1. Cell Cycle/DNA Damage Epigenetics
  2. HDAC
  3. HDAC1 activator-1

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.

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HDAC1 activator-1

HDAC1 activator-1 Chemical Structure

CAS No. : 300399-36-4

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Description

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[1][2].

IC50 & Target[1][2]

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.

Western Blot Analysis[1]

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 (cpd 5104434) (0.3-30 mg/kg; i.p.; 5 days a week; for 1 month) has been tested in FTLD-TDP transgenic mice, with 6 and 30 mg/kg doses restoring cognitive function, motor function and nuclear HDAC1 activity[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].
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).
Molecular Weight

292.37

Formula

C17H24O4

CAS No.
SMILES

O=C1C(CC2C(CC(C)(CC2=O)C)=O)=C(CC(C)(C1)C)O

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HDAC1 activator-1
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HY-186073
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