1. Cell Cycle/DNA Damage
    Apoptosis
    Epigenetics
  2. HDAC
    Apoptosis
  3. WT-161

WT-161 

Cat. No.: HY-100871 Purity: 98.52%
Handling Instructions

WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM.

For research use only. We do not sell to patients.

WT-161 Chemical Structure

WT-161 Chemical Structure

CAS No. : 1206731-57-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 96 In-stock
Estimated Time of Arrival: December 31
5 mg USD 95 In-stock
Estimated Time of Arrival: December 31
10 mg USD 160 In-stock
Estimated Time of Arrival: December 31
25 mg USD 250 In-stock
Estimated Time of Arrival: December 31
50 mg USD 396 In-stock
Estimated Time of Arrival: December 31
100 mg USD 594 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM.

IC50 & Target

HDAC6

0.4 nM (IC50)

HDAC1

8.35 nM (IC50)

HDAC2

15.4 nM (IC50)

HDAC3

51.6 nM (IC50)

HDAC8

1430 nM (IC50)

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[1].

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[1].

Molecular Weight

458.55

Formula

C₂₇H₃₀N₄O₃

CAS No.

1206731-57-8

SMILES

O=C(N/N=C/C1=CC=C(N(C2=CC=CC=C2)C3=CC=CC=C3)C=C1)CCCCCCC(NO)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (218.08 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1808 mL 10.9039 mL 21.8079 mL
5 mM 0.4362 mL 2.1808 mL 4.3616 mL
10 mM 0.2181 mL 1.0904 mL 2.1808 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.45 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.45 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.45 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

MM.1S cells are treated with increasing concentrations of WT161 (0-10 μM) for 48 hours. Cell viability is determined using the MTT assay[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: Mice tumor xenograft are assigned into cohorts receiving vehicle (control), BTZ (0.5 mg/kg, i.v.), WT161 (50 mg/kg, i.p.), or BTZ+WT161. WT161 is administered for five consecutive days each week, and BTZ is given on a twice-weekly schedule. Caliper measurements of the longest perpendicular tumor diameters are performed on alternate days to estimate the tumor volume[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

WT-161WT161WT 161HDACApoptosisHistone deacetylasesInhibitorinhibitorinhibit

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WT-161
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