GSK2593074A - 98%, high purity , CAS No.1337531-06-2

  • ≥98%
Item Number
G651840
Grouped product items
SKUSizeAvailabilityPrice Qty
G651840-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$350.90
G651840-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$550.90
G651840-50mg
50mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,650.90
G651840-100mg
100mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$2,250.90
View related series
Apoptosis RIP kinase

Basic Description

Specifications & Purity≥98%
Biochemical and Physiological MechanismsGSK2593074A (GSK’074) is a necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
Product Description

GSK2593074A (GSK’074) is a necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3

In Vitro

GSK2593074A (GSK’074; 0.01, 0.1, 1, 10, and 100 nM; 6 hours for MOVAS cells; 3 hours for L929 cells) completely rescues cells from necroptosis under different stimuli in both human and murine cells at IC 50 ~3 nM. In multiple cell types including mouse SMCs, fibroblasts (L929), bone marrow derived macrophages (BMDM), and human colon epithelial cells (HT29), GSK2593074A inhibits necroptosis with an IC 50 of ~3 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Mouse smooth muscle cell line MOVAS; Mouse fibroblast cell line L929 Concentration: 0.01, 0.1, 1, 10, and 100 nM Incubation Time: 6 hours for MOVAS cells; 3 hours for L929 cells Result: Inhibited MOVAS and L929 cells with the IC 50 of 3 nM.

In Vivo

GSK2593074A (GSK’074; 0.93 mg/kg/day; i.p. injection; 14 or 28 days) is administrated to Apoe -/- mice immediately following pump implantation. Compared to the DMSO group, GSK2593074A-treated mice show significantly alleviated aneurysm formation, reflected by a much smaller aortic dilatation (DMSO 85.39±15.76% vs GSK2593074A 36.28±5.76%; P<0.05) as well as a reduced abdominal aortic aneurysm (AAA) incidence (from 83.3 to 16.7%). GSK2593074A significantly decreases the extent of aortic expansion (DMSO 66.06±9.17% vs GSK2593074A 27.36±8.25%; P<0.05) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Apoe -/- female mice (9-10 months) Dosage: 0.93 mg/kg/day; 200 µL Administration: Daily i.p. injection; 14 or 28 days Result: Inhibited aneurysm formation in mouse models of aneurysms.

Form:Solid

IC50& Target:RIP1, RIP3

Associated Targets(Human)

EIF2AK3 Tchem Eukaryotic translation initiation factor 2-alpha kinase 3 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
NEK2 Tchem Serine/threonine-protein kinase NEK2 (3514 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NEK9 Tchem Serine/threonine-protein kinase NEK9 (1479 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NEK6 Tchem Serine/threonine-protein kinase NEK6 (1986 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NEK7 Tchem Serine/threonine-protein kinase NEK7 (1804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NEK5 Tchem Serine/threonine-protein kinase Nek5 (349 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EIF2AK2 Tchem Interferon-induced, double-stranded RNA-activated protein kinase (504 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NEK4 Tchem Serine/threonine-protein kinase Nek4 (980 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NEK1 Tchem Serine/threonine-protein kinase Nek1 (1886 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NEK3 Tchem Serine/threonine-protein kinase Nek3 (902 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NEK11 Tchem Serine/threonine-protein kinase Nek11 (645 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EIF2AK1 Tchem Eukaryotic translation initiation factor 2-alpha kinase 1 (688 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EIF2AK3 Tchem Eukaryotic translation initiation factor 2-alpha kinase 3 (635 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NEK10 Tchem Serine/threonine-protein kinase Nek10 (176 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

L929 (3802 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 1-[5-[4-amino-7-(1-methylpyrazol-4-yl)thieno[3,2-c]pyridin-3-yl]-2,3-dihydroindol-1-yl]-2-phenylethanone
INCHI InChI=1S/C27H23N5OS/c1-31-15-20(13-30-31)21-14-29-27(28)25-22(16-34-26(21)25)18-7-8-23-19(12-18)9-10-32(23)24(33)11-17-5-3-2-4-6-17/h2-8,12-16H,9-11H2,1H3,(H2,28,29)
InChi Key LIGGMBSSOOVGAE-UHFFFAOYSA-N
Canonical SMILES CN1C=C(C=N1)C2=CN=C(C3=C2SC=C3C4=CC5=C(C=C4)N(CC5)C(=O)CC6=CC=CC=C6)N
Isomeric SMILES CN1C=C(C=N1)C2=CN=C(C3=C2SC=C3C4=CC5=C(C=C4)N(CC5)C(=O)CC6=CC=CC=C6)N
PubChem CID 53466951
Molecular Weight 465.57

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilityDMSO : 41.67 mg/mL (89.50 mM; Need ultrasonic)

Related Documents

Solution Calculators