Belinostat | PXD101;PX105684;NSC726630 | Apoptosis Inducer | HDAC

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Belinostat/贝利司他 {[allProObj[0].p_purity_real_show]}

货号：A210633 同义名： PXD101; PX105684

Belinostat（PXD101；PX105684）显示出对HDAC的高效抑制作用，在HeLa细胞提取物中的IC50为27 nM。

Belinostat/贝利司他化学结构
CAS号：866323-14-0

Belinostat/贝利司他 3D分子结构
CAS号：866323-14-0

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Belinostat/贝利司他纯度/质量文件产品仅供科研

货号：A210633 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: • Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]; • Cell, 2025. Ambeed. [ A122167 ]; • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]; • Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]; 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-B, IC50: 7.5 nM HD1-A, IC50: 16 nM	+++ HD2, IC50: 10 nM														99%+
MC1568	++ HD1-B (Maize), IC50: 3.4 μM HD1-A (Maize), IC50: 100 nM															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	EGFR,HER2	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。

Belinostat/贝利司他生物活性

靶点	HDAC HDAC, IC50:27 nM
描述	HDACs (Histone deacetylases) are a group of enzymes that remove acetyl groups and regulate the histone tail, protein-DNA interaction, chromatin conformation, and even transcription. There are 18 mammalian HDACs divided into four classes: class I (HDACs 1, 2, 3, 8), class II (HDACs 4, 5, 6, 7, 9, 10), class III (sirtuin family: sirt1-sirt7) and class IV (HDAC11)^[1]. Belinostat, also called as PXD101, is a pan-HDAC inhibitor (IC50 = 27 nM, measured by HDAC enzymatic activity)^[2], inhibiting class I, II and IV HDAC isoforms with nanomolar potency^[3]. Like other HDAC pan inhibitors, the hyperacetylation of H3 and H4, which are the biomarkers for the inhibition of class I HDAC, can be observed in A2780 cells treated with 1 μM belinostat for various times (0.5 - 36h). Belinostat can inhibit the growth of a number of human tumor cell lines from various origins, including A2780, HCT116, HT29, WIL, CALU-3, MCF7, PC3 and HS852 cells, with IC50 ranging 0.2 - 3.4 μM. The induction of P21 and apoptosis, as determined with measurement of PARP cleavage, by belinostat can be observed after drug incubation for 24h with concentration <1 μM in these cell lines, except for PC3 and 2780AD cell line. Belinostat shows good pharmacokinetic and pharmacodynamic properties. Treatment of belinostat 10 - 40 mg/kg daily for a week can inhibit the tumor growth of A2780 tumor-bearing mice in a dose-dependent manner, along with the increase of acetylated histone H4^[2]. Co-administration of belinostat with bortezomib can synergistically induce cell death in CLL cells, which may due to the involving of other mechanism, like NF-kB inactivation and perturbation in the expression of proapoptotic and antiapoptotic proteins^[4]. Belinostat was approved for the treatment of patients with relapsed or refractory PTCL. Its clinical trial of treatment for solid tumors/hematological malignancies is undergoing^[5].
作用机制	The hydroxamic structure of belinostat can chelate the Zn ion of HDACs^[6].

Belinostat/贝利司他细胞实验

Cell Line resting memory CD4 T cells HT29 colon cancer cells PC3 prostate cancer cells SW579 cells Lung squamous cell carcinoma cells	Concentration	Treated Time	Description	References
resting memory CD4 T cells	400 nM	14 days	To evaluate the efficiency of Belinostat in reversing HIV-1 latency, results showed that Belinostat effectively induced HIV-1 replication, and the induced virus was not only replication competent but also infectious.	J Virol. 2015 Dec 9;90(4):1858-71.
HT29 colon cancer cells	2 μM	24 h	To evaluate the effects of Belinostat on cell proliferation and metabolism, results showed that Belinostat significantly inhibited the proliferation of HT29 cells and increased phosphocholine (PC) levels.	Cancer Res. 2012 Feb 15;72(4):990-1000.
PC3 prostate cancer cells	0.9 μM	24 h	To evaluate the effects of Belinostat on cell proliferation and metabolism, results showed that Belinostat significantly inhibited the proliferation of PC3 cells and increased phosphocholine (PC) levels.	Cancer Res. 2012 Feb 15;72(4):990-1000.
SW579 cells	1 µM	24 h	Belinostat at a concentration of 1 µM for 24 h significantly induced cell death in SW579 cells, with a dead/live cell ratio of 120%.	Int J Mol Sci. 2019 Jan 21;20(2):454.
Lung squamous cell carcinoma cells	0.1, 0.2, 0.3, 1, 3 µM	72 h	To determine the sensitivity of Belinostat in lung squamous cell carcinoma cells, the results showed that Belinostat exhibited differential sensitivities in different cell lines and induced apoptosis.	Mol Oncol. 2017 Aug;11(8):965-980.

Belinostat/贝利司他动物实验

Species Mice SCID mice	Animal Model HT29 colon cancer xenograft model Calu-1 xenograft model	Administration	Dosage	Frequency	Description	References
Mice	HT29 colon cancer xenograft model	Oral	60 mg/kg	Once daily for 3 days	To evaluate the effects of Belinostat on tumor growth and metabolism, results showed that Belinostat significantly inhibited the growth of HT29 tumors and increased phosphocholine (PC) levels.	Cancer Res. 2012 Feb 15;72(4):990-1000.
SCID mice	Calu-1 xenograft model	Oral	40 mg/kg	5 days a week for 3 weeks	To evaluate the antitumor activity of Belinostat in the Calu-1 xenograft model, the results showed that Belinostat alone or in combination with cisplatin did not exhibit significant antitumor activity.	Mol Oncol. 2017 Aug;11(8):965-980.

Belinostat/贝利司他动物研究

Dose

Mice (i.p.): min = 20 mg/kg^[7], max = 100 mg/kg^[8]

Administration

i.p.

Pharmacokinetics

Animal	Monkeys^[9]
Dose	10 mg/kg
Administration	IV infusion
T_1/2	0.47 h
AUC_0→∞	13000 ng·h/ml
CL	258 ml/min/m2
Vd_ss	0.20 L/kg
MRT	0.26 h

Belinostat/贝利司他参考文献

[1]Yoon S, Eom GH, et al. HDAC and HDAC Inhibitor: From Cancer to Cardiovascular Diseases. Chonnam Med J. 2016 Jan;52(1):1-11.

[2]Plumb JA, Finn PW, et al. Pharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histone deacetylase inhibitor PXD101. Mol Cancer Ther. 2003 Aug;2(8):721-8.

[3]Sawas A, Radeski D, et al. Belinostat in patients with refractory or relapsed peripheral T-cell lymphoma: a perspective review. Ther Adv Hematol. 2015 Aug;6(4):202-8.

[4]Dai Y, Chen S, et al. Interactions between bortezomib and romidepsin and belinostat in chronic lymphocytic leukemia cells. Clin Cancer Res. 2008 Jan 15;14(2):549-58.

[5]Mottamal M, Zheng S, et al. Histone deacetylase inhibitors in clinical studies as templates for new anticancer agents. Molecules. 2015 Mar 2;20(3):3898-941.

[6]New M, Olzscha H, et al. HDAC inhibitor-based therapies: can we interpret the code? Mol Oncol. 2012 Dec;6(6):637-56.

[7]Qian X, Ara G, et al. Activity of the histone deacetylase inhibitor belinostat (PXD101) in preclinical models of prostate cancer. Int J Cancer. 2008 Mar 15;122(6):1400-10.

[8]Buckley MT, Yoon J, et al. The histone deacetylase inhibitor belinostat (PXD101) suppresses bladder cancer cell growth in vitro and in vivo. J Transl Med. 2007 Oct 12;5:49.

[9]Warren KE, McCully C, et al. Plasma and cerebrospinal fluid pharmacokinetics of the histone deacetylase inhibitor, belinostat (PXD101), in non-human primates. Cancer Chemother Pharmacol. 2008 Aug;62(3):433-7. Epub 2007 Oct 25.

Belinostat/贝利司他实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.14mL

0.63mL

0.31mL

15.71mL

3.14mL

1.57mL

31.41mL

6.28mL

3.14mL

Belinostat/贝利司他技术信息

CAS号	866323-14-0
分子式	C₁₅H₁₄N₂O₄S
分子量	318.34
SMILES Code	O=C(NO)/C=C/C1=CC=CC(S(=O)(NC2=CC=CC=C2)=O)=C1
MDL No.	MFCD08064035

别名	PXD101; PX105684; NSC726630
运输	蓝冰
InChI Key	NCNRHFGMJRPRSK-MDZDMXLPSA-N
Pubchem ID	6918638

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C

溶解方案

细胞实验：

DMSO: 105 mg/mL(329.83 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

无水乙醇: 25 mg/mL(78.53 mM)，配合低频超声，并水浴加热至45℃助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇

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

方案三

Belinostat/贝利司他 {[allProObj[0].p_purity_real_show]}

Belinostat/贝利司他纯度/质量文件产品仅供科研

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Belinostat/贝利司他动物研究

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Belinostat/贝利司他 {[allProObj[0].p_purity_real_show]}

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Belinostat/贝利司他技术信息