ACY-738 |
Catalog No.GC19020
One-Click Copy Product Info
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ACY-738 is an orally active and selective inhibitor of histone deacetylase 6 (HDAC6; IC50=1.7nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1375465-91-0
Sample solution is provided at 25 µL, 10mM.
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ACY-738 is an orally active and selective inhibitor of histone deacetylase 6 (HDAC6; IC50=1.7nM). ACY-738 also inhibits the activity of HDAC1 (IC50=94nM), HDAC2 (IC50=128nM), and HDAC3 (IC50=218nM)[1-2]. ACY-738 can be used in research related to neurodegenerative diseases, tumors, inflammation, and autoimmune diseases[3-4].
In vitro, treatment of human multiple myeloma cell lines (such as U266, NCI-H929, etc.) and primary multiple myeloma cells with ACY-738 (5μM or 10μM) for 48 hours significantly induced tumor cell death[5]. Treatment of patient-derived L0, S3, S7 human glioma cells and murine KR158 glioma cells with ACY-738 (0.5–5μM) for 24 hours to 5 days. ACY-738 significantly inhibited tumor cell proliferation[6].
In vivo, intraperitoneal administration of ACY-738 (20mg/kg) to experimental autoimmune encephalomyelitis (EAE) mice on days 9 and 10 post-immunization significantly delayed disease onset, reduced disease severity, and improved short-term memory[7]. Intraperitoneal administration of ACY-738 (5mg/kg or 20mg/kg) to NZB/W F1 mice five days a week for 16 weeks. ACY-738 significantly alleviated the severity of proteinuria and improved mouse survival. ACY-738 increased the proportion of splenic regulatory T cells and reduced the deposition of IgG and C3 immune complexes in the kidneys, as well as SLE-related renal pathological damage[8].
References:
[1] Jochems J, Boulden J, Lee BG, et al. Antidepressant-like properties of novel HDAC6-selective inhibitors with improved brain bioavailability. Neuropsychopharmacology. 2014 Jan;39(2):389-400.
[2] Ren J, Liao X, Vieson MD, et al. Selective HDAC6 inhibition decreases early stage of lupus nephritis by down-regulating both innate and adaptive immune responses. Clin Exp Immunol. 2018 Jan;191(1):19-31.
[3] Majid T, Griffin D, Criss Z 2nd, et al. Pharmocologic treatment with histone deacetylase 6 inhibitor (ACY-738) recovers Alzheimer's disease phenotype in amyloid precursor protein/presenilin 1 (APP/PS1) mice. Alzheimers Dement (N Y). 2015 Oct 11;1(3):170-181.
[4] Xu D, Luo XM, Reilly CM. HDAC6 Deletion Decreases Pristane-induced Inflammation. Immunohorizons. 2024 Sep 1;8(9):668-678.
[5] Mithraprabhu S, Khong T, Jones SS, 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.
[6] Shi P, Hoang-Minh LB, Tian J, et al. HDAC6 Signaling at Primary Cilia Promotes Proliferation and Restricts Differentiation of Glioma Cells. Cancers (Basel). 2021 Apr 1;13(7):1644.
[7] Regna NL, Vieson MD, Luo XM, et al. Specific HDAC6 inhibition by ACY-738 reduces SLE pathogenesis in NZB/W mice. Clin Immunol. 2016 Jan;162:58-73.
[8] LoPresti P. The Selective HDAC6 Inhibitor ACY-738 Impacts Memory and Disease Regulation in an Animal Model of Multiple Sclerosis. Front Neurol. 2019 Jun 28;10:519.
| Cell experiment [1]: | |
Cell lines | Patient-derived L0, S3, S7 human glioma cells and murine KR158 glioma cells |
Preparation Method | Patient-derived glioma cells were grown as floating spheres in serum-free neural stem cell media. Murine KR158 glioma cells were grown adherent in DMEM supplemented with 10% fetal bovine serum (FBS). Cells were treated with ACY-738 (0.5–5μM). |
Reaction Conditions | 0.5–5μM; 24 hours to 5 days. |
Applications | ACY-738 significantly inhibited tumor cell proliferation. ACY-738 concurrently reduced the expression of the proliferative marker Ki67 and increased the expression of the differentiation marker TUJ1, thereby inducing cell differentiation. This effect at low concentrations was dependent on the presence of primary cilia on the tumor cells. |
| Animal experiment [2]: | |
Animal models | C57BL/6 female mice with Experimental Autoimmune Encephalomyelitis (EAE) induced by myelin oligodendrocyte glycoprotein (MOG35-55) emulsion. |
Preparation Method | EAE was induced in mice via subcutaneous immunization. The mice was treated with ACY-738 (20mg/kg). |
Dosage form | 20mg/kg; i.p.; administered on day 9 and day 10 post-immunization. |
Applications | CY-738 treatment delayed disease onset and reduced disease severity in EAE mice. ACY-738 increased short-term memory in the cross-maze test. |
References: | |
| Cas No. | 1375465-91-0 | SDF | |
| Canonical SMILES | O=C(NO)C(C=N1)=CN=C1NC2(CC2)C3=CC=CC=C3 | ||
| Formula | C14H14N4O2 | M.Wt | 270.29 |
| Solubility | DMSO : ≥ 32 mg/mL (118.39 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6997 mL | 18.4986 mL | 36.9973 mL |
| 5 mM | 739.9 μL | 3.6997 mL | 7.3995 mL |
| 10 mM | 370 μL | 1.8499 mL | 3.6997 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)