Ricolinostat | ACY-1215 | HDAC6 Inhibitor | AmBeed-信号通路专用抑制剂

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2-(二苯基氨基)-N-[7-(羟基氨基)-7-氧代庚基]-5-嘧啶甲酰胺 /Ricolinostat {[allProObj[0].p_purity_real_show]}

货号：A173859 同义名： ACY-1215;Rocilinostat

Ricolinostat (ACY-1215) 是一种有效且选择性的HDAC6抑制剂，IC50为5 nM。它还抑制HDAC1、HDAC2和HDAC3的IC50值分别为58 nM、48 nM和51 nM。

Ricolinostat 化学结构
CAS号：1316214-52-4

Ricolinostat 3D分子结构
CAS号：1316214-52-4

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Ricolinostat 纯度/质量文件产品仅供科研

货号：A173859 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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组蛋白去乙酰化酶亚型比较

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-A, IC50: 16 nM HD1-B, IC50: 7.5 nM	+++ HD2, IC50: 10 nM														{[allProObj[0].p_purity_real_show]}
MC1568	++ HD1-B (Maize), IC50: 3.4 μM HD1-A (Maize), IC50: 100 nM															{[allProObj[0].p_purity_real_show]}
Trichostatin A			++++ HDAC, IC50: ~1.8 nM													{[allProObj[0].p_purity_real_show]}
Scriptaid			✔													{[allProObj[0].p_purity_real_show]}
Valproic acid sodium			✔												Autophagy	{[allProObj[0].p_purity_real_show]}
AR-42			+++ HDAC, IC50: 30 nM													{[allProObj[0].p_purity_real_show]}
Dacinostat			+++ HDAC, IC50: 32 nM													{[allProObj[0].p_purity_real_show]}
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	EGFR,HER2	{[allProObj[0].p_purity_real_show]}
M344			++ HDAC, IC50: 100 nM													{[allProObj[0].p_purity_real_show]}
Splitomicin			+ Sir2p, IC50: 60 μM													{[allProObj[0].p_purity_real_show]}
Panobinostat			++++ HDAC (Reh cells), IC50: 20 nM HDAC (MOLT-4 cells), IC50: 5 nM													{[allProObj[0].p_purity_real_show]}
Sodium 4-Phenylbutyrate			✔													{[allProObj[0].p_purity_real_show]}
Vorinostat			+++ HDAC, IC50: ~10 nM													{[allProObj[0].p_purity_real_show]}
Curcumin			✔												Nrf2,NF-κB	{[allProObj[0].p_purity_real_show]}
Belinostat			+++ HDAC, IC50: 27 nM													{[allProObj[0].p_purity_real_show]}
RG-2833				++ HDAC1, Ki: 32 nM				++ HDAC3, Ki: 5 nM								{[allProObj[0].p_purity_real_show]}
Valproic acid				+ HDAC1, IC50: 0.4 mM												{[allProObj[0].p_purity_real_show]}
BG45				+ HDAC1, IC50: 2 μM			+ HDAC2, IC50: 2.2 μM	+ HDAC3, IC50: 289 nM								{[allProObj[0].p_purity_real_show]}
Entinostat				+ HDAC1, IC50: 0.51 μM				+ HDAC3, IC50: 1.7 μM								{[allProObj[0].p_purity_real_show]}
Resminostat				+++ HDAC1, IC50: 42.5 nM				++ HDAC3, IC50: 50.1 nM			++ HDAC6, IC50: 71.8 nM					{[allProObj[0].p_purity_real_show]}
Romidepsin				+++ HDAC1, IC50: 36 nM			+++ HDAC2, IC50: 47 nM									{[allProObj[0].p_purity_real_show]}
Parthenolide				✔											NF-κB,p53	{[allProObj[0].p_purity_real_show]}
Tacedinaline				+ HDAC1, IC50: 0.9 μM			+ HDAC2, IC50: 0.9 μM	+ HDAC3, IC50: 1.2 μM								{[allProObj[0].p_purity_real_show]}
Mocetinostat				++ HDAC1, IC50: 0.15 μM		+ HDAC11, IC50: 0.59 μM	+ HDAC2, IC50: 0.29 μM	+ HDAC3, IC50: 1.66 μM								{[allProObj[0].p_purity_real_show]}
WT-161				++++ HDAC1, IC50: 8.35 nM			+++ HDAC2, IC50: 15.4 nM				++++ HDAC6, IC50: 0.4 nM					{[allProObj[0].p_purity_real_show]}
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					{[allProObj[0].p_purity_real_show]}
Tucidinostat				++ HDAC1, IC50: 95 nM	++ HDAC10, IC50: 78 nM		++ HDAC2, IC50: 160 nM	++ HDAC3, IC50: 67 nM								{[allProObj[0].p_purity_real_show]}
Santacruzamate A							++++ HDAC2, IC50: 119 pM									{[allProObj[0].p_purity_real_show]}
(E,E)-RGFP966								++ HDAC3, IC50: 80 nM								{[allProObj[0].p_purity_real_show]}
LMK-235									+++ HDAC4, IC50: 11.9 nM	++++ HDAC5, IC50: 4.2 nM						{[allProObj[0].p_purity_real_show]}
Tasquinimod									✔							{[allProObj[0].p_purity_real_show]}
CAY10603											++++ HDAC6, IC50: 2 pM					{[allProObj[0].p_purity_real_show]}
Tubastatin A											+++ HDAC6, IC50: 15 nM					{[allProObj[0].p_purity_real_show]}
Tubacin											++++ HDAC6, IC50: 4 nM					{[allProObj[0].p_purity_real_show]}
ACY-738											++++ HDAC6, IC50: 1.7 nM					{[allProObj[0].p_purity_real_show]}
Nexturastat A											++++ HDAC6, IC50: 5 nM					{[allProObj[0].p_purity_real_show]}
BRD73954											+++ HDAC6, IC50: 36 nM		++ HDAC8, IC50: 120 nM			{[allProObj[0].p_purity_real_show]}
Tubastatin A HCl											+++ HDAC6, IC50: 15 nM		+ HDAC8, IC50: 854 nM			{[allProObj[0].p_purity_real_show]}
PCI-34051													+++ HDAC8, IC50: 10 nM			{[allProObj[0].p_purity_real_show]}
Ricolinostat				++ HDAC1, IC50: 58 nM			++ HDAC2, IC50: 48 nM	++ HDAC3, IC50: 51 nM			++++ HDAC6, IC50: 4.7 nM		++ HDAC8, IC50: 100 nM			{[allProObj[0].p_purity_real_show]}
Droxinostat								+ HDAC3, IC50: 16.9 μM			+ HDAC6, IC50: 2.47 μM		+ HDAC8, IC50: 1.46 μM			{[allProObj[0].p_purity_real_show]}
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			{[allProObj[0].p_purity_real_show]}
Citarinostat				+++ HDAC1, IC50: 35 nM			+++ HDAC2, IC50: 45 nM	+++ HDAC3, IC50: 46 nM			++++ HDAC6, IC50: 2.6 nM		++ HDAC8, IC50: 137 nM			{[allProObj[0].p_purity_real_show]}
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			{[allProObj[0].p_purity_real_show]}
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			{[allProObj[0].p_purity_real_show]}
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		{[allProObj[0].p_purity_real_show]}
TMP269									++ HDAC4, IC50: 157 nM	++ HDAC5, IC50: 97 nM		+++ HDAC7, IC50: 43 nM		+++ HDAC9, IC50: 23 nM		{[allProObj[0].p_purity_real_show]}
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		{[allProObj[0].p_purity_real_show]}
TMP195									++ HDAC4, Ki: 59 nM	++ HDAC5, Ki: 60 nM		+++ HDAC7, Ki: 26 nM		+++ HDAC9, Ki: 15 nM		{[allProObj[0].p_purity_real_show]}
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。

Ricolinostat 生物活性

靶点	HDAC8 HDAC8, IC50:100 nM HDAC3 HDAC3, IC50:51 nM HDAC6 HDAC6, IC50:4.7 nM HDAC2 HDAC2, IC50:48 nM HDAC1 HDAC1, IC50:58 nM
描述	There are 18 mammalian HDACs, HDAC 1 - 11 and sirt 1 - 7. One of the member, HDAC6 can target specific substrates like HSP90 andα-tubulin which involve in protein trafficking and degradation or cell shape and migration, thus participates in the pathways relating to neurodegenerative diseases, cancer, and immunology^[1]. ACY-1215, also called Rocilinostat, is a potent and selective HDAC6 inhibitor with IC50 value of 4.7 nM (measured by HDAC enzymatic assays), while exhibits minimal inhibition on HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1, and Sirtuin2 (IC50 > 1 μM) and slightly inhibits HDAC8 (IC50 = 0.1 μM). A dose-dependent increased acetylatedα-tubulin and no affecting acetylation of histones can be observed in MM.1S cells with treatment of ACY-1215 for 6 hours, which confirming the selective inhibition of ACY-1215 on low dose (0.62 μM). ACY-1215 (0 - 4 μM) in combination with bortezomib (0 - 5 nM) for 24 and 48 hours in MM.1S cells and for 48 hours in RPMI8226 cells induce synergistic anti-MM activity. This may due to ACY-1215 disrupting aggresome formation with increased levels of polyubiquitinated protein, then triggers the apoptosis by the induction of ER stress and UPR. And a significant therapeutic advantage was found by combining ACY-1215 (50 mg/kg, IP) with bortezomib (0.5 mg/kg, IV) compared with either agent alone for 3 weeks, which echoes the synergistic activity cellar study^[2]. ACY-1215 alone/ in combination with dexametrasone and either bortezomib or lenalidomide is currently under phase I, II clinical trials for multiple myeloma^[3].
作用机制	ACY-1215 can monodentate Zn²⁺ of HDAC6 through its phenylhydroxamate structure^[4].

Ricolinostat 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
A-172	10 nM	Growth Inhibition Assay	24/48 h	inhibits cell growth time dependently	26150340
CCL-119		Growth Inhibition Assay	48 h	IC50=1.7 μM	26116270
H9		Growth Inhibition Assay	48 h	IC50=1.2 μM	26116270
Hbl-1		Growth Inhibition Assay	48 h	IC50=1.6 μM	26116270

Ricolinostat 动物研究

Dose

Mice^[5] (i.p.): 50 mg/kg

Administration

i.p.

Pharmacokinetics

Animal	Mice^[2]
Dose	50 mg/kg
Administration	i.p.
C_max	2133 ng/ml

Ricolinostat 参考文献

[1]Wang XX, Wan RZ, et al. Recent advances in the discovery of potent and selective HDAC6 inhibitors. Eur J Med Chem. 2018 Jan 1;143:1406-1418.

[2]Santo L, Hideshima T, et al. Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma. Blood. 2012 Mar 15;119(11):2579-89.

[3]Seidel C, Schnekenburger M, et al. Histone deacetylase 6 in health and disease. Epigenomics. 2015;7(1):103-18.

[4]Porter NJ, Mahendran A, et al. Unusual zinc-binding mode of HDAC6-selective hydroxamate inhibitors. Proc Natl Acad Sci U S A. 2017 Dec 19;114(51):13459-13464.

[5]Selective Inhibition of HDAC6 with a New Prototype Inhibitor (ACY-1215) Overcomes Bortezomib Resistance In Multiple Myeloma (MM)

Ricolinostat 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.53mL

2.31mL

1.15mL

23.07mL

4.61mL

2.31mL

Ricolinostat 技术信息

CAS号	1316214-52-4
分子式	C₂₄H₂₇N₅O₃
分子量	433.503

别名	ACY-1215;Rocilinostat;ACY-63
运输	蓝冰

存储条件

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 50 mg/mL(115.34 mM)，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

动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 11 mg/mL clear

PO 0.5% CMC-Na 40 mg/mL suspension

2-(二苯基氨基)-N-[7-(羟基氨基)-7-氧代庚基]-5-嘧啶甲酰胺 /Ricolinostat {[allProObj[0].p_purity_real_show]}

Ricolinostat 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Ricolinostat 质控信息

Ricolinostat 生物活性

Ricolinostat 细胞研究

Ricolinostat 动物研究

Ricolinostat 参考文献

Ricolinostat 实验方案

Ricolinostat 技术信息

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HDAC8	HDAC8, IC50:100 nM
HDAC3	HDAC3, IC50:51 nM
HDAC6	HDAC6, IC50:4.7 nM
HDAC2	HDAC2, IC50:48 nM
HDAC1	HDAC1, IC50:58 nM

2-(二苯基氨基)-N-[7-(羟基氨基)-7-氧代庚基]-5-嘧啶甲酰胺 /Ricolinostat {[allProObj[0].p_purity_real_show]}

Ricolinostat 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Ricolinostat 质控信息

Ricolinostat 生物活性

Ricolinostat 细胞研究

Ricolinostat 动物研究

Ricolinostat 参考文献

Ricolinostat 实验方案

Ricolinostat 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Ricolinostat 纯度/质量文件产品仅供科研