Givinostat (ITF2357)

Catalog No.S2170

Givinostat (ITF2357) Chemical Structure

Molecular Weight(MW): 475.97

Givinostat (ITF2357) is a potent HDAC inhibitor for maize HD2, HD1B and HD1A with IC50 of 10 nM, 7.5 nM and 16 nM in cell-free assays. Phase 2.

Size Price Stock Quantity  
In DMSO USD 320 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 12 Publications

4 Customer Reviews

  • Cells were treated with indicated HDAC inhibitors for 4 days and then cultured without drug for an additional 4 days. On day 8, HDAC inhibitors were added back to the culture for another 4 days. The percentage of GFP-positive cells was measured at days 4, 8 and 12. The concentrations of HDAC inhibitors used for the experiments are as follows: vorinostat, 1 uM; TsA, 200 nM; oxamflatin, 1 uM; scriptaid, 1 uM; belinostat, 200 nM; and givinostat, 200 nM. The fraction of GFP-positive cells was measured by flow cytometry at the indicated timepoints. The effect of HDAC inhibitors or anti-CD3 plus anti-CD28 antibodies over time was normalized to the effect of anti-CD3 plus anti-CD28 antibodies at day 2. Error bars represent SEM, n = 3. APHA, 3-(1-methyl-4-phenylacetyl-1H-2-pyrrolyl)-N-hydroxypropenamide.

    J Antimicrob Chemother 2014 69(1), 28-33. Givinostat (ITF2357) purchased from Selleck.

    Representative confocal images of motor axons directly posterior to brains in third instar larvae co-expressing a synaptotagmin-e-GFP fusion protein (syt-eGFP) along with dTip60E431Q under the control of the pan neuronal elav-GAL4 driver reared on food treated with either no drug, ms-275, Givinostat.

    J Neurosci 2013 33(17), 7535-47. Givinostat (ITF2357) purchased from Selleck.

  • Western blot analysis of acetylated histone and histone. 0-10μM ITF2357 was added.



    Dr. Zhang of Tianjin Medical University. Givinostat (ITF2357) purchased from Selleck.

    (e–h) Cytokine secretion. Pancreatic islets were isolated from 12-week (wk)-old non-diabetic, untreated diabetic or givinostat (Givi)-treated diabetic NOD-huCD3ε mice (after 3–4 weeks of treatment) (n = 5–9 per group). Islets were cultured at 37°C for 48 h and supernatant fractions were collected. Concentrations of (e) IL-1β, (f) IL-6, (g) TNF-α and (h) IL-10 were determined by ELISA; *p < 0.05.

    Diabetologia, 2018, 61(2):389-398. Givinostat (ITF2357) purchased from Selleck.

Purity & Quality Control

Choose Selective HDAC Inhibitors

Biological Activity

Description Givinostat (ITF2357) is a potent HDAC inhibitor for maize HD2, HD1B and HD1A with IC50 of 10 nM, 7.5 nM and 16 nM in cell-free assays. Phase 2.
Features An orally active, potent inhibitor of histone deacetylases (HDACs).
HD1-B [1]
(Cell-free assay)
HD2 [1]
(Cell-free assay)
HD1-A [1]
(Cell-free assay)
7.5 nM 10 nM 16 nM
In vitro

In LPS-stimulated cultured human peripheral blood mononuclear cells (PBMCs), ITF2357 reduces the release of TNFα, IL-1α, IL-1β, and IFNγ, with IC50 of 10-25 nM, respectively. Using the combination of IL-12 plus IL-18, ITF2357 reduces IFNγ and IL-6 production with IC50 of 12.5-25 nM, independent of decreased IL-1 or TNFα. [1] ITF2357 is cytotoxic in multiple myeloma (MM) cell lines (RPMI8226, NCI-H929, JJN3, KMS 11, KMS 12, KMS 18, and KMS 20) and acute myelogenous leukemia (AML) cell lines (HL-60, THP-1, U937, KASUMI, KG-1, and TF-1), with IC50 of 200 nM. ITF2357 activates the intrinsic apoptotic pathway, upregulates p21 and downmodulates Bcl-2 and Mcl-1. ITF2357 inhibits the production of IL-6, VEGF, and IFNγ in mesenchymal stromal cells (MSCs) by 80-95%. [2] ITF2357 favors β-cell survival during inflammatory conditions. ITF2357 at concentrations of 25 and 250 nM increases islet cell viability, enhances insulin secretion, inhibits release of MIP-1α and MIP-2, reduces NO production and decreases apoptosis rates. [3]

Methods Test Index PMID
Western blot
SOD2(K68) / SOD2 / p53(K120) / p53(K382) / p53 / p65(K310) / p65; 

PubMed: 26217084     

Effects of givinostat on the post-translational modifications of superoxide dismutase (SOD)2, p53, nuclear factor (NF)-κB, and p65 were analyzed by Western blotting. SOD2 (acetyl K68) acetylation was upregulated, while the expression profile of SOD2 protein showed no significant change. The ratios show a significant difference when compared with those in the control group, in particular at 24 h. Similarly, acetylation of NF-κB p65 (acetyl K310) was upregulated, while its protein expression showed no significant change. There were no obvious changes in the expression profiles of p53, p53 (acetyl K382), and p53 (acetyl K120);

pERK / ERK / pJNK / JNK / pp38 / p38 ; 

PubMed: 26217084     

Expression of extracellular signal-regulated kinase (ERK)1/2, phosphorylated ERK1/2, p38, and phosphorylated p38 was upregulated after lipopolysaccharide (LPS) treatment; in contrast, givinostat inhibited the upregulated expression of phosphorylated ERK1/2 and phosphorylated P38 induced by LPS in a time-dependent manner, while no obvious effect on c-Jun N-terminal kinase (JNK)1/2 and phosphorylated JNK1/2 was found.

PARP / Cleaved PARP / Pro-Caspase 7 / Cleaved caspase 7 / Pro-caspase 3 / Cleaved Caspase 3; 

PubMed: 28050230     

Western blotting of cultured cells treated with or without Givinostat (0.25μM) to reveal activation of apoptotic cascade in Ph+ leukemia cells. The data represents one of three repeats. The cleaved forms of caspase-3 were at 17 kDa, caspase-7 at 20 kDa, and PARP1 at 85 KDa. PARP1, Poly (ADP-Ribose) Polymerase 1; C7 Caspase 7; C3: Caspase 3; GAPDH: Glyceraldehyde-3-Phosphate Dehydrogenase.

CHK1 / p53 / p21; 

PubMed: 28050230     

Western blotting of cultured cells treated with or without Givinostat (0.25μM) to reveal p53 integrality in SUP-B15 (left) and K562 (right) at 24 to 72hrs. GAPDH: Glyceraldehyde-3-Phosphate Dehydrogenase.

α-SMA / TGF-β1 / VEGF ; 

PubMed: 26217084     

In JS-1 cells, treatment with givinostat for 24 h or 48 h significantly suppressed expression of α-smooth muscle actin (SMA), transforming growth factor (TGF)-β1 and Vascular endothelial growth factor (VEGF) compared with the control group. aP < 0.05, bP < 0.01 vs control group.

26217084 28050230
In vivo ITF2357 (1-10 mg/kg) reduces LPS-induced serum TNFα and IFNγ by more than 50% in mice. Anti-CD3-induced cytokines are not suppressed by ITF2357 in PBMCs in the circulation in mice. In concanavalin-A-induced hepatitis, ITF2357 (1 or 5 mg/kg) significantly reduces liver damage. [1] ITF2357 (10 mg/kg) significantly prolongs survival of severe combined immunodeficient mice inoculated with the AML-PS in vivo passaged cell line. [2] In a mouse model of closed head injury (CHI), ITF2357 (10 mg/kg) improves neurobehavioral recovery, decreases neuronal degeneration, reduces lesion volume, and induces glial apoptosis. [4]


Kinase Assay:[1]
+ Expand

Enzymatic Assay for HDAC Inhibitory Activity of Synthetic Compounds:

The assay is performed by adding 100 μL substrate (2×105 cpm), 40 μL buffer (50 mM Tris-HCl, pH 8.0, 750 mM NaCl, 5 mM PMSF, 50% glycerol) and 95 μL distilled water to the crude cellular extract (5 μL). ITF2357 (50 μL) is added to test for HDAC inhibition. The mixture is incubated overnight at room temperature and the reaction quenched by adding 50 μL of a solution containing 259 μL 37% HCl and 28 μL acetic acid in 1 mL distilled water. The [3H]acetyl residues released from the substrate are separated by organic extraction with 600 μL of ethyl acetate, 200 μL of the organic phase is added to standard scintillation fluid, and radioactivity is measured by a beta-counter. Inhibition of HDACs is expressed as the concentration inhibiting 50% of the control activity (by comparing the radioactivity of the samples containing inhibitors to that of the control containing cellular crude extract alone).
Cell Research:[1]
+ Expand
  • Cell lines: peripheral blood mononuclear cells (PBMCs)
  • Concentrations: 1 nM - 1 μM
  • Incubation Time: 24 hours
  • Method: After washing, the isolated PBMCs are resuspended in RPMI containing 5% FCS at 5×106/mL, added to a 50-mL conical polypropylene tube, and placed at 4 °C overnight. The PBMCs are resuspended the next morning and added to a 96-well flat microtiter plate (100 μL per well). ITF2357 is then added for inhibition studies, and the plates are incubated at 37 °C for 1 hour, after which the cells are stimulated with LPS or other stimulants in a final volume of 200 μL per well. The supernatants are removed after incubation at 37 °C for 24 hours, and frozen at -80 °C until assayed for cytokines.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Mice. For LPS induction of serum cytokines: BALB/c; for anti-CD3-induced cytokines: CD1; for concanavalin A (Con A)-induced acute hepatitis: BALB/c or C57Bl6.
  • Formulation: Dissolved in water
  • Dosages: 0.01-50 mg/kg
  • Administration: By gavage in 100 μL water.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 95 mg/mL (199.59 mM)
Ethanol 3 mg/mL (6.3 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 475.97


CAS No. 732302-99-7
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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

  • Mass
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

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 in 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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03238235 Recruiting Becker Muscular Dystrophy Italfarmaco December 12 2017 Phase 2
NCT03238235 Recruiting Becker Muscular Dystrophy Italfarmaco December 12 2017 Phase 2
NCT03373968 Recruiting Duchenne Muscular Dystrophy Italfarmaco|Cromsource October 24 2017 Phase 2|Phase 3
NCT03373968 Recruiting Duchenne Muscular Dystrophy Italfarmaco|Cromsource October 24 2017 Phase 2|Phase 3
NCT02851797 Recruiting Duchenne Muscular Dystrophy Italfarmaco|Syneos Health June 1 2017 Phase 3
NCT02851797 Recruiting Duchenne Muscular Dystrophy Italfarmaco|Syneos Health June 1 2017 Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

HDAC Signaling Pathway Map

HDAC Inhibitors with Unique Features

Related HDAC Products5

Tags: buy Givinostat (ITF2357) | Givinostat (ITF2357) supplier | purchase Givinostat (ITF2357) | Givinostat (ITF2357) cost | Givinostat (ITF2357) manufacturer | order Givinostat (ITF2357) | Givinostat (ITF2357) distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID