MRT67307

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Clon N/A
Menge 10mg
ArtNr HY-13018-10mg
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
Synonyms
MRT 67307, MRT-67307
CAS No.
1190378-57-4
Purity
>98%
MW
464603
Formula
C26H36N6O2
Solubility
10 mM in DMSO
Biological Description
MRT67307 is a dual inhibitor of the IKKepsilon and TBK-1, which mediates the phosphorylation of interferon regulatory factor 3 (IRF3), with IC50 values of 160 and 19 nM when assayed at 0.1 mM ATP in vitro, and also targets ULK1 and ULK2 with high potency (IC50 values of 45 and 38 nm, respectively).
IC50 & Target: IC50: 160 nM (IKKepsilon, ATP), 19 nM (TBK-1, ATP), 45 nM (ULK1), 38 nM (ULK2)
In Vitro: MRT67307 actually enhances phosphorylation in IKKalpha?/? MEFs, the IL-1-stimulated phosphorylation of p105 at Ser933 and RelA at both Ser468 and Ser536. MRT67307 also enhances IL-1-stimulated activation of NF-kappaB-dependent gene transcription in wild-type MEFs. Treatment of macrophages with MRT67307 leads to an increase in the poly(I:C)- and LPS-stimulated phosphorylation of p105 and RelA and enhanced NF-kappaB transcriptional activity[1]. MRT67307 (10 uM) is sufficient to reduce phospho-ATG13 to control levels, and in line with the in vitro IC50 values, 10-fold less MRT68921 (1 uM) results in a similar reduction. MRT67307 and MRT68921 inhibit ULK and block autophagy in cells[2]. MRT67307 increases IL-10 production and suppresses proinflammatory cytokine production in macrophages. MRT67307 increases CREB-dependent gene transcription by promoting the dephosphorylation of CRTC3. MRT67307 does not inhibit the brain-specific kinases (BRSKs) and only inhibits the maternal embryonic leucine zipper kinase (MELK) and AMPK itself more weakly[3].
Publications
Nat Commun. 2015 Jan 21; 6:6074.
Patent. US 20150202223 A1.
Free  Sample
Available in quantities of 0, 5mg-1mg. Three different samples per customer per year!

Sicherheitsdatenblatt

HY-13018-10mg.pdf

Menge: 10mg
Lieferbar: In stock
Listenpreis: 202,14 €
Rabatt: -10,0%
Preis: 181,93 €
Sie sparen: 20,21 €
lieferbar

Angebot anfordern

Fragen zum Produkt?

Ihr Ansprechpartner:

Arne Pelz

sales@hoelzel.de

 
Schließen