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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 |
|---|
| 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. |
| Daminozide
Daminozide is a selective KDM2/7 inhibitor. |
| CP2
CP2 is a cyclic peptide that inhibits the JmjC histone demethylases KDM4 with IC50 values of 42 nM and 29 nM for KDM4A and KDM4C, respectively. |
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