1. Cell Cycle/DNA Damage Epigenetics
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  3. J22352

J22352 is a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC50 value of 4.7 nM. J22352 promotes HDAC6 degradation and induces anticancer effects by inhibiting autophagy and eliciting the antitumor immune response in glioblastoma cancers, and leading to the restoration of host antitumor activity by reducing the immunosuppressive activity of PD-L1.

For research use only. We do not sell to patients.

J22352 Chemical Structure

J22352 Chemical Structure

CAS No. : 2252395-44-9

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Description

J22352 is a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC50 value of 4.7 nM. J22352 promotes HDAC6 degradation and induces anticancer effects by inhibiting autophagy and eliciting the antitumor immune response in glioblastoma cancers, and leading to the restoration of host antitumor activity by reducing the immunosuppressive activity of PD-L1[1].

IC50 & Target[1]

HDAC6

4.7 nM (IC50)

In Vitro

J22352 (0.1-20 μM; 72 hours) decreases U87MG cell viability in a dose-dependent manner[1].
J22352 (10 μM; 24 hours) shows a dose-dependent decrease in HDAC6 protein abundance[1].

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

Cell Viability Assay[1]

Cell Line: U87MG cells
Concentration: 0.1 μM; 0.5 μM; 1μM; 2.5 μM; 5 μM; 10 μM; 20 μM
Incubation Time: 72 hours
Result: A dose-dependent decrease on U87MG cell proliferation.

Western Blot Analysis[1]

Cell Line: U87MG cells
Concentration: 10 μM
Incubation Time: 24 hours
Result: A dose-dependent decrease in aberrant overexpression of HDAC6 in glioblastoma.
In Vivo

J22352 (10 mg/kg; given i.p. per day for 14 days in male nude mice) results in a >80% tumor growth inhibition (TGI) rate. J22352 is well tolerated in mice[1].

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

Animal Model: Male nude mice (BALB/cAnN.Cg-Foxnlnu/CrlNarl, 4-6 weeks old)[1]
Dosage: 10 mg/kg
Administration: Given i.p.; per day for 14 days
Result: Marked anti-tumor effects and well tolerated in mice.
Molecular Weight

415.44

Formula

C24H21N3O4

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=CC=C1N2CC3=CC=C(C(NO)=O)C=C3)N(CCC4=CC=CC=C4)C2=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (300.89 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 2.4071 mL 12.0354 mL 24.0709 mL
5 mM 0.4814 mL 2.4071 mL 4.8142 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, 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.08 mg/mL (5.01 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.01 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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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(per animal)

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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).
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, 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 2.4071 mL 12.0354 mL 24.0709 mL 60.1772 mL
5 mM 0.4814 mL 2.4071 mL 4.8142 mL 12.0354 mL
10 mM 0.2407 mL 1.2035 mL 2.4071 mL 6.0177 mL
15 mM 0.1605 mL 0.8024 mL 1.6047 mL 4.0118 mL
20 mM 0.1204 mL 0.6018 mL 1.2035 mL 3.0089 mL
25 mM 0.0963 mL 0.4814 mL 0.9628 mL 2.4071 mL
30 mM 0.0802 mL 0.4012 mL 0.8024 mL 2.0059 mL
40 mM 0.0602 mL 0.3009 mL 0.6018 mL 1.5044 mL
50 mM 0.0481 mL 0.2407 mL 0.4814 mL 1.2035 mL
60 mM 0.0401 mL 0.2006 mL 0.4012 mL 1.0030 mL
80 mM 0.0301 mL 0.1504 mL 0.3009 mL 0.7522 mL
100 mM 0.0241 mL 0.1204 mL 0.2407 mL 0.6018 mL
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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.

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J22352
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