| Size | Price | Stock | Qty |
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| Targets |
HDAC6 (histone deacetylase 6). J22352 is a highly selective HDAC6 inhibitor with >2000-fold selectivity over class I HDACs (HDAC1, HDAC2, and HDAC3) and little activity against HDAC8. The compound promotes HDAC6 degradation through a PROTAC-like mechanism, leading to sustained target inhibition.
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| ln Vitro |
J22352 (0.1–20 μM; 72 hours) dose-dependently decreases the viability of U87MG cells[1]. J22352 (10 μM; 24 hours) decreases the quantity of HDAC6 protein in a dose-dependent manner [1].
J22352 inhibits HDAC6 with an IC₅0 of 4.7 nM. It shows >2000-fold selectivity for HDAC6 over HDAC1, HDAC2, and HDAC3. In cell-based assays, J22352 treatment (24 hours) shows a dose-dependent decrease in HDAC6 protein abundance, confirming its degradation activity. The compound induces anticancer effects through autophagy inhibition. |
| ln Vivo |
J22352 (10 mg/kg; intraperitoneally injected daily for 14 days in nude hamster mice) resulted in a >80% tumor growth inhibition (TGI) rate. J22352 is well tolerated in mice [1].
In vivo, J22352 demonstrates antitumor efficacy in glioblastoma models. It promotes HDAC6 degradation and induces anticancer effects by inhibiting autophagy and eliciting antitumor immune responses. The compound restores host antitumor activity by reducing PD-L1-mediated immunosuppression. These effects position J22352 as a promising agent for cancer immunotherapy. |
| Enzyme Assay |
HDAC6 enzymatic activity is measured using a fluorogenic assay with a peptide substrate containing an acetylated lysine residue. Recombinant HDAC6 enzyme is incubated with the substrate and serial dilutions of test compound. After deacetylation, the substrate is developed with a developer solution, and fluorescence is measured. IC₅0 values are calculated from dose-response curves.
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| Cell Assay |
Cell Viability Assay[1] Cell
Cell Types: U87MG Cell Tested Concentrations: 0.1 μM; 0.5 μM; 1 μM; 2.5 μM; 5 μM; 10 μM; 20 μM Incubation Duration: 72 hrs (hours) Experimental Results: U87MG cell proliferation diminished in a dose-dependent manner. Western Blot Analysis[1] Cell Types: U87MG Cell Tested Concentrations: 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Aberrant overexpression of HDAC6 in glioblastoma demonstrated a dose-dependent decrease. Cancer cell lines (e.g., glioblastoma, melanoma, or breast cancer cells) are treated with J22352 at various concentrations for 24-72 hours. HDAC6 protein levels are assessed by Western blotting to confirm degradation. Autophagy markers (LC3-II, p62) are measured. Cell viability is assessed using MTT or CellTiter-Glo assays. PD-L1 expression is evaluated by flow cytometry or Western blotting. |
| Animal Protocol |
Animal/Disease Models: Male nude mice (BALB/cAnN.Cg-Foxnlnu/CrlNarl, 4-6 weeks old) [1]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 14 days Experimental Results: Significant Anti-tumor effects and well tolerated in mice. Mice bearing subcutaneous or orthotopic tumor xenografts (e.g., glioblastoma) are administered J22352 intraperitoneally or orally at various doses. Tumor growth is monitored by caliper measurements or bioluminescence imaging. Tumors are harvested for pharmacodynamic analysis of HDAC6 degradation, autophagy markers, and immune cell infiltration. Survival is assessed in orthotopic models. |
| ADME/Pharmacokinetics |
J22352 has a molecular weight of 415.44 g/mol and formula C24H21N3O4. Standard PK parameters (half-life, Cmax, AUC, clearance, volume of distribution, oral bioavailability) would be determined in rodent PK studies. The compound is formulated in suitable vehicles for in vivo administration. As a PROTAC-like molecule, it may have distinct PK properties compared to conventional small molecule inhibitors.
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| Toxicity/Toxicokinetics |
Toxicology data for J22352 are not publicly available. Standard preclinical safety assessment would include cytotoxicity profiling, hERG inhibition testing, and repeat-dose toxicology studies in rodents. Given its HDAC6 selectivity, J22352 is expected to have an improved safety profile compared to pan-HDAC inhibitors.
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| References | |
| Additional Infomation |
J22352 is a preclinical research compound for cancer and immunotherapy studies. It is not FDA-approved. The compound's PROTAC-like mechanism (inducing HDAC6 degradation rather than just enzymatic inhibition) provides sustained target suppression. J22352 is a valuable tool for studying HDAC6 biology and developing novel cancer immunotherapies.
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| Molecular Formula |
C24H27N3O4
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| Molecular Weight |
421.488886117935
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| Exact Mass |
415.153
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| CAS # |
2252395-44-9
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| PubChem CID |
138377601
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
31
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| Complexity |
655
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1C2CCCCC2N(CC2C=CC(C(NO)=O)=CC=2)C(N1CCC1C=CC=CC=1)=O
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| InChi Key |
JBJIKUXUKSADFV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H21N3O4/c28-22(25-31)19-12-10-18(11-13-19)16-27-21-9-5-4-8-20(21)23(29)26(24(27)30)15-14-17-6-2-1-3-7-17/h1-13,31H,14-16H2,(H,25,28)
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| Chemical Name |
4-[[2,4-dioxo-3-(2-phenylethyl)quinazolin-1-yl]methyl]-N-hydroxybenzamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~300.89 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.01 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.01 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.01 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3725 mL | 11.8627 mL | 23.7254 mL | |
| 5 mM | 0.4745 mL | 2.3725 mL | 4.7451 mL | |
| 10 mM | 0.2373 mL | 1.1863 mL | 2.3725 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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