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Givinostat hydrochloride

Catalog No. T6279L CAS 199657-29-9

Synonyms: ITF2357 hydrochloride, Givinostat HCl, ITF2357, ITF 2357, ITF-2357, ITF2357 HCl

Givinostat hydrochloride (ITF2357 hydrochloride) is an inhibitor of HDAC with IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat hydrochloride exhibits anti-inflammatory, anti-angiogenic, and antineoplastic activities.

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Givinostat hydrochloride Chemical Structure

Givinostat hydrochloride, CAS 199657-29-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 67.00
2 mg	In stock	$ 95.00
5 mg	In stock	$ 136.00
10 mg	In stock	$ 227.00
25 mg	In stock	$ 477.00
50 mg	In stock	$ 698.00
100 mg	In stock	$ 993.00
500 mg	In stock	$ 1,990.00
1 mL * 10 mM (in DMSO)	In stock	$ 219.00

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Purity: 98.01%

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Description	Givinostat hydrochloride (ITF2357 hydrochloride) is an inhibitor of HDAC with IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat hydrochloride exhibits anti-inflammatory, anti-angiogenic, and antineoplastic activities.
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 hydrochloride inhibits JS-1 cell proliferation in a concentration-dependent manner. Givinostat hydrochloride (≥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 hydrochloride ≥250 nM plus LPS and the group without LPS treatment[3]. Givinostat hydrochloride (25, 50, and 100 nM) reduces IL-1β secretion more than 70%. Givinostat hydrochloride 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, but at 100 and 200 nM, there is no reduction[4].
In vivo	Givinostat hydrochloride (10 mg/kg) reduces serum TNFα by 60%. Pretreatment of Givinostat hydrochloride (0.1 mg/kg) significantly reduces the circulating TNFα by nearly 90%[4].

Synonyms	ITF2357 hydrochloride, Givinostat HCl, ITF2357, ITF 2357, ITF-2357, ITF2357 HCl
Molecular Weight	457.95
Formula	C24H28ClN3O4
CAS No.	199657-29-9

Storage

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

Solubility Information

DMSO: 27.5 mg/mL (60.05 mM)

References and Literature

1. Zappasodi R, et al. Pleiotropic antitumor effects of the pan-HDAC inhibitor ITF2357 against c-Myc-overexpressing human B-cell non-Hodgkin lymphomas. Int J Cancer. 2014 Nov 1;135(9):2034-45. 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. 4. 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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Histone Modification Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library Clinical Compound Library DNA Damage & Repair Compound Library

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Keywords

Givinostat hydrochloride 199657-29-9 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC ITF2357 hydrochloride inhibit Givinostat HCl Givinostat Hydrochloride ITF-2357 Hydrochloride Histone deacetylases ITF2357 ITF 2357 Hydrochloride Givinostat ITF 2357 ITF-2357 Inhibitor ITF2357 Hydrochloride ITF2357 HCl inhibitor

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