Art. -Nr.: HY-100508

ITSA-1

19 Cited Publications

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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.

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Reinheit: 99.73%
CAS. Nr.: 200626-61-5
Formel: C₁₃H₇Cl₂N₃O
Molecular Weight:292.12

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

ITSA-1 Chemical Structure

CAS. Nr.: 200626-61-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (19)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

ITSA-1 is an activator of histone deacetylase (HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation^[1].

IC₅₀ & Target^[1]

HDAC

Alle HDAC Isoform-spezifische Produkte anzeigen :

In Vitro

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.

Cell Cycle Analysis^[1]

Cell Line:

Murine ES cells
Concentration:

50 μM
Incubation Time:
Result:

Served to revert the TSA-arrested population to a normal cell cycle distribution.

Apoptosis Analysis^[1]

Cell Line:

A549 cells
Concentration:

50 μM
Incubation Time:

5 hours
Result:

Reduced the number of apoptosis.

Western Blot Analysis^[1]

Cell Line:

A549 and murine ES cells
Concentration:

50 μM
Incubation Time:

2 hours
Result:

Reduced histone acetylation to the baseline level.

RT-PCR^[1]

Cell Line:

Murine ES cells
Concentration:

50 μM
Incubation Time:

30 minutes
Result:

Suppressed TSA-activated transcription.

In Vivo

ITSA-1 (0.5 mg/kg; intraperitoneal injection; 3 times/week; for 8 weeks; CBS^+/ mice) balances deacetylation activity and suppresses IL-6 and TNF-α expression and thereby attenuated histone acetylationdependent infammatory signaling^[2].

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

Animal Model:

CBS^+/− mice^[2]
Dosage:

0.5 mg/kg
Administration:

Intraperitoneal injection; 3 times/week; for 8 weeks
Result:

Balanced deacetylation activity and suppressed IL-6 and TNF-α expression.

Chemical Information

CAS. Nr. 200626-61-5
Appearance Solid
Molecular Weight 292.12
Formel C₁₃H₇Cl₂N₃O
Color White to off-white
SMILES

O=C(N1N=NC2=CC=CC=C21)C3=CC=C(Cl)C=C3Cl
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (19)

All WBCell Proliferation/Viability Assay

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Journal Impact Factor

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.
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.
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.
Int Immunopharmacol

Targeting PARK7: Sodium 4-Phenylbutyrate shields endothelial cells from oxidative stress and GSDME-mediated Pyroptosis in acute lung injury. [Abstract]

2025 Oct 30:164:115386. 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)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

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.
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
SSRN

2023 Oct 18.
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

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.4233 mL

17.1163 mL

34.2325 mL

5 mM

0.6847 mL

3.4233 mL

6.8465 mL

10 mM

0.3423 mL

1.7116 mL

3.4233 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 90% Corn Oil

Solubility: ≥ 5 mg/mL (17.12 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 2

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.

Protocol 3

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
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

Keywords

ITSA-1

19 Cited Publications

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ITSA-1

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Oxygen Sensing Compound Library

Anti-Pancreatic Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) ITSA-1

Alle HDAC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (19)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ITSA-1

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Oxygen Sensing Compound Library

Anti-Pancreatic Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) ITSA-1

Alle HDAC Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (19)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ITSA-1 Related Classifications

HY-100508 Related Classifications