol Res Perspect. 2017 Dec;5(6). doi: 10.1002/prp2.377 PMID:29226625

[3]. Weisel K, Scott NE, Tompson DJ, Votta BJ, Madhavan S, Povey K, Wolstenholme A, Simeoni M, Rudo T, Richards-Peterson L, Sahota T, Wang JG, Lich J, Finger J, Verticelli A, Reilly M, Gough PJ, Harris PA, Bertin J, Wang ML. Pharmacol Res Perspect. 2017 Dec;5(6). doi: 10.1002/prp2.365. PMID:29226626

[4].Gutiérrez-Martínez; Rubio; Piedra-Quintero; Lopez-Mendez; Serrano; Reyes-Maldonado; Salinas-Lara;Villegas-Sepúlveda; Nava – Translational Oncology 2019 vol. 12 # 1 p. 24 – 35

[5]. Harris PA, Berger SB, Jeong JU, Nagilla R, Bandyopadhyay D, Campobasso N, Capriotti CA, Cox JA, Dare L, Dong X, Eidam PM, Finger JN, Hoffman SJ, Kang J, Kasparcova V, King BW, Lehr R, Lan Y, Leister LK, Lich JD, MacDonald TT, Miller NA, Ouellette MT, Pao CS, Rahman A, Reilly MA, Rendina AR, Rivera EJ, Schaeffer MC, Sehon CA, Singhaus RR, Sun HH, Swift BA, Totoritis RD, Vossenkämper A, Ward P, Wisnoski DD, Zhang D, Marquis RW, Gough PJ, Bertin J. Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases. J Med Chem. 2017 Feb 10. doi: 10.1021/acs.jmedchem.6b01751. [Epub ahead of print] PubMed PMID: 28151659.