ACY-738
Based on 7 publication(s) in Google Scholar
ACY-738 is a potent, selective and orally-bioavailable HDAC6 inhibitor, with an IC50 of 1.7 nM; ACY-738 also inhibits HDAC1, HDAC2, and HDAC3, with IC50s of 94, 128, and 218 nM.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 99.92%
- CAS 番号: 1375465-91-0
- 分子式: C14H14N4O2
- 分子量:270.29
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 ACY-738
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Cell Death Dis. 2023 Apr 6;14(4):250. [Abstract]
- Cancer Lett. 2022 Nov 28:549:215911. [Abstract]
- EMBO J. 2025 Aug 20. [Abstract]
- Int Immunopharmacol. 2026 May 1:176:116466. [Abstract]
- J Neurochem. 2026 Jun;170(6):e70493. [Abstract]
- Int J Parasitol Drugs Drug Resist. 2026 May 17;31:100649.
生物活性
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HDAC6 1.7 nM (IC50) |
HDAC1 94 nM (IC50) |
HDAC2 128 nM (IC50) |
HDAC3 218 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 697 | IC50 |
3390 nM
Compound: ACY-738
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Cytotoxicity against human 697 cells after 48 hrs by CellTiter 96 aqueous one solution assay
Cytotoxicity against human 697 cells after 48 hrs by CellTiter 96 aqueous one solution assay
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[PMID: 31710483] |
| Sf9 | IC50 |
2 nM
Compound: ACY-738
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Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method
Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method
|
[PMID: 31710483] |
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 1375465-91-0
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性状 Solid
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分子量 270.29
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分子式 C14H14N4O2
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Color White to off-white
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SMILES
O=C(NO)C(C=N1)=CN=C1NC2(CC2)C3=CC=CC=C3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Cell Death Dis
2023 Apr 6;14(4):250. PMID: 37024472 -
Cancer Lett
HDAC6-dependent deacetylation of AKAP12 dictates its ubiquitination and promotes colon cancer metastasis. [Abstract]2022 Nov 28:549:215911. PMID: 36122629 -
EMBO J
2025 Aug 20. PMID: 40836035 -
Int Immunopharmacol
Central amygdala HDAC6 contributes to visceral hypersensitivity and affective comorbidities in IBS-like rats. [Abstract]2026 May 1:176:116466. PMID: 41797088 -
J Neurochem
Effects of Lysine Deacetylation Inhibition Alone or in Combination With Arimoclomol on TDP-43 Proteinopathy. [Abstract]2026 Jun;170(6):e70493. PMID: 42283221 -
溶剤 & 溶解度
DMSO : ≥ 32 mg/mL (118.39 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.08 mg/mL (7.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (7.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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
Mice are injected i.p. 5 days/week with the vehicle control (DMSO), ACY-738 treatment at 5 mg/kg (low-dose), or ACY-738 treatment at 20 mg/kg (high-dose) beginning at 22-weeks-of-age until euthanasia at 38 weeks-of-age. The total volume injected is 80 μL. Proteinuria and weight are measured every 2 weeks and blood is collected every four weeks for sera analysis. Proteinuria is measured by a standard semi-quantitative test using Siemens Uristix dipsticks. Results are quantified and scored as follows: dipstick reading of 0 mg/dL = 0, trace = 1, 30-100 mg/dL = 2, 100-300 mg/dL = 3, 300-2000 mg/dL = 4, and 2000 + mg/dL = 5[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (278 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Jochems J, et al. Antidepressant-like properties of novel HDAC6-selective inhibitors with improved brain bioavailability. Neuropsychopharmacology. 2014 Jan;39(2):389-400. [Content Brief]
[2]. Regna NL, et al. Specific HDAC6 inhibition by ACY-738 reduces SLE pathogenesis in NZB/W mice. Clin Immunol. 2016 Jan;162:58-73. [Content Brief]
[3]. Mithraprabhu S, et al. Histone deacetylase (HDAC) inhibitors as single agents induce multiple myeloma cell death principally through the inhibition of class I HDAC. Br J Haematol. 2013 Aug;162(4):559-62. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.6997 mL | 18.4986 mL | 36.9973 mL | 92.4932 mL |
| 5 mM | 0.7399 mL | 3.6997 mL | 7.3995 mL | 18.4986 mL | |
| 10 mM | 0.3700 mL | 1.8499 mL | 3.6997 mL | 9.2493 mL | |
| 15 mM | 0.2466 mL | 1.2332 mL | 2.4665 mL | 6.1662 mL | |
| 20 mM | 0.1850 mL | 0.9249 mL | 1.8499 mL | 4.6247 mL | |
| 25 mM | 0.1480 mL | 0.7399 mL | 1.4799 mL | 3.6997 mL | |
| 30 mM | 0.1233 mL | 0.6166 mL | 1.2332 mL | 3.0831 mL | |
| 40 mM | 0.0925 mL | 0.4625 mL | 0.9249 mL | 2.3123 mL | |
| 50 mM | 0.0740 mL | 0.3700 mL | 0.7399 mL | 1.8499 mL | |
| 60 mM | 0.0617 mL | 0.3083 mL | 0.6166 mL | 1.5416 mL | |
| 80 mM | 0.0462 mL | 0.2312 mL | 0.4625 mL | 1.1562 mL | |
| 100 mM | 0.0370 mL | 0.1850 mL | 0.3700 mL | 0.9249 mL |