| Bioactivity | KH-259 (compound 1) is a potent, selective and CNS-penetrant HDAC6 inhibitor, with an IC50 of 0.26 μM. KH-259 has antidepressant effects in mice through the inhibition of HDAC6 in the brain. KH-259 can be used for neurodegenerative diseases research[1]. |
| Invitro | KH-259 (compound 1) exhibits acceptable metabolic stability in both mouse and human liver microsomes[1]. |
| In Vivo | KH-259 (compound 1) (10 mg/kg, IP, once) in mice significantly increases acetylated α-tubulin levels without increasing acetylated histone H3K9 levels in the brain, indicating that KH-259 has antidepressant effects in mice through the inhibition of HDAC6 in the brain[1]. |
| Name | KH-259 |
| Formula | C20H25N3O2 |
| Molar Mass | 339.43 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Kosuke Hashimoto, et al. Discovery of Benzylpiperazine Derivatives as CNS-Penetrant and Selective Histone Deacetylase 6 Inhibitors. ACS Med. Chem. Lett. 2022 June 28. |