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TC-H 106

Cat. No. M7374
TC-H 106 Structure
Synonym:

RGFA-8; Histone Deacetylase Inhibitor VII

Size Price Availability Quantity
10mg USD 80  USD80 In stock
25mg USD 130  USD130 In stock
50mg USD 220  USD220 In stock
100mg USD 400  USD400 In stock
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Quality Control & Documentation
Biological Activity

TC-H 106 is a class I histone deacetylase (HDAC) inhibitor (IC50 values are 150, 370, 760 and 5000 nM for HDAC1, HDAC3, HDAC2 and HDAC8 respectively). TC-H 106 exhibits slow, tight-binding inhibitory activity. TC-H 106 displays no activity against class II HDACs. Brain penetrant.

Chemical Information
Molecular Weight 339.43
Formula C20H25N3O2
CAS Number 937039-45-7
Solubility (25°C) DMSO 25 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] Maria Beconi, et al. PLoS One. Oral administration of the pimelic diphenylamide HDAC inhibitor HDACi 4b is unsuitable for chronic inhibition of HDAC activity in the CNS in vivo

[2] Anindita Chakrabarty, et al. Proc Natl Acad Sci U S A. Feedback upregulation of HER3 (ErbB3) expression and activity attenuates antitumor effect of PI3K inhibitors

[3] Chunping Xu, et al. Chem Biol. Chemical probes identify a role for histone deacetylase 3 in Friedreichs ataxia gene silencing

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Keywords: TC-H 106, RGFA-8; Histone Deacetylase Inhibitor VII supplier, HDAC, inhibitors, activators


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