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

Givinostat hydrochloride  (Synonyms: ITF-2357 hydrochloride)

Cat. No.: HY-14842A Purity: 98.06%
COA
SDS
Handling Instructions Technical Support

Givinostat (ITF-2357) hydrochloride is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat hydrochloride can penetrate the blood-brain barrier (BBB)..

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

CAS No. : 199657-29-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Givinostat hydrochloride:

Givinostat hydrochloride Related Antibodies

Top Publications Citing Use of Products

    Givinostat hydrochloride 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 hydrochloride 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 hydrochloride 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) hydrochloride is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat hydrochloride can penetrate the blood-brain barrier (BBB).[1][2][3][4].

    IC50 & Target[1][3]

    hHDAC3

    157 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)

    HD1-B

    7.5 nM (IC50)

    HD1-A

    16 nM (IC50)

    HD2

    10 nM (IC50)

    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 reduces IL-1β secretion more than 70%. Givinostat 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]. Givinostat (ITF-2357) inhibits JS-1 cell proliferation in a concentration-dependent manner in the CCK-8 assay. Treatment with Givinostat (ITF-2357) ≥500 nM is associated with significant inhibition of JS-1 cell proliferation. Also, the cell inhibition rate significantly differs between the group cotreated with Givinostat (ITF-2357) ≥250 nM plus LPS and the group without LPS treatment[2].

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

    Givinostat hydrochloride Related Antibodies
    In Vivo

    Givinostat (ITF2357) at 10 mg/kg is used as a positive control and reduces serum TNFα by 60%. Pretreatment of Givinostat (ITF-2357) 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[1].

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

    457.95

    Formula

    C24H28ClN3O4
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(OCC1=CC=C2C=C(CN(CC)CC)C=CC2=C1)NC3=CC=C(C(NO)=O)C=C3.[H]Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 175 mg/mL (382.14 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 2.1836 mL 10.9182 mL 21.8364 mL
    5 mM 0.4367 mL 2.1836 mL 4.3673 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

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

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation
    References
    Kinase Assay
    [1]

    Recombinant human HDAC enzymes (HDAC1- HDAC11) are used. Activity of HDAC1, HDAC2, HDAC3, HDAC6, HDAC10 and HDAC11 is assayed using the Fluor de Lys deacetylase substrate. HDAC8 activity is assayed using Fluor de Lys Green deacetylase substrate. N-Trifluoroacetyl-L-lysine is used to assay activity of HDAC4, HDAC5, HDAC7 and HDAC9. Recombinant enzymes are preincubated with Givinostat (ITF2357) or ITF3056 at 30°C in a volume of 25 μL in wells of a microtiter plate. After a brief incubation, 25 μL of substrate is added, and the fluorescent signal is generated by the addition of 50 μL of developer containing 2 μM Trichostatin A. For each assay, the amount of enzyme, incubation times, assay buffer, and concentration of the substrates are optimized. Positive control for enzyme activity consisted of enzyme plus substrate without Givinostat or ITF3056. The fluorescence signal is detected using a Victor multilabel plate reader[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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 concentrations of 0 nM, 125 nM, 250 nM, 500 nM, and 1000 nM. In the second group, Givinostat (ITF-2357) 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 Givinostat (ITF-2357) 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 (sealed storage, away from moisture). 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 2.1836 mL 10.9182 mL 21.8364 mL 54.5911 mL
    5 mM 0.4367 mL 2.1836 mL 4.3673 mL 10.9182 mL
    10 mM 0.2184 mL 1.0918 mL 2.1836 mL 5.4591 mL
    15 mM 0.1456 mL 0.7279 mL 1.4558 mL 3.6394 mL
    20 mM 0.1092 mL 0.5459 mL 1.0918 mL 2.7296 mL
    25 mM 0.0873 mL 0.4367 mL 0.8735 mL 2.1836 mL
    30 mM 0.0728 mL 0.3639 mL 0.7279 mL 1.8197 mL
    40 mM 0.0546 mL 0.2730 mL 0.5459 mL 1.3648 mL
    50 mM 0.0437 mL 0.2184 mL 0.4367 mL 1.0918 mL
    60 mM 0.0364 mL 0.1820 mL 0.3639 mL 0.9099 mL
    80 mM 0.0273 mL 0.1365 mL 0.2730 mL 0.6824 mL
    100 mM 0.0218 mL 0.1092 mL 0.2184 mL 0.5459 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Givinostat hydrochloride 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:

    Givinostat199657-29-9ITF-2357ITF2357ITF 2357HDACHistone deacetylasesInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Requested Quantity *

    Applicant Name *

    		 

    Salutation

    Email Address *

    		 

    Phone Number *

    Department

    		 

    Organization Name *

    City

    State

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Givinostat hydrochloride
    Cat. No.:
    HY-14842A
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    English - EN (394 KB) Français - FR (394 KB) Deutsch - DE (394 KB) Norwegian - NO (394 KB) Español - ES (394 KB) Swedish - SV (394 KB) Italian - IT (394 KB) Korean - KR (394 KB) Portuguese - PT (394 KB)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.