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.
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
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.
Molecular Weight | 417.5 |
Formula | C24H27N5O2 |
CAS Number | 1394854-51-3 |
Purity | >98% |
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
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
T-3775440 hydrochloride is a potent, selecitve, irreversible LSD1 inhibitor with IC50 value of 2.1 nM. |
QC6352
QC6352 is a potent KDM4C inhibitor. |
CPI-455 HCl
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
IOX1 is a histone demethylase inhibitor; cell permeable. IOX1 also inhibits ALKBH5. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.