Quisinostat 2HCl | JNJ-26481585 dihydrochloride | Pan-HDAC Inhibitor

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Quisinostat 2HCl {[allProObj[0].p_purity_real_show]}

货号：A562597 同义名： JNJ-26481585 dihydrochloride; Quisinostat dihydrochloride

Quisinostat 2HCl是一种第二代 HDAC 抑制剂，对 HDAC1 的 IC50 为 0.11 nM，适度抑制 HDAC2、4、10 和 11，对 HDAC3、5、8、9 的选择性超过 30 倍，广泛用于抗肿瘤研究。

Quisinostat 2HCl 化学结构
CAS号：875320-31-3

Quisinostat 2HCl 3D分子结构
CAS号：875320-31-3

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Quisinostat 2HCl 纯度/质量文件产品仅供科研

货号：A562597 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

全球学术期刊中引用的产品: • Adv. Funct. Mater., 2025, 2500696. Ambeed. [ A245395 ]; • JACS, 2025. Ambeed. [ A505336 ]; • Sci. Adv., 2025, 11(13): eadr0006. Ambeed. [ A152627 ]; • ACS Appl. Mater. Interfaces, 2025, 17(12): 18046-18058. Ambeed. [ A739356 , A171817 ]; • Food Res. Int., 2025, 116191. Ambeed. [ A1452012 ]; 更多 >

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														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 (Reh cells), IC50: 20 nM HDAC (MOLT-4 cells), IC50: 5 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				✔											NF-κB,p53	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。

Quisinostat 2HCl 生物活性

靶点	HDAC8 HDAC8, IC50:4.26 nM HDAC10 HDAC10, IC50:0.46 nM HDAC3 HDAC3, IC50:4.86 nM HDAC4 HDAC4, IC50:0.64 nM
描述	The inhibition of HDACs increases the acetylation of histone proteins, which affects the tertiary chromatin structure and leads to altered expression of genes involved in cell proliferation, apoptosis and differentiation. Thus, it makes a key role for inhibition of HDACs in anti-proliferation of tumor cells. Quisinostat is an oral pan-HDAC inhibitor with highest potency for HDAC1 (IC50=0.11±0.03nM, measured by recombinant HDAC enzyme activity), modest potent to HDAC 2, 4, 10 and 11nM and a lower potency on the rest HDACs. Increased level of acetylated histone H3 (H3 Ac), H4 (H4 Ac), histone H4-acetyl K16 (H4-K16 Ac) and histone H4-trimethyl K20 (H4-K20Me3) (acetylation regulated by HDAC1-3), p21 and E-cadherin (expression regulated by HDAC1), as well as increased tubulin acetylation, induction of Hsp70, and loss of Hsp90 client c-Raf can be observed in a dose-dependent manner (30-1000nM) after 24-hour treatment with Quisinostat in human A2780 ovarian carcinoma cells, which shows activity against pan-HDAC inhibition. Also, Quisinostat can inhibit cell growth in all lung, breast, colon, prostate, brain, and ovarian tumor cell lines tested with IC50 values ranging from 3.1 to 246nM, which shows its antiproliferative effect in a broad panel of human tumor cell lines from both solid and hematologic origin. Compared with the first generation of HDAC inhibitors (SAHA or TSA), Quisinostat shows prolonged pharmacodynamic response in vivo. Quisinostat can induce continuous H3 acetylation in tumor tissue from A2780 ovarian tumor-bearing nude mice when treated with Quisinostat at 10mg/kg as well as increased level of HDAC1-regulated p21^[1]. Up to now, a phase I study of Quisinostat in patients with advanced solid tumors has been done^[2].
作用机制	Quisinostat is a pyrimidyl-hydroxamic acid analogue, which can chelate the Zn²⁺ ion of HDAC. ^[1]

Quisinostat 2HCl 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.70mL

2.14mL

1.07mL

21.40mL

4.28mL

2.14mL

Quisinostat 2HCl 技术信息

CAS号	875320-31-3
分子式	C₂₁H₂₈Cl₂N₆O₂
分子量	467.39
SMILES Code	O=C(C1=CN=C(N2CCC(CNCC3=CN(C)C4=C3C=CC=C4)CC2)N=C1)NO.[H]Cl.[H]Cl
MDL No.	MFCD29905457

别名	JNJ-26481585 dihydrochloride; Quisinostat dihydrochloride
运输	蓝冰
InChI Key	NRUIZESXVMJDKR-UHFFFAOYSA-N
Pubchem ID	122129987

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, 2-8°C

溶解方案

细胞实验：

DMSO: 30 mg/mL(64.19 mM)，配合低频超声，并水浴加热至45℃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

动物实验：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

动物实验配方

IP 2% DMSO+water 7 mg/mL clear

PO 0.5% CMC-Na 40 mg/mL suspension

Quisinostat 2HCl {[allProObj[0].p_purity_real_show]}

Quisinostat 2HCl 纯度/质量文件产品仅供科研

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HDAC8	HDAC8, IC50:4.26 nM
HDAC10	HDAC10, IC50:0.46 nM
HDAC3	HDAC3, IC50:4.86 nM
HDAC4	HDAC4, IC50:0.64 nM
HDAC11	HDAC11, IC50:0.37 nM
HDAC5	HDAC5, IC50:3.69 nM
HDAC2	HDAC2, IC50:0.33 nM
HDAC1	HDAC1, IC50:0.11 nM

Quisinostat 2HCl {[allProObj[0].p_purity_real_show]}

Quisinostat 2HCl 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Quisinostat 2HCl 质控信息

Quisinostat 2HCl 生物活性

Quisinostat 2HCl 实验方案

Quisinostat 2HCl 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

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临床研究

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Quisinostat 2HCl 纯度/质量文件产品仅供科研