(+)-JQ-1

Hersteller MedChem Express
Kategorie Produkte / Inhibitors
Typ Inhibitors
Specific against other
Clon N/A
Menge 10mg
ArtNr HY-13030-10mg
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
Synonyms
JQ-1, JQ1
CAS No.
1268524-70-4
Purity
>98%
MW
4569882
Formula
C23H25ClN4O2S
Solubility
DMSO: >= 45 mg/mL
Biological Description
(+)-JQ-1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for the first and second bromodomain (BRD4(1/2)).
IC50 & Target: IC50: 77/33 nM (BRD4(1/2))[1]
In Vitro: (+)-JQ1 represents a potent, highly specific and Kac competitive inhibitor for the BET family of bromodomains. (+)-JQ1 (100 nM, 48 h) prompts squamous differentiation exhibited by cell spindling, flattening and increased expression of keratin. (+)-JQ1 (250 nM) induces rapid expression of keratin in treated NMC 797 cells compared to (-)-JQ1 (250 nM) and vehicle controls, as determined by quantitative immunohistochemistry.(+)-JQ1 (250 nM) elicits a time-dependent induction of strong (3+) keratin staining of treated NMC 797 cells, compared to (-)-JQ1 (250 nM)[1]. (+)-JQ1 is a potent thienodiazepine inhibitor (Kd=90 nM) of the BET family coactivator protein BRD4, which is implicated in the pathogenesis of cancer via transcriptional control of the MYC oncogene. Dose-ranging studies of (+)-JQ1 demonstrates potent inhibition of H4Kac4 binding with a IC50 value of 10 nM for murine BRDT(1) and 11 nM for human BRDT(1)[2].
In Vivo: Pharmacokinetic studies of (+)-JQ1 are performed in CD1 mice following intravenous and oral administration. Mean plasma concentration-time profiles of (+)-JQ1 after intravenous dosing (5 mg/kg). The pharmacokinetic parameters for intravenous (+)-JQ1 demonstrate excellent drug exposure (AUC=2090 hr*ng/mL) and an approximately one hour half-life (T1/2). Mean plasma concentration-time profiles of (+)-JQ1 after oral dosing (10 mg/kg). The pharmacokinetic parameters for oral (+)-JQ1 demonstrate excellent oral bioavailability (F=49%), peak plasma concentration (Cmax=1180 ng/mL) and drug exposure (AUC=2090 hr*ng/mL)[1].
Publications
J Cell Biochem. 2017 Jan 6.
Nat Chem Biol. 2016 Jul; 12(7):504-10.
Mol Cancer Ther. 2016 Jun; 15(6):1217-26.
Biochim Biophys Acta. 2016 Dec; 1859(12):1527-1537.
PLoS Pathog. 2016 Oct 20; 12(10):e1005950.
ACS Chem Biol. 2015 Aug 21; 10(8):1770-7.
Metabolism. 2016 Oct; 65(10):1478-88.
J Biol Chem. 2016 Nov 4; 291(45):23756-23768.
Free  Sample
Available in quantities of 0, 5mg-1mg. Three different samples per customer per year!
Menge: 10mg
Lieferbar: In stock
Listenpreis: 155,00 €
Preis: 155,00 €
lieferbar

Angebot anfordern

Technische Fragen zu diesem Produkt?


Salesmanager: Arne Pelz

Email: sales@hoelzel.de

Schließen