1. Cell Cycle/DNA Damage Epigenetics
  2. HDAC
  3. ITSA-1

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.

ITSA-1 Chemical Structure

ITSA-1 Chemical Structure

CAS No. : 200626-61-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
5 mg USD 25 In-stock
10 mg USD 40 In-stock
25 mg USD 80 In-stock
50 mg USD 130 In-stock
100 mg USD 200 In-stock
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Customer Review

Based on 14 publication(s) in Google Scholar

Top Publications Citing Use of Products

    ITSA-1 purchased from MedChemExpress. Usage Cited in: Inflamm Res. 2023 Jan 14.  [Abstract]

    ITSA-1 (10 μM) nullifies the promoting impacts of sh-HDAC2 on H3K27ac and SNRK protein expression in HK-2 cells.

    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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    Description

    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

     

    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.
    Molecular Weight

    292.12

    Formula

    C13H7Cl2N3O

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 32 mg/mL (109.54 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.4233 mL 17.1163 mL 34.2325 mL
    5 mM 0.6847 mL 3.4233 mL 6.8465 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, 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.

    • 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

    Concentration (start)

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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: ≥ 2.5 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.
    • Protocol 2

      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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

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    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).
    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, 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
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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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    Cat. No.:
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