PROTAC HDAC6 degrader 11
Based on 1 Customer Validation
PROTAC HDAC6 degrader 11 is a PROTAC degrader targeting HDAC6, with a DC50 of 19.39 nM in HL-60 leukemia cells. PROTAC HDAC6 degrader 11 can form a ternary complex with HDAC6 and the cereblon E3 ligase, inducing polyubiquitination and proteasomal degradation of HDAC6. PROTAC HDAC6 degrader 11 inhibits the enzymatic activity of HDAC1 and does not trigger HDAC1 degradation. PROTAC HDAC6 degrader 11 induces hyperacetylation of α-tubulin. PROTAC HDAC6 degrader 11 can be used in related research on leukemia.
(Pink: HDAC6 ligand (HY-184979); Blue: Cereblon ligand (HY-103597); Black: linker).
For research use only. We do not sell to patients.
- Purity : 98.12%
- CAS No.: 2785404-83-1
- Formula: C41H41F4N7O11
- Molecular Weight:883.80
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
HDAC6 19.4 nM (DC50) |
In Vitro
PROTAC HDAC6 degrader 11 (120 min) potently inhibits purified recombinant HDAC6 with 129-fold selectivity over recombinant HDAC1[1].
PROTAC HDAC6 degrader 11induces selective HDAC6 degradation in HL-60 cells exclusively via ternary complex formation and the canonical ubiquitin-proteasome pathway[1].
PROTAC HDAC6 degrader 11 (1 μM; 6 h) does not induce any detectable off-target changes to the cellular proteome beyond selective HDAC6 degradation, matching the selective proteome profile of the related PROTAC A6[1].
PROTAC HDAC6 degrader 11 (compound B4) (6 h) selectively degrades HDAC6 with a DC50 of 19.39 nM in HL-60 leukemia cells, with no effect on HDAC1 or HDAC4 protein abundance[1].
PROTAC HDAC6 degrader 11 HDAC6 degrading activity is not restricted to leukemia cell lines and is also active in the U266 multiple myeloma cell line, matching the performance of the related PROTAC A6 in this cell model[1].
PROTAC HDAC6 degrader 11 (72 h) does not exhibit antiproliferative activity against a panel of human leukemia cell lines at concentrations up to 50 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HL-60 human acute promyelocytic leukemia cells
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Concentration:1 μM
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Incubation Time:6 h
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Result:Did not induce any detectable off-target changes in the cellular proteome apart from the selective degradation of HDAC6.
Chemical Information
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CAS No. 2785404-83-1
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Appearance Solid
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Molecular Weight 883.80
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Formula C41H41F4N7O11
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Color Off-white to light yellow
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SMILES
FC(F)(F)C(O)=O.O=C(CCCCCCCNC(COC1=CC=CC(C(N2C3CCC(NC3=O)=O)=O)=C1C2=O)=O)NC4=CC5=C(C=C4)N(C(C)=N5)CC6=C(C=C(C=C6)C(NO)=O)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (113.15 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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 (2.83 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 (2.83 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.
In Vivo Dissolution Calculator
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Purity & Documentation
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Data Sheet (273 KB)
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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)
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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 (sealed storage, away from moisture). 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 |
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| DMSO | 1 mM | 1.1315 mL | 5.6574 mL | 11.3148 mL | 28.2869 mL |
| 5 mM | 0.2263 mL | 1.1315 mL | 2.2630 mL | 5.6574 mL | |
| 10 mM | 0.1131 mL | 0.5657 mL | 1.1315 mL | 2.8287 mL | |
| 15 mM | 0.0754 mL | 0.3772 mL | 0.7543 mL | 1.8858 mL | |
| 20 mM | 0.0566 mL | 0.2829 mL | 0.5657 mL | 1.4143 mL | |
| 25 mM | 0.0453 mL | 0.2263 mL | 0.4526 mL | 1.1315 mL | |
| 30 mM | 0.0377 mL | 0.1886 mL | 0.3772 mL | 0.9429 mL | |
| 40 mM | 0.0283 mL | 0.1414 mL | 0.2829 mL | 0.7072 mL | |
| 50 mM | 0.0226 mL | 0.1131 mL | 0.2263 mL | 0.5657 mL | |
| 60 mM | 0.0189 mL | 0.0943 mL | 0.1886 mL | 0.4714 mL | |
| 80 mM | 0.0141 mL | 0.0707 mL | 0.1414 mL | 0.3536 mL | |
| 100 mM | 0.0113 mL | 0.0566 mL | 0.1131 mL | 0.2829 mL |
PROTAC HDAC6 degrader 11 Related Classifications
HY-152134 Related Classifications
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