GSK2983559 active metabolite |CAS 1423186-80-4

Cas No.:	1423186-80-4
Chemical Name:	GSK2983559-AM
Synonyms:	GSK2983559,GSK-2983559,GSK 2983559
SMILES:	C1=C(S(=O)(=O)C(C)(C)C)C(OCCO)=CC2N=CN=C(NC3=CC4N=CSC=4C=C3)C1=2
Formula:	C₂₁H₂₂N₄O₄S₂
M.Wt:	458.55
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[1]. Linda N. Casillas, et al. Prodrugs of amino quinazoline kinase inhibitor. PCT Int. Appl. (2014), WO 2014043446 A1 20140320.

Description:

GSK2983559 active metabolite is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043446 A1, compound example 1.

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[1].

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC73134	GNE-684	GNE-684 is a potent, cross-species, specific RIP1 kinase (RIPK1) inhibitor with IC50 of 21, 189 and 691 nM for human, mouse and rat RIP1, respectively.
DC73130	AC-003	AC-003 is a novel, orally administered small-molecule inhibitor targeting receptor-interacting protein kinase 1 (RIPK1), demonstrating therapeutic potential for the treatment of idiopathic pulmonary fibrosis (IPF).
DC70698	PK68	PK68 (RIPK1 inhibitor PK68) is a potent necroptosis inhibitor seletively targeting RIPK1 kinase activity, potently inhibits TNF-induced necroptosis (EC50, 23 and 13 nM in human and mouse cells, respectively).PK68 blocks cellular activation of RIPK1, RIPK3, and MLKL upon necroptotic stimuli.PK68 is a type II inhibitor of RIP1 kinase, highly selective inhibitor of RIPK1 kinase activity with IC50 of 90 nM, does not affect RIPK3 kinase activity at 1 uM, also demonstrated a reasonable selectivity against a panel of 369 kinases.PK68 exhibits a favorable pharmacokinetic profile and no obvious toxicity in mice.PK68 ameliorates TNF-induced systemic inflammatory response syndrome, and displays preventive suppression of tumor metastasis in the mouse cancer models.
DC70652	Nigratine	Nigratine (6E11) is a highly specific, non-ATP competitive inhibitor of RIPK1 kinase (IC50=1.6 uM), inhibits necroptosis and ferroptosis.Nigratine inhibits necroptotic cell-death induced by TNF-α in Jurkat-Fadd def cells with IC50 of 4.6 uM.Nigratine is significantly more potent than the specific RIPK1 necroptosis inhibitor, Nec-1s.Nigratine (50 uM) strongly inhibits the ferroptotic cell death induced by excess of glutamate, erastin, and RSL3, in both murine HT22 and human SH-SY5Y cell lines, protects SH-SY5Y human neuroblastoma cell line from cell death triggered by both class I and II-inducers of ferroptosis.Nigratine protects porcine kidney epithelial LLC-PK1 cell line from lipid peroxidation and cell death triggered by RSL3.Nigratine protects human bronchial organoids from necroptosis and ferroptosis.
DC45531	ICCB-19 hydrochloride	ICCB-19 hydrochloride is an inhibitor of TNFRSF1A Associated Via Death Domain (TRADD) with IC50 of 1.12 μM and 2.01 μM for protecting Velcade-induced apoptosis in Jurkat cells and protecting RDA in MEFs, respectively. ICCB-19 indirectly inhibits Receptor-interacting serine/threonine-protein kinase 1 (RIPK1). ICCB-19 effectively induces autophagy.
DC10389	RIPA-56	RIPA-56 is a highly potent, selective, and metabolically stable inhibitor of receptor-interacting protein 1 (RIP1) with an IC50 of 13 nM.
DC9721	GSK2983559 active metabolite	GSK2983559 active metabolite is an active metabolite of GSK2983559. GSK2983559 active metabolite is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043446 A1, compound example 1.