WT-161
Based on 10 publication(s) in Google Scholar
WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM. WT-161 also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.04%
- No. CAS: 1206731-57-8
- Fòrmula: C27H30N4O3
- Peso molecular:458.55
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
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Publications Citing Use of MedChemExpress (MCE) WT-161
More- Cell Death Dis. 2023 Apr 6;14(4):250. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- Sci Rep. 2025 Nov 17;15(1):40178. [Abstract]
- Biosci Rep. 2021 Apr 30;41(4):BSR20203905. [Abstract]
- Invest New Drugs. 2025 Apr;43(2):223-242. [Abstract]
- J Appl Toxicol. 2023 Aug;43(8):1214-1224. [Abstract]
- Cancer Chemother Pharmacol. 2025 Jan 17;95(1):22. [Abstract]
- bioRxiv. 2025 March 15.
- Research Square Preprint. 2021 Jun.
- Research Square Preprint. 2020 Aug.
Ver todos los productos específicos de isoformas Beta-lactamase
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Actividad biológica
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HDAC6 0.4 nM (IC50) |
HDAC1 8.35 nM (IC50) |
HDAC2 15.4 nM (IC50) |
HDAC3 51.6 nM (IC50) |
HDAC8 1430 nM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1206731-57-8
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Appearance Solid
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Peso molecular 458.55
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Fòrmula C27H30N4O3
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Color White to off-white
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SMILES
O=C(N/N=C/C1=CC=C(N(C2=CC=CC=C2)C3=CC=CC=C3)C=C1)CCCCCCC(NO)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (10)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
2023 Apr 6;14(4):250. PMID: 37024472 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
Sci Rep
Selective HDAC6 inhibitor WT161 modulates the VLA-4/FAK pathway by inhibiting PKA activity in acute lymphoblastic leukemia. [Abstract]2025 Nov 17;15(1):40178. PMID: 41249257 -
Biosci Rep
HDAC6 inhibitor WT161 performs anti-tumor effect on osteosarcoma and synergistically interacts with 5-FU. [Abstract]2021 Apr 30;41(4):BSR20203905. PMID: 33860796 -
Invest New Drugs
HDAC6 inhibition through WT161 synergizes with temozolomide, induces apoptosis, reduces cell motility, and decreases β-catenin levels in glioblastoma cells. [Abstract]2025 Apr;43(2):223-242. PMID: 39954199 -
J Appl Toxicol
Inorganic arsenic exposure promotes malignant progression by HDAC6-mediated down-regulation of HTRA1. [Abstract]2023 Aug;43(8):1214-1224. PMID: 36861143 -
Cancer Chemother Pharmacol
WT161, a selective HDAC6 inhibitor, decreases growth, enhances chemosensitivity, promotes apoptosis, and suppresses motility of melanoma cells. [Abstract]2025 Jan 17;95(1):22. PMID: 39821335 -
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Solvente y solubilidad
DMSO : ≥ 100 mg/mL (218.08 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Hideshima T, et al. Discovery of selective small-molecule HDAC6 inhibitor for overcoming proteasome inhibitor resistance in multiple myeloma. Proc Natl Acad Sci U S A. 2016 Nov 15;113(46):13162-13167. [Content Brief]
[2]. Severin Lechner, et al. Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target. Nat Chem Biol. 2022 Apr 28. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1808 mL | 10.9039 mL | 21.8079 mL | 54.5197 mL |
| 5 mM | 0.4362 mL | 2.1808 mL | 4.3616 mL | 10.9039 mL | |
| 10 mM | 0.2181 mL | 1.0904 mL | 2.1808 mL | 5.4520 mL | |
| 15 mM | 0.1454 mL | 0.7269 mL | 1.4539 mL | 3.6346 mL | |
| 20 mM | 0.1090 mL | 0.5452 mL | 1.0904 mL | 2.7260 mL | |
| 25 mM | 0.0872 mL | 0.4362 mL | 0.8723 mL | 2.1808 mL | |
| 30 mM | 0.0727 mL | 0.3635 mL | 0.7269 mL | 1.8173 mL | |
| 40 mM | 0.0545 mL | 0.2726 mL | 0.5452 mL | 1.3630 mL | |
| 50 mM | 0.0436 mL | 0.2181 mL | 0.4362 mL | 1.0904 mL | |
| 60 mM | 0.0363 mL | 0.1817 mL | 0.3635 mL | 0.9087 mL | |
| 80 mM | 0.0273 mL | 0.1363 mL | 0.2726 mL | 0.6815 mL | |
| 100 mM | 0.0218 mL | 0.1090 mL | 0.2181 mL | 0.5452 mL |
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