| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
ACY-1083 targets histone deacetylase 6 (HDAC6), a unique HDAC isoform that primarily deacetylates non-histone proteins such as α-tubulin. It is a potent inhibitor with an IC₅₀ of 3 nM. It is 260-fold more selective for HDAC6 than other HDAC isoforms. It modulates tubulin acetylation and protein homeostasis.
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|---|---|
| ln Vitro |
Treatment with ACY-1083 (30 and 300 nM) greatly enhanced cell viability in a dose-dependent way [2].
In vitro, ACY-1083 potently inhibits HDAC6 with an IC₅₀ of 3 nM. It shows high selectivity for HDAC6 over other HDAC isoforms (260-fold). It modulates tubulin acetylation and affects cell migration, inflammation, and neurological functions. |
| ln Vivo |
ACY-1083 (ip; 10 mg/kg; for 7 days) efficiently alleviates cisplatin-induced mechanical allodynia in C57BL/6J mice ACY-1083 (oral dose 3 mg/kg ACY-1083 for 7 days ) can reverse paclitaxel-induced mechanical allodynia in adult male SD rats. In mice treated 5 mg/kg ACY-1083 via intraperitoneal (ip) injection, the maximum plasma concentration (Cmax) was 936 ng/mL, the half-life (T1/2) was 3.5 hours, and the bioactive plasma exposure was 8 postdose. Hour.
In vivo, ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy in adult male SD rats at 3 mg/kg. It penetrates the brain and modulates HDAC6 activity in the central nervous system. It has been studied for its potential in treating neurological disorders. |
| Enzyme Assay |
The in vitro enzyme assay for ACY-1083 measures the inhibition of HDAC6 deacetylase activity. Recombinant HDAC6 enzyme is incubated with the compound and a fluorogenic or radiometric substrate. The deacetylation of the substrate is quantified, and IC₅₀ values are calculated.
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| Cell Assay |
Cell Viability Assay [2]
Cell Types: Mouse Hippocampus (HT22) Cell Tested Concentrations: 30 and 300 nM Incubation Duration: Experimental Results: Cell viability was Dramatically improved. In vitro cell-based assays for ACY-1083 are performed using neuronal cell lines or other cell types. Cells are treated with ACY-1083, and HDAC6 activity is measured by assessing the acetylation of α-tubulin or other substrates. Cell viability, migration, and other functional readouts are assessed. |
| Animal Protocol |
Animal/Disease Models: 8-10 weeks old adult male C57BL/6J mice [1]
Doses: 3 or 10 mg/kg Route of Administration: intraperitoneal (ip) injection; daily; 7 days Experimental Results: 10 mg/kg dose can alleviate cisplatin ( 2.3 mg/kg), but not the 3 mg/kg dose. Animal/Disease Models: Adult male Sprague Dawley rats [1] Doses: 3 mg/kg Route of Administration: Two oral doses per day for 7 days. Experimental Results: Paclitaxel (6 mg/kg or 12 mg/kg)-induced mechanical allodynia was reversed. In vivo animal experiments for ACY-1083 have been conducted in rat models of chemotherapy-induced peripheral neuropathy. Animals are administered the compound orally or via other routes, and neuropathy is assessed using behavioral tests such as mechanical allodynia and thermal hyperalgesia. Biomarkers such as α-tubulin acetylation are measured in nerve tissues. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of ACY-1083 have been characterized in preclinical species. It is brain-penetrating. Detailed PK parameters such as half-life, clearance, and brain penetration are determined from plasma and brain concentration-time profiles.
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| Toxicity/Toxicokinetics |
Toxicological data for ACY-1083 are limited. In standard preclinical safety assessments, it would be evaluated for potential off-target effects and general toxicity. The compound is intended for research use only and not for therapeutic use in humans.
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| References |
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| Additional Infomation |
ACY-1083 is a selective HDAC6 inhibitor that has shown promise for reversing chemotherapy-induced peripheral neuropathy. It is brain-penetrating and has been studied for its potential in treating neurological disorders. It has not been approved for clinical use.
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| Molecular Formula |
C17H18F2N4O2
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|---|---|
| Molecular Weight |
348.3472
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| Exact Mass |
348.139
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| CAS # |
1708113-43-2
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| PubChem CID |
91844718
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| Appearance |
White to off-white solid powder
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| LogP |
2.5
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
454
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1(C([H])([H])C([H])([H])C(C2C([H])=C([H])C([H])=C([H])C=2[H])(C([H])([H])C1([H])[H])N([H])C1=NC([H])=C(C(N([H])O[H])=O)C([H])=N1)F
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| InChi Key |
MRWCVKLVSWYIFO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H18F2N4O2/c18-17(19)8-6-16(7-9-17,13-4-2-1-3-5-13)22-15-20-10-12(11-21-15)14(24)23-25/h1-5,10-11,25H,6-9H2,(H,23,24)(H,20,21,22)
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| Chemical Name |
2-[(4,4-difluoro-1-phenylcyclohexyl)amino]-N-hydroxypyrimidine-5-carboxamide
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| Synonyms |
ACY-1083; ACY 1083; ACY1083
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~200 mg/mL (~574.14 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (14.35 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 5 mg/mL (14.35 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (14.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8707 mL | 14.3534 mL | 28.7068 mL | |
| 5 mM | 0.5741 mL | 2.8707 mL | 5.7414 mL | |
| 10 mM | 0.2871 mL | 1.4353 mL | 2.8707 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 Structure, selectivity and pharmacokinetics of ACY-1083.Pain.2017 Jun;158(6):1126-1137. |
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 Effect of repeated or prolonged ACY-1083 treatment on symptoms of cisplatin-induced peripheral neuropathy.Pain.2017 Jun;158(6):1126-1137. |
 ACY-1083 enhances mitochondrial bioenergetics and contents in the tibial nerve of cisplatin-treated mice.Pain.2017 Jun;158(6):1126-1137. |
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