GSK2983559-AM

GSK2983559-AM, also known as GSK2983559 active metabolite, is an active metabolite of GSK2983559, also known as RIPK2-IN-1, is a potent and selective inhibitor of receptor interacting protein-2 (RIP2) kinase.

Product information

CAS Number: 1423186-80-4

Molecular Weight: 458.55

Formula: C21H22N4O4S2

Synonym:

GSK2983559-AM

GSK2983559-active metabolite

GSK-2983559

RIPK2-IN-1

RIPK2 inhibitor-1

GSK2983559

GSK-2983559  

GSK 2983559  

RIPK2 IN 1

RIPK2IN1

RIPK2 inhibitor 1

Chemical Name: 2-[[4-(5-Benzothiazolylamino)-6-[(1,1-dimethylethyl)sulfonyl]-7-quinazolinyl]oxy]ethanol

Smiles: CC(C)(C)S(=O)(=O)C1=CC2=C(NC3C=C4N=CSC4=CC=3)N=CN=C2C=C1OCCO

InChiKey: UHDOJINBFLDQJM-UHFFFAOYSA-N

InChi: 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)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

GSK2983559 active metabolite is a novel prodrug of a quinazolyl amine that inhibits RIP2 kinase. Receptor interacting protein-2 (RIP2) kinase, which is also referred to as CARD3, RICK, CARDIAK, or RIPK2, is a TKL family serine/threonine protein kinase involved in innate immune signaling. RIP2 kinase is composed of an N-terminal kinase domain and a C-terminal caspase-recruitment domain (CARD) linked via an intermediate (IM) region. The CARD domain of RIP2 kinase mediates interaction with other CARD-containing proteins, such as NODI and NOD2. NODI and NOD2 are cytoplasmic receptors which play a key role in innate immune surveillance. They recognize both gram positive and gram negative bacterial pathogens and are activated by specific peptidoglycan motifs, diaminopimelic acid (i.e., DAP) and muramyl dipeptide.

References:

1. Sheridan C. Publisher Correction: Death by inflammation: drug makers chase the master controller. Nat Biotechnol. 2019;37(4):480. doi:10.1038/s41587-019-0082-6.

Products are for research use only. Not for human use.