[CAS NO. ] GSK2983559

Name: GSK2983559
Brand: Arctom Scientific
SKU: HY-112038A

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PRODUCTS SPECIFICATIONS

Distributor

Catalog

HY-112038A

Brand

MCE

CAS

-

DESCRIPTION

Overview

MDL	-
Molecular Weight	611.61
Molecular Formula	C21H28CaN4O10PS2+
SMILES	CC(C)(C)S(C(C(OCCOP(O)([O-])=O)=CC1=NC=N2)=CC1=C2NC3=CC(N=CS4)=C4C=C3)(=O)=O.[H]O[H].[H]O[H].[H]O[H].[Ca+2].[1/2]

For research use only. We do not sell to patients.

Summary

GSK2983559 is an orally active and potent receptor interacting protein 2 ( RIP2 ) kinase inhibitor. GSK2983559 blocks many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples ^[1] .

IC50 & Target

RIPK2

In Vitro

GSK2983559 (1-1024 nM; 2 h) blocks MDP-induced IL-8 in THP-1 cells ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay ^[2]

Cell Line:	THP-1 cells
Concentration:	1-1024 nM
Incubation Time:	2 hours
Result:	Inhibited IL-8 production with an IC ₅₀ of 1.34 nM.

In Vivo

GSK2983559 (oral gavage; 3 and 10 mg/kg; once) inhibits effectively MDP-induced IL-6 in mouse ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL/6 mice (female) injected with MDP (100 μg) ^[2]
Dosage:	3 and 10 mg/kg
Administration:	Oral gavage; 3 and 10 mg/kg; once
Result:	Suppressed serum IL-6 levels in a dose-dependent manner.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03358407	GlaxoSmithKline	Inflammatory Bowel Diseases	January 11, 2018	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H ₂ O : 2 mg/mL ( 3.27 mM ; Need ultrasonic)

DMSO : < 1 mg/mL (ultrasonic;warming;heat to 80°C) (insoluble or slightly soluble)

DMF : < 1 mg/mL (ultrasonic;warming;heat to 80°C) (insoluble)

Ethanol : < 1 mg/mL (ultrasonic) (insoluble)

* GSK2983559 is usually formulated as a suspension.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6350 mL	8.1751 mL	16.3503 mL
5 mM	---	---	---
10 mM	---	---	---

* Please refer to the solubility information to select the appropriate solvent.