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

Givinostat  (Synonyms: ITF-2357)

Cat. No.: HY-14842 Purity: 98.16%
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Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively.

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

Givinostat Chemical Structure

Givinostat Chemical Structure

CAS No. : 497833-27-9

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5 mg USD 90 In-stock
10 mg USD 160 In-stock
25 mg USD 350 In-stock
50 mg USD 560 In-stock
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Givinostat:

Givinostat Related Antibodies

Top Publications Citing Use of Products

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.

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)

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 : 250 mg/mL (593.13 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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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
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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