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WT161

Cat. No. M6073
WT161 Structure
Synonym:

WT 161

Size Price Availability Quantity
5mg USD 110 In stock
10mg USD 195 In stock
25mg USD 415 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

In vitro: WT161 selectively inhibits HDAC6 and dramatically increases levels of acetylated α-tubulin (Ac-α-tubulin) with little effect on global lysine acetylation. WT161 induces significant toxicity in all multiple myeloma cell lines tested, with IC50s between 1.5 and 4.7 μM . WT161 in combination with bortezomib triggers significant accumulation of polyubiquitinated proteins and cell stress, followed by caspase activation and apoptosis. More importantly, this combination treatment is effective in bortezomib-resistant cells and in the presence of bone marrow stromal cells, which have been shown to mediate multiple myeloma cell drug resistance. In vivo: WT161 shows toxicity at 100 mg/kg i.p., but WT161 is well tolerated at 50 mg/kg i.p.. Bortezomib combined with WT161 demonstrates a significant antitumor effect.

Protocol
Cell Experiment
Cell lines MM cells
Preparation method Cells cultured with WT161, BTZ, and CFZ were harvested, washed, and lysed using lysis buffer, and complete protease inhibitor mixture.
Concentrations 1 µM
Incubation time 6 h
Animal Experiment
Animal models mice
Formulation
Dosages 50–100 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 458.55
Formula C27H30N4O3
CAS Number 1206731-57-8
Purity >99%
Solubility 100 mg/mL in DMSO
Storage at -20°C
References

Discovery of selective small-molecule HDAC6 inhibitor for overcoming proteasome inhibitor resistance in multiple myeloma.
Hideshima T, et al. Proc Natl Acad Sci U S A. 2016 Nov 15;113(46):13162-13167. PMID: 27799547.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: WT161, WT 161 supplier, HDAC, inhibitors

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