Givinostat (hydrochloride monohydrate)
Based on 12 publication(s) in Google Scholar
Givinostat hydrochloride monohydrate (ITF-2357 hydrochloride monohydrate) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat hydrochloride monohydrate can penetrate the blood-brain barrier (BBB).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.63%
- CAS 番号: 732302-99-7
- 分子式: C24H30ClN3O5
- 分子量:475.97
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Givinostat hydrochloride monohydrate
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
生物活性
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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) |
Givinostat (ITF2357) suppresses total LPS-induced IL-1β production robustly compared with the reduction by ITF3056. At 25, 50, and 100 nM, Givinostat reduced IL-1β secretion more than 70%. Givinostat (ITF2357) 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 (ITF2357), but at 100 and 200 nM, there is no reduction[1]. As shown by the CCK-8 assay, Givinostat (ITF2357) inhibits JS-1 cell proliferation in a concentration-dependent manner. Treatment with Givinostat (ITF2357) ≥500 nM is associated with significant inhibition of JS-1 cell proliferation (P<0.01). Also, the cell inhibition rate significantly differs between the group cotreated with Givinostat ≥250 nM plus LPS and the group without LPS treatment (same Givinostat concentration) (P<0.05)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 732302-99-7
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性状 Solid
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分子量 475.97
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分子式 C24H30ClN3O5
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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.O
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別名
ITF-2357 hydrochloride monohydrate
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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 monohydrate 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 monohydrate 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 monohydrate 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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溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (210.10 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 2.94 mg/mL (6.18 mM; ultrasonic and warming and heat to 60°C)
* "≥" means soluble, but saturation unknown.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.17 mg/mL (4.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.17 mg/mL (4.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
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 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
C57BL/6 mice are housed in the animal facility for at least 5 days before use. For the comparison study, Givinostat (ITF2357) at 10 mg/kg is administered orally, and Givinostat (ITF2357) is injected intraperitoneally. One hour after administration of the compounds, the animals are treated intraperitoneally with LPS from Salmonella typhimurium at a dose of 2.5 mg/kg. 90 min after the LPS treatment, mice are sacrificed, and sera are collected and stored at -80°C until further analysis of cytokine productions.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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参考文献
[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]. 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]
[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. [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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.1010 mL | 10.5049 mL | 21.0097 mL | 52.5243 mL |
| 5 mM | 0.4202 mL | 2.1010 mL | 4.2019 mL | 10.5049 mL | |
| DMSO | 10 mM | 0.2101 mL | 1.0505 mL | 2.1010 mL | 5.2524 mL |
| 15 mM | 0.1401 mL | 0.7003 mL | 1.4006 mL | 3.5016 mL | |
| 20 mM | 0.1050 mL | 0.5252 mL | 1.0505 mL | 2.6262 mL | |
| 25 mM | 0.0840 mL | 0.4202 mL | 0.8404 mL | 2.1010 mL | |
| 30 mM | 0.0700 mL | 0.3502 mL | 0.7003 mL | 1.7508 mL | |
| 40 mM | 0.0525 mL | 0.2626 mL | 0.5252 mL | 1.3131 mL | |
| 50 mM | 0.0420 mL | 0.2101 mL | 0.4202 mL | 1.0505 mL | |
| 60 mM | 0.0350 mL | 0.1751 mL | 0.3502 mL | 0.8754 mL | |
| 80 mM | 0.0263 mL | 0.1313 mL | 0.2626 mL | 0.6566 mL | |
| 100 mM | 0.0210 mL | 0.1050 mL | 0.2101 mL | 0.5252 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Givinostat hydrochloride monohydrate 関連分類
HY-14842B 関連分類
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