Vergleich

GSK2593074A

ArtNr V3532-5mg
Hersteller InvivoChem LLC
CAS-Nr. 1337531-06-2
Menge 5 mg
Quantity options 100 mg 10 mg 250 mg 25 mg 50 mg
Kategorie
Typ Biochemicals
Specific against other
ECLASS 10.1 32160490
ECLASS 11.0 32160490
UNSPSC 12000000
Alias 1337531-06-2
Lieferbar
Description
InvivoChem Cat #:V3532CAS #:1337531-06-2Purity >=98%

Description: GSK2593074A (also known as GSK’074) is a novel and potent necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3. GSK2593074A displayed structural similarity to the established RIP3 inhibitor GSK'843. In multiple cell types including mouse SMCs, fibroblasts (L929), bone marrow derived macrophages (BMDM), and human colon epithelial cells (HT29), GSK'074 inhibited necroptosis with an IC50 of ca.3?nM. Furthermore, GSK'074, but not Nec-1s, blocked cytokine production by SMCs. Biochemical analyses identified both RIP1 and RIP3 as the biological targets of GSK'074. Unlike GSK'843 which causes profound apoptosis at high doses (> 3?uM), GSK'074 showed no detectable cytotoxicity even at 20?uM. Daily intraperitoneal injection of GSK'074 at 0.93?mg/kg significantly attenuated aortic expansion in two mouse models of AAA (calcium phosphate: DMSO 66.06?+/-?9.17% vs GSK'074 27.36?+/-?8.25%, P?< ?0.05; Angiotensin II: DMSO 85.39?+/-?15.76% vs GSK'074 36.28?+/-?5.76%, P?< ?0.05). Histologically, GSK'074 treatment diminished cell death and macrophage infiltration in aneurysm-prone aortae. GSK'074 represents a new class of necroptosis inhibitors with dual targeting ability to both RIP1 and RIP3. The high potency and minimum cytotoxicity make GSK'074 a desirable drug candidate of pharmacological therapies to attenuate AAA progression and other necroptosis related diseases.

References: 2019 Mar 6; 10(3):226.

GSK2593074A

Molecular Weight: 465.57
Formula: C??H??N?OS
CAS No.: 1337531-06-2
SMILES: CN1N=CC(C2=CN=C(N)C3=C2SC=C3C4=CC5=C(N(C(CC6=CC=CC=C6)=O)CC5)C=C4)=C1
Storage
-20C for 3 years in powder form
-80C for 2 years in solvent
Technical Information
GSK2593074A; GSK'074; GSK-2593074A; GSK 074; GSK 2593074A; GSK-074;

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Alle Produkte sind nur für Forschungszwecke bestimmt. Nicht für den menschlichen, tierärztlichen oder therapeutischen Gebrauch.

Menge: 5 mg
Lieferbar: In stock
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