PROTAC HDAC6 degrader 2
Based on 1 Customer Validation
PROTAC HDAC6 degrader 2 is a non‑hydroxamate selective HDAC6 PROTAC degrader with an IC50 of 0.643 μM and shows high selectivity for HDAC6 over HDAC1-4. PROTAC HDAC6 degrader 2 recruits VHL E3 ubiquitin ligase to trigger HDAC6 ubiquitination and subsequent proteasomal degradation. PROTAC HDAC6 degrader 2 selectively elevates acetylated α-tubulin levels in cancer cells, and does not induce histone H3 hyperacetylation or obvious loss of cell viability. PROTAC HDAC6 degrader 2 is applicable for research on multiple myeloma.
(Pink: HDAC6 ligand (HY-171141); Blue: VHL ligand (HY-10984); Black: linker).
For research use only. We do not sell to patients.
- Purity : 99.45%
- Formula: C34H33F2N9O8
- Molecular Weight:733.68
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
All PROTACs Isoforms
More
Biological Activity
Description
IC50 & Target
[1]|
HDAC6 0.643 μM (IC50) |
In Vitro
PROTAC HDAC6 degrader 2 (compound 1) potently and selectively inhibits HDAC6 enzymatic activity with an IC50 of 0.643 μM, and is inactive against HDAC1-4 (IC50 >30 μM)[1].
PROTAC HDAC6 degrader 2 (1 μM; 24 h) induces 84% maximal HDAC6 degradation in MM.1S multiple myeloma cells[1].
PROTAC HDAC6 degrader 2 (Serial dilutions; 90 min) exhibits inhibitory activity against human recombinant HDAC1, HDAC2, HDAC3/NcoR2, HDAC4, and HDAC6[1].
PROTAC HDAC6 degrader 2 (1 μM; 24 h) induces HDAC6 degradation in human multiple myeloma MM.1S cells[1].
PROTAC HDAC6 degrader 2 (1-10 μM; 72 h) exhibits cytotoxic potential in human multiple myeloma MM.1S cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
-
Cell Line:MM.1S multiple myeloma cells
-
Concentration:1 μM
-
Incubation Time:24 h
-
Result:Induced 84% maximal HDAC6 degradation.
-
Cell Line:human multiple myeloma MM.1S cells
-
Concentration:1 μM
-
Incubation Time:24 h
-
Result:Induced degradation of HDAC6 protein.
-
Cell Line:human multiple myeloma MM.1S cells
-
Concentration:1-10 μM
-
Incubation Time:72 h
-
Result:Exhibited cytotoxic potential.
Chemical Information
-
Appearance Solid
-
Molecular Weight 733.68
-
Formula C34H33F2N9O8
-
Color Light yellow to green yellow
-
SMILES
FC(C1=NN=C(C2=CN=C(NCC3=CC(CNC(COCCOCCNC4=CC=CC5=C4C(N(C6CCC(NC6=O)=O)C5=O)=O)=O)=CC=C3)N=C2)O1)F
-
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 (136.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 (3.41 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
-
CCK-8/WST-8 Cell Proliferation Assay
The CCK-8/WST-8 assay is based on the reduction of the water-soluble tetrazolium salt WST-8 to a water-soluble formazan product by cellular dehydrogenases in metabolically active cells, where the generated formazan amount is proportional to the number of living cells and is quantified by measuring absorbance in the visible range, providing a colorimetric readout for cell viability and proliferation assessment. This class of tetrazolium-based assays improves upon earlier MTT-based systems by producing a water-soluble formazan, eliminating the need for organic solubilization steps and enabling direct spectrophotometric measurement in culture medium.
-
MTT Cell Proliferation Assay
The MTT assay is a colorimetric endpoint assay for estimating viable cell number, cell growth, cytotoxicity, or cell activation in cultured mammalian cells. Living cells reduce the yellow tetrazolium salt MTT into purple/blue formazan, while dead cells do not generate the same signal; the resulting color can be quantified with a multiwell spectrophotometer. MTT reduction is commonly interpreted as a readout of metabolic activity that often correlates with viable cell number, but it should not be treated as a direct cell-counting method unless the assay is optimized for the cell type and experimental condition. Studies show that MTT reduction can involve mitochondrial and non-mitochondrial reducing systems, and formazan may accumulate in intracellular lipid droplets rather than simply marking mitochondria.
-
Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
-
Data Sheet (271 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.3630 mL | 6.8150 mL | 13.6299 mL | 34.0748 mL |
| 5 mM | 0.2726 mL | 1.3630 mL | 2.7260 mL | 6.8150 mL | |
| 10 mM | 0.1363 mL | 0.6815 mL | 1.3630 mL | 3.4075 mL | |
| 15 mM | 0.0909 mL | 0.4543 mL | 0.9087 mL | 2.2717 mL | |
| 20 mM | 0.0681 mL | 0.3407 mL | 0.6815 mL | 1.7037 mL | |
| 25 mM | 0.0545 mL | 0.2726 mL | 0.5452 mL | 1.3630 mL | |
| 30 mM | 0.0454 mL | 0.2272 mL | 0.4543 mL | 1.1358 mL | |
| 40 mM | 0.0341 mL | 0.1704 mL | 0.3407 mL | 0.8519 mL | |
| 50 mM | 0.0273 mL | 0.1363 mL | 0.2726 mL | 0.6815 mL | |
| 60 mM | 0.0227 mL | 0.1136 mL | 0.2272 mL | 0.5679 mL | |
| 80 mM | 0.0170 mL | 0.0852 mL | 0.1704 mL | 0.4259 mL | |
| 100 mM | 0.0136 mL | 0.0681 mL | 0.1363 mL | 0.3407 mL |
PROTAC HDAC6 degrader 2 Related Classifications
HY-171139 Related Classifications
Powered by Bioz