WT161 |
Catalog No.GC18206
One-Click Copy Product Info
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WT161은 IC50이 0.40nM인 강력하고 선택적인 HDAC6 억제제입니다. WT161은 또한 메탈로-β-락타마제 도메인 함유 단백질 2(MBLAC2)을 억제합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1206731-57-8
Sample solution is provided at 25 µL, 10mM.
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WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM.
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].
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].
References:
[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.
Cell experiment: | 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]. |
Animal experiment: | 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]. |
References: [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. | |
| Cas No. | 1206731-57-8 | SDF | |
| Chemical Name | 8-(hydroxyamino)-8-oxo-octanoic acid, 2-[[4-(diphenylamino)phenyl]methylene]hydrazide | ||
| Canonical SMILES | ONC(CCCCCCC(N/N=C/C(C=C1)=CC=C1N(C2=CC=CC=C2)C3=CC=CC=C3)=O)=O | ||
| Formula | C27H30N4O3 | M.Wt | 458.6 |
| Solubility | DMF: 10 mg/ml,DMSO: 10 mg/ml,DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1805 mL | 10.9027 mL | 21.8055 mL |
| 5 mM | 436.1 μL | 2.1805 mL | 4.3611 mL |
| 10 mM | 218.1 μL | 1.0903 mL | 2.1805 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)