2. Cell Cycle/DNA Damage Epigenetics PROTAC
  3. HDAC PROTACs
  4. HDAC6 degrader-3

HDAC6 degrader-3 is a potent and selective HDAC6 degrader via ternary complex formation and the ubiquitin-proteasome pathway with a DC50 value of 19.4 nM. HDAC6 degrader-3 has IC50s of 4.54 nM and 0.647 μM for HDAC6 and HDAC1, respectively. HDAC6 degrader-3 causes strong hyperacetylation of α-tubulin.

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HDAC6 degrader-3 Chemical Structure

HDAC6 degrader-3 Chemical Structure

CAS No. : 2785404-83-1

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Based on 1 publication(s) in Google Scholar

HDAC6 degrader-3 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

HDAC6 degrader-3 is a potent and selective HDAC6 degrader via ternary complex formation and the ubiquitin-proteasome pathway with a DC50 value of 19.4 nM. HDAC6 degrader-3 has IC50s of 4.54 nM and 0.647 μM for HDAC6 and HDAC1, respectively. HDAC6 degrader-3 causes strong hyperacetylation of α-tubulin[1].

IC50 & Target[1]

HDAC6

19.4 nM (ID50)

HDAC6

4.54 nM (IC50)

HDAC1

0.647 μM (IC50)

Cereblon

 

In Vitro

HDAC6 degrader-3 (compound B4; 100-1000 nM; 24 h) demonstrates potent HDAC6 degradation as well as hyperacetylation of α-tubulin[1].
HDAC6 degrader-3 (0.5-50 μM; 72 h) does not display any inhibitory effects on the cellular viability of leukemic cell lines (697, HL-60, KASUMI-1, MV4-11, REH, THP-1, SKNO-1, MOLM-13)[1].

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

HDAC6 degrader-3 Related Antibodies

Western Blot Analysis[1]

Cell Line: U266 multiple myeloma cell line
Concentration: 100 nM and 1000 nM
Incubation Time: 24 h
Result: Demonstrated potent HDAC6 degradation as well as hyperacetylation of α-tubulin.
Molecular Weight

883.80

Formula

C41H41F4N7O11
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

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.FC(F)(F)C(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1315 mL 5.6574 mL 11.3148 mL
5 mM 0.2263 mL 1.1315 mL 2.2630 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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
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
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HDAC6 degrader-3 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HDAC6 degrader-32785404-83-1HDACPROTACsHistone deacetylasesHDAC6HDAC1hyperacetylationα-tubulinInhibitorinhibitorinhibit

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