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ACY-775 {[allProObj[0].p_purity_real_show]}

货号:A725076

ACY-775是一种强效且选择性的组蛋白去乙酰化酶 6(HDAC6)抑制剂,IC50 值为 7.5 nM。

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
ACY-775 化学结构 CAS号:1375466-18-4
ACY-775 化学结构
CAS号:1375466-18-4
ACY-775 3D分子结构
CAS号:1375466-18-4
ACY-775 化学结构 CAS号:1375466-18-4
ACY-775 3D分子结构 CAS号:1375466-18-4
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ACY-775 纯度/质量文件 产品仅供科研

货号:A725076 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 HD1 HD2 HDAC HDAC1 HDAC10 HDAC11 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 其他靶点 纯度
Givinostat HCl monohydrate ++++

HD1-B, IC50: 7.5 nM

HD1-A, IC50: 16 nM

+++

HD2, IC50: 10 nM

99%+
MC1568 ++

HD1-A (Maize), IC50: 100 nM

HD1-B (Maize), IC50: 3.4 μM

96%
Trichostatin A ++++

HDAC, IC50: ~1.8 nM

99%+
Scriptaid 99%+
Valproic acid sodium Autophagy 97%
AR-42 +++

HDAC, IC50: 30 nM

99%+
Dacinostat +++

HDAC, IC50: 32 nM

98+%
CUDC-101 ++++

HDAC, IC50: 4.4 nM

++++

HDAC1, IC50: 4.5 nM

+++

HDAC10, IC50: 26.1 nM

+++

HDAC2, IC50: 12.6 nM

++++

HDAC3, IC50: 9.1 nM

+++

HDAC4, IC50: 13.2 nM

+++

HDAC5, IC50: 11.4 nM

++++

HDAC6, IC50: 5.1 nM

+

HDAC7, IC50: 373 nM

++

HDAC8, IC50: 79.8 nM

++

HDAC9, IC50: 67.2 nM

HER2,EGFR 99%+
M344 ++

HDAC, IC50: 100 nM

99%+
Splitomicin +

Sir2p, IC50: 60 μM

99%
Panobinostat ++++

HDAC (MOLT-4 cells), IC50: 5 nM

HDAC (Reh cells), IC50: 20 nM

98%
Sodium 4-Phenylbutyrate 98%
Vorinostat +++

HDAC, IC50: ~10 nM

98%
Curcumin Nrf2,NF-κB 98%
Belinostat +++

HDAC, IC50: 27 nM

98%
RG-2833 ++

HDAC1, Ki: 32 nM

++

HDAC3, Ki: 5 nM

98%
Valproic acid +

HDAC1, IC50: 0.4 mM

98%
BG45 +

HDAC1, IC50: 2 μM

+

HDAC2, IC50: 2.2 μM

+

HDAC3, IC50: 289 nM

99%+
Entinostat +

HDAC1, IC50: 0.51 μM

+

HDAC3, IC50: 1.7 μM

98%
Resminostat +++

HDAC1, IC50: 42.5 nM

++

HDAC3, IC50: 50.1 nM

++

HDAC6, IC50: 71.8 nM

98+%
Romidepsin +++

HDAC1, IC50: 36 nM

+++

HDAC2, IC50: 47 nM

99%+
Parthenolide p53,NF-κB 97% HPLC
Tacedinaline +

HDAC1, IC50: 0.9 μM

+

HDAC2, IC50: 0.9 μM

+

HDAC3, IC50: 1.2 μM

98%
Mocetinostat ++

HDAC1, IC50: 0.15 μM

+

HDAC11, IC50: 0.59 μM

+

HDAC2, IC50: 0.29 μM

+

HDAC3, IC50: 1.66 μM

98%
WT-161 ++++

HDAC1, IC50: 8.35 nM

+++

HDAC2, IC50: 15.4 nM

++++

HDAC6, IC50: 0.4 nM

99%+
Fimepinostat ++++

HDAC1, IC50: 1.7 nM

++++

HDAC10, IC50: 2.8 nM

++++

HDAC11, IC50: 5.4 nM

++++

HDAC2, IC50: 5.0 nM

++++

HDAC3, IC50: 1.8 nM

+++

HDAC6, IC50: 27 nM

99%+
Tucidinostat ++

HDAC1, IC50: 95 nM

++

HDAC10, IC50: 78 nM

++

HDAC2, IC50: 160 nM

++

HDAC3, IC50: 67 nM

99%+
Santacruzamate A ++++

HDAC2, IC50: 119 pM

99%+
(E,E)-RGFP966 ++

HDAC3, IC50: 80 nM

99%+
LMK-235 +++

HDAC4, IC50: 11.9 nM

++++

HDAC5, IC50: 4.2 nM

99%+
Tasquinimod 99%+
CAY10603 ++++

HDAC6, IC50: 2 pM

98%
Tubastatin A +++

HDAC6, IC50: 15 nM

98%
Tubacin ++++

HDAC6, IC50: 4 nM

99%+
ACY-738 ++++

HDAC6, IC50: 1.7 nM

99%+
Nexturastat A ++++

HDAC6, IC50: 5 nM

99%+
BRD73954 +++

HDAC6, IC50: 36 nM

++

HDAC8, IC50: 120 nM

99%
Tubastatin A HCl +++

HDAC6, IC50: 15 nM

+

HDAC8, IC50: 854 nM

98%
PCI-34051 +++

HDAC8, IC50: 10 nM

99%+
Ricolinostat ++

HDAC1, IC50: 58 nM

++

HDAC2, IC50: 48 nM

++

HDAC3, IC50: 51 nM

++++

HDAC6, IC50: 4.7 nM

++

HDAC8, IC50: 100 nM

99%+
Droxinostat +

HDAC3, IC50: 16.9 μM

+

HDAC6, IC50: 2.47 μM

+

HDAC8, IC50: 1.46 μM

99%+
Abexinostat ++++

HDAC1, Ki: 7 nM

+++

HDAC10, IC50: 24 nM

+++

HDAC2, Ki: 19 nM

++++

HDAC3/SMRT, Ki: 8.2 nM

+++

HDAC6, Ki: 17 nM

+

HDAC8, IC50: 280 nM

98%+
Citarinostat +++

HDAC1, IC50: 35 nM

+++

HDAC2, IC50: 45 nM

+++

HDAC3, IC50: 46 nM

++++

HDAC6, IC50: 2.6 nM

++

HDAC8, IC50: 137 nM

99%+
HPOB +

HDAC1, IC50: 2.9 μM

+

HDAC10, IC50: 3.0 μM

+

HDAC2, IC50: 4.4 μM

+

HDAC3, IC50: 1.7 μM

++

HDAC6, IC50: 56 nM

+

HDAC8, IC50: 2.8 μM

97%
Quisinostat 2HCl ++++

HDAC1, IC50: 0.11 nM

++++

HDAC10, IC50: 0.46 nM

++++

HDAC11, IC50: 0.37 nM

++++

HDAC2, IC50: 0.33 nM

++++

HDAC3, IC50: 4.86 nM

++++

HDAC4, IC50: 0.64 nM

++++

HDAC5, IC50: 3.69 nM

++++

HDAC8, IC50: 4.26 nM

97%
Domatinostat +

HDAC1, IC50: 1.20 μM

+

HDAC10, IC50: 21 μM

+

HDAC11, IC50: 9.7 μM

+

HDAC2, IC50: 1.12 μM

+

HDAC3, IC50: 0.57 μM

+

HDAC5, IC50: 11.3 μM

+

HDAC9, IC50: 50 μM

99%+
TMP269 ++

HDAC4, IC50: 157 nM

++

HDAC5, IC50: 97 nM

+++

HDAC7, IC50: 43 nM

+++

HDAC9, IC50: 23 nM

99%+
Pracinostat ++

HDAC1, IC50: 49 nM

+++

HDAC10, IC50: 40 nM

++

HDAC11, IC50: 93 nM

++

HDAC2, IC50: 96 nM

+++

HDAC3, IC50: 43 nM

++

HDAC4, IC50: 56 nM

+++

HDAC5, IC50: 47 nM

+

HDAC6, IC50: 1.008 μM

++

HDAC7, IC50: 137 nM

++

HDAC8, IC50: 140 nM

++

HDAC9, IC50: 70 nM

99%+
TMP195 ++

HDAC4, Ki: 59 nM

++

HDAC5, Ki: 60 nM

+++

HDAC7, Ki: 26 nM

+++

HDAC9, Ki: 15 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

ACY-775 生物活性

描述 HDAC6 (histone deacetylase 6) is a structurally and functionally unique class Iib isoform localized almost exclusively to the cytoplasm. HDAC6 loss of function results in an antidepressant-like phenotype. ACE-775 is a potent and selective HDAC6 inhibitor with an IC50 value of 7.5 nM. In RN46A-B14 cells treated with ACY-775 (2.5 μM) for 4 hours, there was an increase in the acetylated (lysine 40) fraction of α-tubulin. ACY-775 rapidly distribute to the brain leading to a total drug exposure in CNS comparable to that of peripheral tissues. In wild-type mice, ACY-775 (50 mg/kg; 24 h, 4 h, and 30 min) caused significant increases in α-tubulin acetylation in all tested brain regions: cortex, hippocampus and cerebellum and stimulated mouse exploratory behaviors in novel environments[3].
作用机制 Activity of ACY-775 is fully explained by inhibition of the C terminal catalytic domain of HDAC6[3].

ACY-775 细胞实验

Cell Line
Concentration Treated Time Description References
RN46A-B14 cells 2.5 μM 4 h To evaluate the inhibitory effect of ACY-775 on HDAC6 and its impact on α-tubulin acetylation. Results showed that ACY-775 significantly increased the acetylation of α-tubulin but had no significant effect on histone H3K9 acetylation. Neuropsychopharmacology. 2014 Jan;39(2):389-400.
Dorsal root ganglion (DRG) neurons 2.5 μM Overnight To evaluate the ability of ACY-738 and ACY-775 to restore mitochondrial axonal transport defects. Results showed that both inhibitors significantly increased mitochondrial motility and total number, and significantly enhanced the number of retrogradely transported mitochondria. Neurotherapeutics. 2017 Apr;14(2):417-428.
Mouse neuroblastoma (N2a) cells 1 μM Overnight To assess the effect of ACY-738 and ACY-775 on the acetylation status of α-tubulin and histone 3. Results showed that both inhibitors significantly enhanced α-tubulin acetylation at 1 μM concentration, while histone acetylation remained unaffected. Neurotherapeutics. 2017 Apr;14(2):417-428.

ACY-775 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice NIH Swiss mice Intraperitoneal injection 50 mg/kg Single administration To evaluate the antidepressant-like effects of ACY-775 in vivo. Results showed that ACY-775 significantly reduced immobility time in the tail suspension test, demonstrating antidepressant-like effects. Additionally, ACY-775 increased α-tubulin acetylation levels in the brain. Neuropsychopharmacology. 2014 Jan;39(2):389-400.
Mice HSPB1 S135F-induced CMT2 mouse model Intraperitoneal injection 3 mg/kg Once daily for 21 days To evaluate the effect of ACY-775 on reversing motor and sensory deficits in the CMT2 mouse model. Results showed that ACY-775 significantly improved motor and sensory nerve action potential amplitudes and increased reinnervation of neuromuscular junctions. Neurotherapeutics. 2017 Apr;14(2):417-428.
Macaque Macaque model Intravenous injection 0.1 and 2 mg/kg Single dose, lasting 120 minutes Compare HDAC6 target occupancy between EKZ-317 and ACY-775, showing that EKZ-317 achieved high occupancy (≥90%) at both 0.1 and 2 mg/kg doses, while ACY-775 only achieved similar occupancy at 2 mg/kg dose ACS Chem Neurosci. 2020 Apr 1;11(7):1093-1101

ACY-775 参考文献

[1]Veronick Benoy, et al. Development of Improved HDAC6 Inhibitors as Pharmacological Therapy for Axonal Charcot-Marie-Tooth Disease. Neurotherapeutics. 2017 Apr; 14(2): 417-428.

[2]Jeanine Jochems et al. Antidepressant-Like Properties of Novel HDAC6-Selective Inhibitors with Improved Brain Bioavailability. Neuropsychopharmacology. 2014 Jan; 39(2): 389-400.

[3]Jochems J, et al. Antidepressant-like properties of novel HDAC6-selective inhibitors with improved brain bioavailability. Neuropsychopharmacology. 2014 Jan;39(2):389-400

ACY-775 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.03mL

0.61mL

0.30mL

15.14mL

3.03mL

1.51mL

30.27mL

6.05mL

3.03mL

ACY-775 技术信息

CAS号1375466-18-4
分子式C17H19FN4O2
分子量 330.36
SMILES Code O=C(C1=CN=C(NC2(C3=CC=CC(F)=C3)CCCCC2)N=C1)NO
MDL No. MFCD30533691
别名
运输蓝冰
InChI Key IYBURCQQEUNLDL-UHFFFAOYSA-N
Pubchem ID 57382288
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, 2-8°C

溶解方案

DMSO: 25 mg/mL(75.68 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
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