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Tenovin 6 Hydrochloride

Cat. No. M6241
Tenovin 6 Hydrochloride Structure
Synonym:

Tenovin 2

Size Price Availability Quantity
10mM/1mL In DMSO USD 240 In stock
5mg USD 220 In stock
10mg USD 350 In stock
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Quality Control
Biological Activity

In vitro: Tenovin-6 inhibits the growth of S. cerevisiae cultures with an IC50 of 30 μM and is more toxic to yeast than the less water-soluble tenovin-1. Tenovin-6 rapidly increases the levels of endogenous K382-Ac p53 in MCF-7 cells. Tenovin-6 (0 to 15 μM) dose dependently increases the level of LC3-II in diverse cell types, and the increase is ATG5/7 dependent. Tenovin-6 treatment also increases the number and intensity of autophagic vesicles with or without the presence of Torin 1, and prevents Torin 1-induced SQSTM1/p62 degradation. Tenovin-6 affects the acidification of autolysosomes and impairs the hydrolytic activity of lysosomes but does not affect the fusion between autophagosomes and lysosomes. That tenovin-6 inhibits autophagy does not correlate with p53 activation and SIRT1/2 inhibition by knockdown or knockout cannot mimic the effect of tenovin-6 on LC3B accumulation. Tenovin-6 (0, 1, 2.5, 5 or 10 μM) potently inhibits cell proliferation in a dose- and time-dependent manner in all OCI-Ly1, DHL-10, U2932, RIVA, HBL1 and OCI-Ly10 cell lines. Tenovin-6 consistently increases LC3B-II level in DLBCL cell lines by inhibiting the classical autophagy pathway, without activating p53, and the increase is independent of SIRT1/2/3 and p53. Tenovin-6 induces apoptosis through the extrinsic cell-death pathway. Tenovin-6 suppresses the growth of UM cells with IC50 of 12.8 μM, 11.0 μM, 14.58 μM and 9.62 μM for 92.1, Mel 270, Omm 1 and Omm 2.3 cells, respectively.

In vivo: Tenovin-6 (50 mg/kg, i.p.) inhibits the growth of tumor in mice.

Protocol
Cell Experiment
Cell lines UM cells
Preparation method UM cells are seeded into each well of 96-well plates (5,000 cells/well) and treated the next day with control or Tenovin-6 in an increasing concentrations from 0 to 20 μM for 68 h, and then MTS is added at 20 μL/well to be read at a wave length of 490 nm, the IC50 is determined by curve fitting of the sigmoidal dose-response curve.
Concentrations 0 to 20 μM
Incubation time 68 h
Animal Experiment
Animal models SCID mice
Formulation cyclodextrin 20% (w/v) and DMSO 10% (v/v)
Dosages 50 mg/kg
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 491.09
Formula C25H35ClN4O2S
CAS Number 1011301-29-3
Purity 99.66%
Solubility 49 mg/mL in DMSO
Storage at -20°C
References

Tenovin-6 impairs autophagy by inhibiting autophagic flux.
Yuan H, et al. Cell Death Dis. 2017 Feb 9;8(2):e2608. PMID: 28182004.

Class III-specific HDAC inhibitor Tenovin-6 induces apoptosis, suppresses migration and eliminates cancer stem cells in uveal melanoma.
Dai W, et al. Sci Rep. 2016 Mar 4;6:22622. PMID: 26940009.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Tenovin 6 Hydrochloride, Tenovin 2 supplier, inhibitors

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