GSK-J5 is a cell-permeable, inactive control for histone demethylase JMJD3/UTX inhibitor GSK-J4. Like GSK-J4, this isomer is cell-permeable and hydrolyzed to a free base.3 However, the free base is a weak inhibitor of JMJD3 (IC50 > 100 μM), making it an ideal inactive control molecule for elucidating the functional role of JMJD3 inhibition.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO ≥ 25 mg/mL|
|Storage||2-8°C, dry, protect from light, sealed|
A Selective Jumonji H3K27 Demethylase Inhibitor Modulates the Proinflammatory Macrophage Response.
Kruidenier L, et al. Nature. 2012 Aug 16;488(7411):404-8. PMID: 22842901.
UTX and JMJD3 Are Histone H3K27 Demethylases Involved in HOX Gene Regulation and Development.
Agger K, et al. Nature. 2007 Oct 11;449(7163):731-4. PMID: 17713478.
|Related Histone demethylases Products|
Seclidemstat is an orally active, reversible, noncompetitive inhibitor of lysine-specific demethylase 1 (LSD1, or KDM1A) with a mean IC50 of 127 nM, it has potential antineoplastic activity.
T-3775440 hydrochloride is a potent, selecitve, irreversible LSD1 inhibitor with IC50 value of 2.1 nM.
QC6352 is a potent KDM4C inhibitor.
CPI-455 HCl is a potent and selective inhibitor of KDM5 demethylases which reduces survival of drug-tolerant cancer cells, with a half-maximal inhibitory concentration (IC50) of 10 ± 1 nM for full-length KDM5A in enzymatic assays.
IOX1 is a histone demethylase inhibitor; cell permeable. IOX1 also inhibits ALKBH5.
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