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

HDAC1 activator-1 是一种特异性 HDAC1 激活剂,具备口服活性,对其他 HDAC 家族成员无显著作用。HDAC1 activator-1具有神经保护活性,可通过减少神经元丢失与神经胶质增生改善认知及运动功能缺陷。HDAC1 activator-1 可在人神经母细胞瘤细胞系 SH-SY5Y 中特异性激活 HDAC1,抑制异常细胞周期进程、减轻 DNA 损伤。HDAC1 activator-1可用于肌萎缩侧索硬化 (ALS) 等 TDP43 蛋白相关神经退行性疾病,以及脑缺血相关神经损伤的研究。

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HDAC1 activator-1

HDAC1 activator-1 Chemical Structure

CAS No. : 300399-36-4

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

HDAC1 Activator-1 可剂量依赖性激活 HDAC1 酶活性,对 HDAC2、HDAC3 和 HDAC8 无显著作用,对 HDAC1 具有高度选择性[1][2]
HDAC1 Activator-1 可在体外人神经母细胞瘤细胞系 SH-SY5Y 中特异性激活 HDAC1[1][2]
HDAC1 Activator-1 (2.5 μM、25 μM) 可在氧糖剥夺 (OGD) 处理的原代皮质神经元中恢复 HDAC1 酶活性[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Cell line: HEK-293T cells, human hepatocytes, human renal cells
Concentration: 1 μM-50 μM
Incubation Time: 72 h
Result: No significant cytotoxicity; does not affect cell survival/proliferation; no hepatotoxicity or nephrotoxicity.

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.
体内研究
(In Vivo)

HDAC1 Activator-1 (0.3、6、30 mg/kg;腹腔注射;每周 5 天;连续 1 个月) 已在 FTLD-TDP 转基因小鼠中进行测试,其中 6 和 30 mg/kg 剂量可恢复认知功能、运动功能和核 HDAC1 活性[1][2]
HDAC1 Activator-1 (6 mg/kg;腹腔注射;每周 5 天;连续 2 个月) 可改善 FTLD-TDP 转基因小鼠的认知缺陷和运动功能障碍,逆转异常细胞周期、DNA 损伤、神经元丢失和胶质增生[1][2]
HDAC1 Activator-1 (30 mg/kg;腹腔注射;每日一次) 显著恢复脑缺血大鼠模型脑组织中的 HDAC1 活性,减少梗死体积、神经元凋亡、DNA 损伤和氧化应激标志物,改善神经肌肉、平衡和前爪力量功能[1][2]

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).
分子量

292.37

Formula

C17H24O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • 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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产品名称:
HDAC1 activator-1
目录号:
HY-186073
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