KDM5-IN-1

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Menge 10mM*1mL (in DMSO)
ArtNr HY-100422-10mM
eClass 6.1 30220300
eClass 9.0 32160605
Lieferbar
CAS No.
1628210-26-3
Purity
>98%
MW
3243803
Formula
C17H20N6O
Solubility
DMSO: >= 30 mg/mL
Biological Description
KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.
IC50 & Target: IC50: 15.1 nM (KDM5); EC50: 0.34 uM (PC9 H3K4Me3)[1]
In Vitro: KDM5-IN-1 is found to potently inhibit KDM5B and KDM5C isoforms (IC50 of 4.7 and 65.5 nM, respectively). It is significantly less potent against other KDM enzymes (1A, 2B, 3B, 4C, 5A, 6A, 7B), inhibiting KDM4C the strongest with an IC50 of 1.9 uM. KDM5-IN-1 still displays more than 100-fold selectivity for KDM4C vs. KDM5A[1].
In Vivo: When dosed orally in mice at 50 mg/kg twice a day, KDM5-IN-1 shows an unbound maximal plasma concentration Cmax>15-fold over its cell EC50, thereby providing a robust chemical probe for studying KDM5 biological functions in vivo[1].
Menge: 10mM*1mL (in DMSO)
Lieferbar: In stock
Listenpreis: 326,43 €
Preis: 326,43 €
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