ITSA-1
Based on 19 publication(s) in Google Scholar
ITSA-1 is an activator of histone deacetylase (HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation.
For research use only. We do not sell to patients.
- Purity: 99.73%
- CAS No.: 200626-61-5
- Formula: C13H7Cl2N3O
- Molecular Weight:292.12
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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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Cell Cycle/DNA Damage Compound Library
HY-L004
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Epigenetics Compound Library
HY-L005
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Histone Modification Research Compound Library
HY-L024
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Anti-Cancer Compound Library
HY-L025
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Anti-Aging Compound Library
HY-L034
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Oxygen Sensing Compound Library
HY-L045
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Anti-Pancreatic Cancer Compound Library
HY-L077
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
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Lactylation Compound Library
HY-L249
Publications Citing Use of MedChemExpress (MCE) ITSA-1
More- Cancer Cell. 2024 Oct 14;42(10):1729-1746.e8. [Abstract]
- Microbiome. 2023 Jan 31;11(1):17. [Abstract]
- Theranostics. 2021 Mar 20;11(11):5605-5619. [Abstract]
- Adv Sci (Weinh). 2025 Apr;12(15):e2412109. [Abstract]
- Cell Death Dis. 2024 Jan 29;15(1):95. [Abstract]
- Phytomedicine. 2025 Sep:145:157009. [Abstract]
- Am J Chin Med. 2024;52(6):1795-1817. [Abstract]
- Cell Biosci. 2021 May 21;11(1):93. [Abstract]
- Inflamm Res. 2023 Mar;72(3):553-576. [Abstract]
- Int Immunopharmacol. 2025 Aug 19:164:115386. [Abstract]
- Front Pharmacol. 2021 Jun 25:12:673366. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2023 Sep 18;1870(1):166889. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- Mediators Inflamm. 2025 Mar 20:2025:8156593. [Abstract]
- BMC Cancer. 2019 Mar 22;19(1):262. [Abstract]
- Toxicol Appl Pharmacol. 2024 May 10:487:116957. [Abstract]
- Arch Biochem Biophys. 2024 Feb:752:109878. [Abstract]
- SSRN. 2023 Oct 18.
- Aging (Albany NY). 2020 Mar 28;12(6):5411-5422. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Biological Activity
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HDAC |
ITSA-1 (50 μM; A549 cells) treatment serves to revert the TSA-arrested population to a normal cell cycle distribution. ITSA-1 is also able to effect cell cycle rescue over longer duration[1].
ITSA-1 (50 μM; 5 hours; A549 cells) treatment reduces the number of apoptosis in TSA-treated cells[1].
ITSA-1 (50 μM; 2 hours; A549 and murine ES cells cells) treatment suppresses TSA-induced histone acetylation. Importantly, suppression of acetylation levels is only observable when ITSA1 is added concurrent with or post TSA treatment[1].
ITSA-1 (50 μM; 30 minutes; murine ES cells cells) suppresses TSA-activated transcription in murine ES cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Murine ES cells
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Concentration:50 μM
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Incubation Time:
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Result:Served to revert the TSA-arrested population to a normal cell cycle distribution.
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Cell Line:A549 cells
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Concentration:50 μM
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Incubation Time:5 hours
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Result:Reduced the number of apoptosis.
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Cell Line:A549 and murine ES cells
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Concentration:50 μM
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Incubation Time:2 hours
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Result:Reduced histone acetylation to the baseline level.
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Cell Line:Murine ES cells
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Concentration:50 μM
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Incubation Time:30 minutes
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Result:Suppressed TSA-activated transcription.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CBS+/− mice[2]
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Dosage:0.5 mg/kg
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Administration:Intraperitoneal injection; 3 times/week; for 8 weeks
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Result:Balanced deacetylation activity and suppressed IL-6 and TNF-α expression.
Chemical Information
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CAS No. 200626-61-5
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Appearance Solid
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Molecular Weight 292.12
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Formula C13H7Cl2N3O
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Color White to off-white
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SMILES
O=C(N1N=NC2=CC=CC=C21)C3=CC=C(Cl)C=C3Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (19)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Fusobacterium nucleatum facilitates anti-PD-1 therapy in microsatellite stable colorectal cancer. [Abstract]2024 Oct 14;42(10):1729-1746.e8. PMID: 39303724 -
Microbiome
Gut microbiota-derived metabolites mediate the neuroprotective effect of melatonin in cognitive impairment induced by sleep deprivation. [Abstract]2023 Jan 31;11(1):17. PMID: 36721179
ITSA-1 purchased from MedChemExpress. Usage Cited in: Microbiome. 2023 Jan 31;11(1):17. [Abstract]
ITSA‑1 (50 μM; 24 h), acting as an HDAC3 agonist, significantly upregulated the expression of p‑IκB (34.8%) and p‑P65 (88.7%) proteins in BV2 cells compared with the LPS + butyrate treatment group.
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Theranostics
HDAC1 and 2 regulate endothelial VCAM-1 expression and atherogenesis by suppressing methylation of the GATA6 promoter. [Abstract]2021 Mar 20;11(11):5605-5619. PMID: 33859766 -
Adv Sci (Weinh)
NAD+ Metabolism Reprogramming Drives SIRT1-Dependent Deacetylation Inducing PD-L1 Nuclear Localization in Cervical Cancer. [Abstract]2025 Apr;12(15):e2412109. PMID: 39988985 -
Cell Death Dis
CYLD induces high oxidative stress and DNA damage through class I HDACs to promote radiosensitivity in nasopharyngeal carcinoma. [Abstract]2024 Jan 29;15(1):95. PMID: 38287022
ITSA-1 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 Jan 29;15(1):95. [Abstract]
Detection of γH2AX protein level in NPC cells by CYLD overexpression with or without ITSA-1 (10 μM) for 24 h treatment. The results showed that CYLD-induced DNA damage could be restored by the HDAC agonist ITSA-1.
ITSA-1 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 Jan 29;15(1):95. [Abstract]
Colony formation assay showing survival fractions of CYLD overexpressing cells treated with ITSA-1 (10 μM) or untreated at 24 h before irradiation; surviving fractions were calculated by comparing the colony number of each treatment group with untreated groups (0 Gy). The results showed that the increased radiosensitivity caused by the overexpression of CYLD was reversed by ITSA-1.
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Phytomedicine
Jing An decoction alleviates neuroinflammation in Tourette syndrome by regulating butyrate-mediated microbiota-gut-brain axis. [Abstract]2025 Sep:145:157009. PMID: 40674913 -
Am J Chin Med
Astragaloside I from Astragalus Attenuates Diabetic Kidney Disease by Regulating HDAC3/Klotho/TGF- β 1 Loop. [Abstract]2024;52(6):1795-1817. PMID: 39347955 -
Cell Biosci
The ketogenic diet increases Neuregulin 1 expression via elevating histone acetylation and its anti-seizure effect requires ErbB4 kinase activity. [Abstract]2021 May 21;11(1):93. PMID: 34020711 -
Inflamm Res
Human bone marrow mesenchymal stem cell-derived extracellular vesicles reduce inflammation and pyroptosis in acute kidney injury via miR-223-3p/HDAC2/SNRK. [Abstract]2023 Mar;72(3):553-576. PMID: 36640195
ITSA-1 purchased from MedChemExpress. Usage Cited in: Inflamm Res. 2023 Mar;72(3):553-576. [Abstract]
ITSA-1 (10 μM) nullifies the promoting impacts of sh-HDAC2 on H3K27ac and SNRK protein expression in HK-2 cells.
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Int Immunopharmacol
Targeting PARK7: Sodium 4-Phenylbutyrate shields endothelial cells from oxidative stress and GSDME-mediated Pyroptosis in acute lung injury. [Abstract]2025 Aug 19:164:115386. PMID: 40834532 -
Front Pharmacol
Traditional Chinese Medication Tongxinluo Attenuates Lipidosis in Ox-LDL-Stimulated Macrophages by Enhancing Beclin-1-Induced Autophagy. [Abstract]2021 Jun 25:12:673366. PMID: 34248627 -
Biochim Biophys Acta Mol Basis Dis
Maternal obstructive sleep apnea aggravates metabolic dysfunction-associated fatty liver disease via HMGB1-TLR4 signaling-mediated endoplasmic reticulum stress in male offspring rats. [Abstract]2023 Sep 18;1870(1):166889. PMID: 37730152 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
Mediators Inflamm
The Histone Deacetylase Activator ITSA-1 Improves the Prognosis of Cardiac Arrest Rats by Alleviating Systemic Inflammatory Responses Following Cardiopulmonary Resuscitation. [Abstract]2025 Mar 20:2025:8156593. PMID: 40151316 -
BMC Cancer
Short-term stimulation with histone deacetylase inhibitor trichostatin a induces epithelial-mesenchymal transition in nasopharyngeal carcinoma cells without increasing cell invasion ability. [Abstract]2019 Mar 22;19(1):262. PMID: 30902084
ITSA-1 purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2019 Mar 22;19(1):262. [Abstract]
Western blot is used to examine the protein levels of cell proliferation (PCNA), cell cycle (cyclinD1, CDK2 and p16) and EMT-associated genes (E-cadherin and Vimentin) in the treatment of TSA or TSA plus ITSA-1.
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Toxicol Appl Pharmacol
A novel histone deacetylase inhibitor Se-SAHA attenuates isoproterenol-induced heart failure via antioxidative stress and autophagy inhibition. [Abstract]2024 May 10:487:116957. PMID: 38735590 -
Arch Biochem Biophys
Mechanism by which HDAC3 regulates manganese induced H3K27ac in SH-SY5Y cells and intervention by curcumin. [Abstract]2024 Feb:752:109878. PMID: 38151197 -
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Aging (Albany NY)
HDAC6 promotes sepsis development by impairing PHB1-mediated mitochondrial respiratory chain function. [Abstract]2020 Mar 28;12(6):5411-5422. PMID: 32221047
Solvent & Solubility
DMSO : ≥ 100 mg/mL (342.33 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (8.56 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 (8.56 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
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.
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 (286 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Koeller KM et al. Chemical genetic modifier screens: small molecule trichostatin suppressors as probes of intracellular histoneand tubulin acetylation. Chem Biol. 2003 May;10(5):397-410. [Content Brief]
[2]. Behera J, et al. Hydrogen Sulfide Promotes Bone Homeostasis by Balancing Inflammatory Cytokine Signaling in CBS-Deficient Mice through an Epigenetic Mechanism. Sci Rep. 2018 Oct 15;8(1):15226. [Content Brief]
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.4233 mL | 17.1163 mL | 34.2325 mL | 85.5813 mL |
| 5 mM | 0.6847 mL | 3.4233 mL | 6.8465 mL | 17.1163 mL | |
| 10 mM | 0.3423 mL | 1.7116 mL | 3.4233 mL | 8.5581 mL | |
| 15 mM | 0.2282 mL | 1.1411 mL | 2.2822 mL | 5.7054 mL | |
| 20 mM | 0.1712 mL | 0.8558 mL | 1.7116 mL | 4.2791 mL | |
| 25 mM | 0.1369 mL | 0.6847 mL | 1.3693 mL | 3.4233 mL | |
| 30 mM | 0.1141 mL | 0.5705 mL | 1.1411 mL | 2.8527 mL | |
| 40 mM | 0.0856 mL | 0.4279 mL | 0.8558 mL | 2.1395 mL | |
| 50 mM | 0.0685 mL | 0.3423 mL | 0.6847 mL | 1.7116 mL | |
| 60 mM | 0.0571 mL | 0.2853 mL | 0.5705 mL | 1.4264 mL | |
| 80 mM | 0.0428 mL | 0.2140 mL | 0.4279 mL | 1.0698 mL | |
| 100 mM | 0.0342 mL | 0.1712 mL | 0.3423 mL | 0.8558 mL |
ITSA-1 Related Classifications
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