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TH34

Cat. No. M20644
TH34 Structure
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Biological Activity

TH34 is a HDAC inhibitor that shows pronounced selectivity for HDACs 6, 8 and 10 over HDACs 1, 2 and 3. In a NanoBRET assay, TH34 strongly binds HDAC6, 8 and 10 with low-micromolar IC50 concentrations (HDAC6: 4.6 µM, HDAC8: 1.9 µM, HDAC10: 7.7 µM).

Chemical Information
Molecular Weight 256.30
Formula C15H16N2O2
CAS Number 2196203-96-8
Solubility (25°C) DMSO 51 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Anna Raunio, et al. Acta Neuropathol Commun. Distribution of Lewy-related pathology in the brain, spinal cord, and periphery: the population-based Vantaa 85 + study

[2] Eftiola Pojani, et al. Curr Med Chem. Selective Inhibitors of Histone Deacetylase 10 (HDAC-10)

[3] Fiona R Kolbinger, et al. Arch Toxicol. The HDAC6/8/10 inhibitor TH34 induces DNA damage-mediated cell death in human high-grade neuroblastoma cell lines

[4] M V Merculov, et al. Zh Nevrol Psikhiatr Im S S Korsakova. [New possibilities to increase the results of posttraumatic nerve regeneration with sympathectomy]

[5] T Matsumura, et al. Rinsho Shinkeigaku. [A case of idiopathic spinal cord herniation]

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