Givinostat hydrochloride
Based on 12 publication(s) in Google Scholar
Givinostat (ITF-2357) hydrochloride is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat hydrochloride can penetrate the blood-brain barrier (BBB)..
For research use only. We do not sell to patients.
- Purity : 98.06%
- CAS No.: 199657-29-9
- Formula: C24H28ClN3O4
- Molecular Weight:457.95
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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HY-14842
GivinostatHDAC Inhibitor -
HY-14842B
Givinostat hydrochloride monohydrate -
HY-109015
TucidinostatHDAC Inhibitor -
HY-100508
ITSA-1HDAC activator -
HY-N0931
Santacruzamate AHDAC2 Inhibitor -
HY-18361
TMP195HDAC Inhibitor -
HY-19327
ACY-738HDAC6 Inhibitor -
HY-15994
CitarinostatHDAC6 Inhibitor -
HY-111342
HDAC8-IN-1HDAC8 Inhibitor -
HY-100748
ZabadinostatHDAC1/2/3 Inhibitor -
HY-111400
SR-4370HDAC Inhibitor -
HY-100871
WT-161HDAC6 Inhibitor
Publications Citing Use of MedChemExpress (MCE) Givinostat hydrochloride
More- J Am Chem Soc. 2024 Oct 16;146(41):28282-28295. [Abstract]
- Cell Death Dis. 2020 Sep 15;11(9):753. [Abstract]
- Acta Pharmacol Sin. 2022 Feb;43(2):457-469. [Abstract]
- J Orthop Translat. 2021 Jun 1:29:106-112. [Abstract]
- Cell Prolif. 2021 Jul;54(7):e13072. [Abstract]
- Commun Biol. 2021 Oct 29;4(1):1235. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- Int J Parasitol Drugs Drug Resist. 2026 May 17;31:100649.
- Neuroscience. 2021 Jun 15:465:38-45. [Abstract]
- bioRxiv. 2025 January 15.
- Patent. US20240252638A1.
- SSRN. 2024 Mar 13.
Customer Validation & Images
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RT-PCR
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WB
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WB
Biological Activity
Description
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hHDAC3 157 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) |
HD1-B 7.5 nM (IC50) |
HD1-A 16 nM (IC50) |
HD2 10 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 reduces IL-1β secretion more than 70%. Givinostat 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]. Givinostat (ITF-2357) inhibits JS-1 cell proliferation in a concentration-dependent manner in the CCK-8 assay. Treatment with Givinostat (ITF-2357) ≥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 (ITF-2357) ≥250 nM plus LPS and the group without LPS treatment[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 199657-29-9
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Appearance Solid
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Molecular Weight 457.95
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Formula C24H28ClN3O4
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Color White to off-white
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SMILES
O=C(OCC1=CC=C2C=C(CN(CC)CC)C=CC2=C1)NC3=CC=C(C(NO)=O)C=C3.[H]Cl
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Synonyms
ITF-2357 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (12)
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Journal Impact Factor
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Most Recent
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J Am Chem Soc
Inhibitor Development for α-Synuclein Fibril's Disordered Region to Alleviate Parkinson's Disease Pathology. [Abstract]2024 Oct 16;146(41):28282-28295. PMID: 39327912 -
Cell Death Dis
Checkpoint regulator B7x is epigenetically regulated by HDAC3 and mediates resistance to HDAC inhibitors by reprogramming the tumor immune environment in colorectal cancer. [Abstract]2020 Sep 15;11(9):753. PMID: 32934224 -
Acta Pharmacol Sin
2022 Feb;43(2):457-469. PMID: 33850273 -
J Orthop Translat
Personalized medicine modality based on patient-derived xenografts from a malignant transformed GCTB harboring H3F3A G34W mutation. [Abstract]2021 Jun 1:29:106-112. PMID: 34136349 -
Cell Prolif
EZH2-mediated inhibition of KLF14 expression promotes HSCs activation and liver fibrosis by downregulating PPARγ. [Abstract]2021 Jul;54(7):e13072. PMID: 34031939
Givinostat hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2021 Jul;54(7):e13072. [Abstract]
The HSCs shown were treated with DNMTs inhibitors (5-azacytidine, 2 μmol/L), G9a inhibitors (UNC0642, 2 μmol/L), and pan-HDAC inhibitor Givinostat (ITF-2357, 100 nmol/L) for 48 hours, or with EZH2 inhibitors (EPZ-6438, 10 μmol/L) for 72 hours. KLF14 expression was analyzed by RT-qPCR.
Givinostat hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2021 Jul;54(7):e13072. [Abstract]
The HSCs shown were treated with DNMT inhibitors (5-azacytidine, 2 μmol/L), G9a inhibitors (UNC0642, 2 μmol/L), and pan-HDAC inhibitor Givinostat (ITF-2357, 100 nmol/L) for 48 hours, or with EZH2 inhibitors (EPZ-6438, 10 μmol/L) for 72 hours. KLF14 expression was detected by Western blotting.
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Commun Biol
LIFR inhibition enhances the therapeutic efficacy of HDAC inhibitors in triple negative breast cancer. [Abstract]2021 Oct 29;4(1):1235. PMID: 34716410
Givinostat hydrochloride purchased from MedChemExpress. Usage Cited in: Commun Biol. 2021 Oct 29;4(1):1235. [Abstract]
TNBC model cells (MDA-MB-231 and BT-549) were treated with indicated HDACi (Vorinostat: 10 µM; Panobinostat: 1 µM; Romidepsin: 1 µM; Givinostat: 1 µM) for 24 h and expression of LIFR, p-STAT3(Y705), and STAT3 were determined using Western blotting.
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J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
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Neuroscience
Treatment with Non-specific HDAC Inhibitors Administered after Disease Onset does not Delay Evolution in a Mouse Model of Progressive Multiple Sclerosis. [Abstract]2021 Jun 15:465:38-45. PMID: 33862148 -
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Solvent & Solubility
In Vitro:
DMSO : 175 mg/mL (382.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[2]. 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. [Content Brief]
[3]. Wang YG, et al. Givinostat inhibition of hepatic stellate cell proliferation and protein acetylation. World J Gastroenterol. 2015 Jul 21;21(27):8326-39. [Content Brief]
[4]. Taiarol L, et al. Givinostat-Liposomes: Anti-Tumor Effect on 2D and 3D Glioblastoma Models and Pharmacokinetics. Cancers (Basel). 2022 Jun 16;14(12):2978. [Content Brief]
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 (sealed storage, away from moisture). 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 |
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| DMSO | 1 mM | 2.1836 mL | 10.9182 mL | 21.8364 mL | 54.5911 mL |
| 5 mM | 0.4367 mL | 2.1836 mL | 4.3673 mL | 10.9182 mL | |
| 10 mM | 0.2184 mL | 1.0918 mL | 2.1836 mL | 5.4591 mL | |
| 15 mM | 0.1456 mL | 0.7279 mL | 1.4558 mL | 3.6394 mL | |
| 20 mM | 0.1092 mL | 0.5459 mL | 1.0918 mL | 2.7296 mL | |
| 25 mM | 0.0873 mL | 0.4367 mL | 0.8735 mL | 2.1836 mL | |
| 30 mM | 0.0728 mL | 0.3639 mL | 0.7279 mL | 1.8197 mL | |
| 40 mM | 0.0546 mL | 0.2730 mL | 0.5459 mL | 1.3648 mL | |
| 50 mM | 0.0437 mL | 0.2184 mL | 0.4367 mL | 1.0918 mL | |
| 60 mM | 0.0364 mL | 0.1820 mL | 0.3639 mL | 0.9099 mL | |
| 80 mM | 0.0273 mL | 0.1365 mL | 0.2730 mL | 0.6824 mL | |
| 100 mM | 0.0218 mL | 0.1092 mL | 0.2184 mL | 0.5459 mL |
Givinostat hydrochloride Related Classifications
HY-14842A Related Classifications
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