WT161

Catalog No.S8495

For research use only.

WT161 is a potent, selective, and bioavailable HDAC6 inhibitor with IC50 values of 0.4 nM, 8.35 nM and 15.4 nM for HDAC6, HDAC1 and HDAC2, respectively; shown to have >100-fold selectivity over other HDACs. WT161 induces apoptosis.

WT161 Chemical Structure

CAS No. 1206731-57-8

Selleck's WT161 has been cited by 2 Publications

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Biological Activity

Description WT161 is a potent, selective, and bioavailable HDAC6 inhibitor with IC50 values of 0.4 nM, 8.35 nM and 15.4 nM for HDAC6, HDAC1 and HDAC2, respectively; shown to have >100-fold selectivity over other HDACs. WT161 induces apoptosis.
Targets
HDAC6 [1]
(Cell-free assay)
HDAC1 [1]
(Cell-free assay)
HDAC2 [1]
(Cell-free assay)
0.4 nM 8.35 nM 15.4 nM
In vitro

WT161 selectively inhibits HDAC6 and dramatically increases levels of acetylated α-tubulin (Ac-α-tubulin) with little effect on global lysine acetylation. It induces accumulation of acetylated tubulin and cytotoxicity in multiple myeloma (MM) cells. WT161 as a single agent does not induce ER stress, the UPR, or ER stress-mediated apoptosis[1]. Consistent with WT-161 mediated hyperacetylation and inhibition of hsp90 chaperone function, treatment with WT-161 increases the intracellular levels of polyubiuitylated proteins in the cultured MCL JeKo-1 and Z138 cells. WT-161 also dose-dependently depletes the levels of cyclin D1 in the cultured human Mantle Cell Lymphoma (MCL) cells. Treatment with WT-161 induces ER stress response in the MCL cells, demonstrated by increase in the protein levels of Glucose regulated protein (GRP) 78, phosphorylated eIF2 (eukaryotic initation factor 2) α, and induction of the pro-apoptotic transcription factor CHOP (CAAT/Enhancer Binding Protein Homologous Protein)[2]. WT161 triggers apoptotic cell death in MCF7, T47D, BT474, and MDA-MB231 cells, associated with decreased expression of EGFR, HER2, and ERα and downstream signaling[3].

In vivo

WT161 has reasonable half-life in mice (1.4 h) and drug exposure [maximum concentration (Cmax) = 18 mg/L]. It is well tolerated as a single agent[1]. WT161 significantly inhibits in vivo MCF7 cell growth, associated with downregulation of ERα, in a murine xenograft model[3].

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: MM.1S cells 
  • Concentrations: 3 µM
  • Incubation Time: 16 h
  • Method:

    For annexin V-PI staining, MM.1S cells cultured for 16 h with BTZ (3 nM) and/or tubacin/WT161 (3 µM) are washed with PBS and processed.

Animal Research:

[3]

  • Animal Models: Female NCr nu/nu mice subcutaneously (sc) implanted with 17β-estradiol-sustained release pellets and inoculated s.c. with 5 × 106 MCF-7 cells suspended in 30% Matrigel
  • Dosages: 80 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 458.55
Formula

C27H30N4O3

CAS No. 1206731-57-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C=C1)N(C2=CC=CC=C2)C3=CC=C(C=C3)C=NNC(=O)CCCCCCC(=O)NO

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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