HDAC1 activator-1
Based on 1 Customer Validation
HDAC1 activator-1 is a specific HDAC1 activator with orally activity, exerting no significant effects on other HDAC family members. HDAC1 activator-1 exhibits neuroprotective activity, ameliorates cognitive and motor function deficits by reducing neuronal loss and gliosis. HDAC1 activator-1 specifically activates HDAC1 in SH-SY5Y cells and exerts regulatory effects on aberrant cell cycle and DNA damage. HDAC1 activator-1 can be used for the research of TDP-43 proteinopat1-related neurodegenerative diseases including Amyotrophic Lateral Sclerosis (ALS) and cerebral ischemia-related neurological injury.
For research use only. We do not sell to patients.
- Purity : 99.64%
- CAS No.: 300399-36-4
- Formula: C17H24O4
- Molecular Weight:292.37
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
|
HDAC1 |
In Vitro
HDAC1 Activator-1 (cpd 5104434) (1 μM-50 μM) shows dose-dependent activation of HDAC1 enzymatic activity, with no significant effects on HDAC2, HDAC3, and HDAC8, exhibiting high selectivity for HDAC1[1][2].
HDAC1 Activator-1 (1 μM-50 μM; 72 h) specifically activates HDAC1 in the human neuroblastoma cell line SH-SY5Y in vitro[1][2].
HDAC1 Activator-1 (2.5 μM, 25 μM) restores HDAC1 enzymatic activity in primary cortical neurons subjected to oxygen-glucose deprivation (OGD)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Human neuroblastoma SH-SY5Y cell line
-
Concentration:1 μM, 10 μM, 50 μM
-
Incubation Time:72 h
-
Result:Enhances HDAC1 deacetylation function without altering its protein expression.
In Vivo
HDAC1 Activator-1 (6 mg/kg; i.p.; 5 days a week; for 2 months) ameliorates cognitive deficits (Morris water maze, novel object recognition test) and motor dysfunction (rotarod test), reverses aberrant cell cycle, DNA damage, neuronal loss and gliosis in FTLD-TDP transgenic mice[1][2].
HDAC1 Activator-1 (6 mg/kg; i.p.; 5 days a week; for 2 months) ameliorates cognitive deficits (Morris water maze, novel object recognition test) and motor dysfunction (rotarod test), reverses aberrant cell cycle, DNA damage, neuronal loss and gliosis in FTLD-TDP transgenic mice[1][2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Female and male FTLD-TDP transgenic (Tg) mice (6 months old) and age-matched wild-type (WT) FVB mice[1].
-
Dosage:6 mg/kg, 30 mg/kg, 0.3 mg/kg
-
Administration:Intraperitoneal (IP); 5 days a week; for 1-2 months
-
Result:Demonstrated significant improvement in cognitive function and motor function.
Restored nuclear HDAC1 activity and reduced acetyl-histone H3 (Lys9/14) levels.
Reversed aberrant cell cycle activity (downregulated E2F1, PCNA, p21) and attenuated DNA damage.
Alleviated neuronal loss and inhibited gliosis.
No significant toxicity (no impact on cell viability, hepatotoxicity, renotoxicity, or body weight).
Chemical Information
-
CAS No. 300399-36-4
-
Appearance Solid
-
Molecular Weight 292.37
-
Formula C17H24O4
-
SMILES
O=C1C(CC2C(CC(C)(CC2=O)C)=O)=C(CC(C)(C1)C)O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 12.5 mg/mL (42.75 mM; ultrasonic and warming and heat to 60°C; 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. 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. 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)
In Vivo:
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (4.28 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Purity & Documentation
References
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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4203 mL | 17.1016 mL | 34.2032 mL | 85.5081 mL |
| 5 mM | 0.6841 mL | 3.4203 mL | 6.8406 mL | 17.1016 mL | |
| 10 mM | 0.3420 mL | 1.7102 mL | 3.4203 mL | 8.5508 mL | |
| 15 mM | 0.2280 mL | 1.1401 mL | 2.2802 mL | 5.7005 mL | |
| 20 mM | 0.1710 mL | 0.8551 mL | 1.7102 mL | 4.2754 mL | |
| 25 mM | 0.1368 mL | 0.6841 mL | 1.3681 mL | 3.4203 mL | |
| 30 mM | 0.1140 mL | 0.5701 mL | 1.1401 mL | 2.8503 mL | |
| 40 mM | 0.0855 mL | 0.4275 mL | 0.8551 mL | 2.1377 mL |
HDAC1 activator-1 Related Classifications
HY-186073 Related Classifications
Powered by Bioz
Keywords
- HDAC1 activator-1
- 300399-36-4
- HDAC
- Histone deacetylases
- HDAC1 activator
- neuroprotective activity
- inhibits aberrant cell cycle
- DNA damage
- reduces neuronal loss and gliosis
- ameliorates cognitive and motor function deficits
- TDP-43 proteinopathies
- amyotrophic lateral sclerosis (ALS)
- cerebral ischemia
- neurodegenerative diseases
- SH-SY5Y cell line
- HEK-293T cell line
- primary cortical neurons
- frontotemporal lobar degeneration with ubiquitin-positive inclusions (FTLD-TDP) transgenic mice
- rat model of cerebral ischemia
- mouse model of neurodegeneration
- Inhibitor
- inhibitor
- inhibit