| Identification | Back Directory | [Name]
HDAC-IN-67 | [CAS]
2821923-75-3 | [Synonyms]
HDAC-IN-67
1-Piperazineoctanamide, 4-[2-[(1R,3R,4S)-4-ethenyl-4-methyl-3-[1-(1H-pyrazol-1-ylmethyl)ethenyl]cyclohexyl]-2-propen-1-yl]-N-hydroxy-η-oxo- | [Molecular Formula]
C30H47N5O3 | [MOL File]
2821923-75-3.mol | [Molecular Weight]
525.73 |
| Hazard Information | Back Directory | [Uses]
HDAC-IN-67 (compound 27f) is an HDAC inhibitor against HDAC1 and HDAC6, with IC50 values of 22 nM and 8 nM, respectively. HDAC-IN-67 inhibits cell proliferation and induces cell apoptosis. HDAC-IN-67 exhibits antitumor activity[1]. | [in vivo]
HDAC-IN-67 (i.v.:50 mg/kg) reveals a clearance (CL) of 65.1 ml/(h·kg) and a half-life (T1/2) of 0.361 h after i.v.[1].
HDAC-IN-67 (p.o.:10 mg/kg) exhibits low oral bioavailability(F=3.15%)[1].
HDAC-IN-67 (i.p.:50mg/kg once daily for 21 days) demonstrates a moderate in vivo antitumor potency with TGI of 31.5%[1]. | Animal Model: | Female ICR mice/antitumour potency[1] | | Dosage: | i.p., 50 mg/kg once a day for 21 days | | Administration: | Intraperitoneal injection (i.p.) | | Result: | Exhibited in vivo antitumorpotency with TGI of 31.5%. |
| [IC 50]
HDAC6: 8 nM (IC50); HDAC1: 22 nM (IC50) | [References]
[1] Gao Y,et al., Design, synthesis and biological evaluation of novel histone deacetylase (HDAC) inhibitors derived from β-elemene scaffold. J Enzyme Inhib Med Chem. 2023 Dec;38(1):2195991. DOI:10.1080/14756366.2023.2195991 |
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