Home Tools

Givinostat

Catalog No. T36629 CAS 497833-27-9

Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Givinostat, CAS 497833-27-9

Please contact us for prices and availability for the specification of product you are interested at.
Product consultation

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively.
Targets&IC50	HD1-B:7.5 nM (IC50), HDAC10 (human):340 nM (IC50), HDAC6 (human):315 nM (IC50), HDAC3 (human):157 nM (IC50), HD2:10 nM (IC50), HDAC9 (human):541 nM (IC50), HDAC4 (human):1059 nM (IC50), HD1-A:16 nM (IC50), HDAC11 (human):292 nM (IC50), HDAC7 (human):524 nM (IC50), HDAC2 (human):325 nM (IC50), HDAC8 (human):854 nM (IC50), HDAC1 (human):198 nM (IC50), HDAC5 (human):532 nM (IC50)
In vitro	Givinostat (ITF2357) effectively suppresses IL-1β production induced by LPS, achieving a greater than 70% reduction in IL-1β secretion at concentrations of 25, 50, and 100 nM, outperforming ITF3056. It also inhibits IL-6 production in PBMCs triggered by TLR agonists and the combination of IL-12 plus IL-18, with a 50% decrease in IL-6 secretion at 50 nM, although no further reduction is observed at higher concentrations of 100 and 200 nM. Additionally, Givinostat significantly inhibits JS-1 cell proliferation in a concentration-dependent manner, with concentrations ≥500 nM showing substantial inhibition (P<0.01). Notably, cells co-treated with Givinostat ≥250 nM plus LPS exhibit a significantly higher inhibition rate compared to those treated without LPS at the same Givinostat concentration (P<0.05).
In vivo	Givinostat (ITF2357), used as a positive control at a dose of 10 mg/kg, effectively decreased serum TNFα levels by 60%. Notably, pretreatment with ITF3056, starting at a dosage of 0.1 mg/kg, significantly lowered circulating TNFα levels by up to 90%. To induce a substantial raise in serum IL-1β production, an elevated LPS dose (10 mg/kg) is administered, followed by blood collection after 4 hours. Furthermore, lower doses of Givinostat (ITF-2357) at 1 or 5 mg/kg resulted in a 22% and a 40% reduction in TNFα levels, respectively.
Cell Research	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].

Molecular Weight	421.497
Formula	C24H27N3O4
CAS No.	497833-27-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: Soluble

References and Literature

1. Li S, et al. Specific inhibition of histone deacetylase 8 reduces gene expression and production of proinflammatory cytokines in vitro and in vivo. J Biol Chem. 2015 Jan 23;290(4):2368-78. 2. Wang YG, et al. Givinostat inhibition of hepatic stellate cell proliferation and protein acetylation. World J Gastroenterol. 2015 Jul 21;21(27):8326-39. 3. Leoni F, et al. The histone deacetylase inhibitor ITF2357 reduces production of pro-inflammatory cytokines in vitro and systemic inflammation in vivo. Mol Med. 2005 Jan-Dec;11(1-12):1-15.

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Givinostat 497833-27-9 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.