Givinostat Inhibitor CAS No. 732302-99-7

Cat. No.	Name	Size	Price
KI1228	Givinostat	5 mg	$272
	Givinostat	10 mg	$512
	Givinostat	50 mg	$1552
	Givinostat	200 mg	$3952

Chemical Characteristic

Product Name	Givinostat
Synonyms	ITF2357
CAS No.	732302-99-7
Molecular Weight	475.97
Formula	C₂₄H₂₇N₃O₄.HCl.H₂O
Chemical Name	diethyl-[[6-[[4-(hydroxycarbamoyl)phenyl]carbamoyloxymethyl]naphthalen-2-yl]methyl]azanium;chloride;hydrate
Smiles	C(=O)(Nc1ccc(cc1)C(=O)NO)OCc1cc2c(cc1)cc(cc2)CN(CC)CC Cl O
Chemical Structure

Biological activities

Givinostat is a potent inhibitor of HDAC with IC50 values of 10, 7.5 and 16 nM for HD2, HD1-B and HD1-A, respectively. In lipopolysaccharide (LPS)-stimulated cultured human peripheral blood mononuclear cells (PBMCs), givinostat reduces the releases of tumor necrosis factor-α (TNFα), intracellular interleukin (IL)-1α, IL-1β, and interferon-γ (IFNγ) with IC50 values ranging from 10 to 25 nM. Using the combination of IL-12 plus IL-18, givinostat reduces IFNγ and IL-6 production by 50% at 12.5 to 25 nM, independent of decreased IL-1 or TNFα.^[1] In vitro, givinostat induces apoptosis in multiple myeloma (MM) cell lines (including RPMI8226, NCI-H929, JJN3 and KMS 11) and acute myelogenous leukemia (AML) cell lines (including HL-60, THP-1, U937 and KASUMI) with a mean IC50 value of 200 nM. In more physiological conditions, givinostat is still strongly cytotoxic for the IL-6-dependent MM cell line CMA-03, or for AML samples maximally stimulated by co-culture on mesenchymal stromal cells (MSCs), but not for the MSCs themselves.^[2] Oral administration of givinostat (1 to 10 mg/kg) to mice reduces LPS-induced serum TNFα and IFNγ by more than 50%.^[1] Givinostat (10 mg/kg) significantly prolongs survival of severe combined immunodeficient mice inoculated with the AML-PS in vivo passaged cell line.^[2] In mice normalized streptozotocin-induced hyperglycemia, givinostat (1.25-2.5 mg/kg) returns serum nitrite levels to nondiabetic values, improves islet function and increases glucose clearance from 14% to 50%.^[3]

Protocols

In vivo: Givinostat is added to water and heated to 90 °C until dissolved.^[1]

References

[1] 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, 11(1-12): 1-15. [2] Golay J, et al. The histone deacetylase inhibitor ITF2357 has anti-leukemic activity in vitro and in vivo and inhibits IL-6 and VEGF production by stromal cells. Leukemia. 2007, 21(9): 1892-1900. [3] Eli C Lewis, et al. The Oral Histone Deacetylase Inhibitor ITF2357 Reduces Cytokines and Protects Islet β Cells In Vivo and In Vitro. Mol Med. 2011, 17(5-6): 369-377.

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