2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. Givinostat

Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat can be used for Duchenne muscular dystrophy (DMD) research. Givinostat can penetrate the blood-brain barrier (BBB).

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

CAS No. : 497833-27-9

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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Givinostat:

Givinostat Related Antibodies

Top Publications Citing Use of Products

    Givinostat purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2021 Jul;54(7):e13072.  [Abstract]

    The HSCs shown were treated with DNMTs inhibitors (5-azacytidine, 2 μmol/L), G9a inhibitors (UNC0642, 2 μmol/L), and pan-HDAC inhibitor Givinostat (ITF-2357, 100 nmol/L) for 48 hours, or with EZH2 inhibitors (EPZ-6438, 10 μmol/L) for 72 hours. KLF14 expression was analyzed by RT-qPCR.

    Givinostat purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2021 Jul;54(7):e13072.  [Abstract]

    The HSCs shown were treated with DNMT inhibitors (5-azacytidine, 2 μmol/L), G9a inhibitors (UNC0642, 2 μmol/L), and pan-HDAC inhibitor Givinostat (ITF-2357, 100 nmol/L) for 48 hours, or with EZH2 inhibitors (EPZ-6438, 10 μmol/L) for 72 hours. KLF14 expression was detected by Western blotting.

    Givinostat purchased from MedChemExpress. Usage Cited in: Commun Biol. 2021 Oct 29;4(1):1235.  [Abstract]

    TNBC model cells (MDA-MB-231 and BT-549) were treated with indicated HDACi (Vorinostat: 10 µM; Panobinostat: 1 µM; Romidepsin: 1 µM; Givinostat: 1 µM) for 24 h and expression of LIFR, p-STAT3(Y705), and STAT3 were determined using Western blotting.

    View All HDAC Isoform Specific Products:

    View All Isoforms
    HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat can be used for Duchenne muscular dystrophy (DMD) research. Givinostat can penetrate the blood-brain barrier (BBB)[1][2][3][4].

    IC50 & Target[1][3]

    hHDAC3

    157 nM (IC50)

    HD1-B

    7.5 nM (IC50)

    HD1-A

    16 nM (IC50)

    HD2

    10 nM (IC50)

    hHDAC1

    198 nM (IC50)

    hHDAC11

    292 nM (IC50)

    hHDAC6

    315 nM (IC50)

    hHDAC2

    325 nM (IC50)

    hHDAC10

    340 nM (IC50)

    hHDAC7

    524 nM (IC50)

    hHDAC5

    532 nM (IC50)

    hHDAC9

    541 nM (IC50)

    hHDAC8

    854 nM (IC50)

    hHDAC4

    1059 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    697 IC50
    100 nM
    Compound: Givinostat
    Cytotoxicity against human 697 cells after 48 hrs by CellTiter 96 aqueous one solution assay
    Cytotoxicity against human 697 cells after 48 hrs by CellTiter 96 aqueous one solution assay
    		[PMID: 31710483]
    PBMC IC50
    313 nM
    Compound: Givinostat
    Cytotoxicity against human PBMC cells after 72 hrs by CellTiter 96 aqueous one solution assay
    Cytotoxicity against human PBMC cells after 72 hrs by CellTiter 96 aqueous one solution assay
    		[PMID: 31710483]
    Sf9 IC50
    44 nM
    Compound: Givinostat
    Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method
    Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method
    		[PMID: 31710483]
    In Vitro

    Givinostat (ITF2357) suppresses total LPS-induced IL-1β production robustly compared with the reduction by ITF3056. At 25, 50, and 100 nM, Givinostat reduced IL-1β secretion more than 70%. Givinostat (ITF-2357) suppresses the production of IL-6 in PBMCs stimulated with TLR agonists as well as the combination of IL-12 plus IL-18. IL-6 secretion decreases to 50% at 50 nM Givinostat, but at 100 and 200 nM, there is no reduction[1]. As shown by the CCK-8 assay, Givinostat (ITF-2357) inhibits JS-1 cell proliferation in a concentration-dependent manner. Treatment with Givinostat ≥500 nM is associated with significant inhibition of JS-1 cell proliferation (P<0.01). Also, the cell inhibition rate significantly differs between the group cotreated with Givinostat ≥250 nM plus LPS and the group without LPS treatment (same Givinostat concentration) (P<0.05)[2].

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

    Givinostat Related Antibodies
    In Vivo

    Givinostat (ITF2357) at 10 mg/kg is used as a positive control and, as expected, reduced serum TNFα by 60%. Strikingly, pretreatment of ITF3056 starting at 0.1 mg/kg significantly reduces the circulating TNFα by nearly 90%. To achieve a significant increase in serum IL-1β production, a higher dose of LPS is injected (10 mg/kg), and blood is collected after 4 h. Similarly, when pretreated with lower doses of Givinostat (ITF-2357) (1 or 5 mg/kg), there is a 22% reduction for 1 mg/kg and 40% for 5 mg/kg[1].

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

    421.49

    Formula

    C24H27N3O4
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C(OCC1=CC=C2C=C(CN(CC)CC)C=CC2=C1)NC3=CC=C(C(NO)=O)C=C3
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 200 mg/mL (474.51 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 2.3725 mL 11.8627 mL 23.7254 mL
    5 mM 0.4745 mL 2.3725 mL 4.7451 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 3 mg/mL (7.12 mM); Clear solution

    In Vivo Dissolution Calculator
    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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    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

    Purity: 98.67%

    SDS (396 KB)

    COA (244 KB) HNMR (264 KB) RP-HPLC (251 KB) LCMS (97 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    After the JS-1 cell line is cultured in DMEM with 10% fetal bovine serum for 24 h, 30 wells of JS-1 cells are divided into two groups. In the first group, the culture medium is replaced by complete medium with final Givinostat (ITF-2357) concentrations of 0 nM, 125 nM, 250 nM, 500 nM, and 1000 nM. In the second group, Givinostat of relevant concentrations is added concomitantly with 100 nM of LPS solution. Three replicates are performed for each group. After inoculation at 37°C and 5% CO2 for 24 h, each well (100 μL) is incubated with 10 μL of CCK-8 solution. The plates are incubated at 37°C for 1 h and the absorbance is measured at 450 nm using a microplate reader[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    C57BL/6 mice are housed in the animal facility for at least 5 days before use. For the comparison study, Givinostat (ITF2357) at 10 mg/kg is administered orally, and ITF3056 is injected intraperitoneally. One hour after administration of the compounds, the animals are treated intraperitoneally with LPS from Salmonella typhimurium at a dose of 2.5 mg/kg. 90 min after the LPS treatment, mice are sacrificed, and sera are collected and stored at -80°C until further analysis of cytokine productions.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3725 mL 11.8627 mL 23.7254 mL 59.3134 mL
    5 mM 0.4745 mL 2.3725 mL 4.7451 mL 11.8627 mL
    10 mM 0.2373 mL 1.1863 mL 2.3725 mL 5.9313 mL
    15 mM 0.1582 mL 0.7908 mL 1.5817 mL 3.9542 mL
    20 mM 0.1186 mL 0.5931 mL 1.1863 mL 2.9657 mL
    25 mM 0.0949 mL 0.4745 mL 0.9490 mL 2.3725 mL
    30 mM 0.0791 mL 0.3954 mL 0.7908 mL 1.9771 mL
    40 mM 0.0593 mL 0.2966 mL 0.5931 mL 1.4828 mL
    50 mM 0.0475 mL 0.2373 mL 0.4745 mL 1.1863 mL
    60 mM 0.0395 mL 0.1977 mL 0.3954 mL 0.9886 mL
    80 mM 0.0297 mL 0.1483 mL 0.2966 mL 0.7414 mL
    100 mM 0.0237 mL 0.1186 mL 0.2373 mL 0.5931 mL
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    Givinostat Related Classifications

    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.

    Keywords:

    Givinostat497833-27-9ITF-2357ITF2357ITF 2357HDACHistone deacetylasesInhibitorinhibitorinhibit

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