Pracinostat | SB939 | HDAC/MBLAC2 Inhibitor | AmBeed-信号通路专用抑制剂

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Pracinostat {[allProObj[0].p_purity_real_show]}

货号：A477591 同义名： SB939

Pracinostat is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6 and has no activity against the class III isoenzyme SIRT I.

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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+
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Pracinostat 化学结构
CAS号：929016-96-6

Pracinostat 3D分子结构
CAS号：929016-96-6

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Pracinostat 纯度/质量文件产品仅供科研

货号：A477591 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: • Cell, 2024, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 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													95%
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			✔												NF-κB,Nrf2	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			98%
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			99+%
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。

Pracinostat 生物活性

靶点	HDAC8 HDAC8, IC50:140 nM HDAC10 HDAC10, IC50:40 nM HDAC3 HDAC3, IC50:43 nM HDAC4 HDAC4, IC50:56 nM
描述	HDACs 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 (HDAC 11)^[1]. Pracinostat (SB-939) is identified as a potent hydroxamate-based inhibitor of class I, II and IV HDACs, inhibiting the isolated enzymes with IC50 values of 43 to 140 nM, 40 to 137 nM (class II), and 93 nM (class IV) with the exception of HDAC6. Pracinostat is effective on cell proliferation of various kinds of human cancer cell lines, including T-cell lymphoma cells and leukemia cells with IC50 values ranging from 50 nM to 170 nM, colon and prostate cancer cell lines with IC50 values ranging from 340 to 540 nM. However, no inhibition of the proliferation of normal human dermal fibroblasts at concentrations up to 100 μM can be observed. Treatment of pracinostat >0.125 μM can induce ac-H3 and the acetylation of α-tubulin in HCT-116 cells after 24h. Meanwhile, pracinostat >0.25 μM leads to decreased retinoblastoma serine phosphorylation on S807/811 and an increase of the cyclin-dependant kinase inhibitor p21Cip/WAF. Echoed to that, the increase in cell cycle arrest goes hand in hand with a dose-dependent increase of PARP. In animal study, a single dose of either 50 or 125 mg/kg of pracinostat causes increased ac-H3 in the tumor tissue of HCT-116 xenografted nude mice. Oral treatment of pracinostat once a day for 21 days, on dose of 100 mg/kg, achieves 94% tumor growth inhibition. These results show the superior pharmacokinetic and pharmacodynamic properties of pracinostat in in vivo study^[2]. A phase 3 study of pracinostat in combination with azacitidine in adults with acute myeloid leukemia and a phase 2 study of pracinostat with azacitidine in patients with previously untreated myelodysplastic syndrome can be seen (https://www.cancer.gov/).
作用机制	Pracinostat is an hydroxamate-based HDAC inhibitor, structure of which can chelate Zn ion of HDACs.

Pracinostat 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
HCT116 cells		Proliferation assay	48 h	Antiproliferative activity against human HCT116 cells after 48 hrs by sulforhodamine B assay, GI50=0.24 μM	24119555
MCF7 cells		Proliferation assay	48 h	Antiproliferative activity against human MCF7 cells after 48 hrs by sulforhodamine B assay, GI50=0.17 μM	24119555
MDA-MB-435 cells		Proliferation assay	48 h	Antiproliferative activity against human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay, GI50=0.48 μM	24119555
NCI-H460 cells		Proliferation assay	48 h	Antiproliferative activity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay, GI50=0.22 μM	24119555

Pracinostat 动物研究

Dose

Mice^[4] (p.o.): min = 50 mg/kg, max = 200 mg/kg

Administration

p.o.

Pharmacokinetics

Animal	Nude mice^[2]
Administration	i.d.
C_max	2632 ng/ml
T_1/2	2.44 h
AUC_0→∞	1841 ng·h/L
F	0.34
T_max	0.17 h
AUC_0→last	1836 ng·h/L

Pracinostat 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]Novotny-Diermayr V, Sangthongpitag K, et al. SB939, a novel potent and orally active histone deacetylase inhibitor with high tumor exposure and efficacy in mouse models of colorectal cancer. Mol Cancer Ther. 2010 Mar;9(3):642-52.

[3]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.

[4]Wang H, Yu N, et al. Discovery of (2E)-3-{2-butyl-1-[2-(diethylamino)ethyl]-1H-benzimidazol-5-yl}-N-hydroxyacrylamide (SB939), an orally active histone deacetylase inhibitor with a superior preclinical profile. J Med Chem. 2011 Jul 14;54(13):4694-720.

Pracinostat 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.79mL

0.56mL

0.28mL

13.95mL

2.79mL

1.39mL

27.90mL

5.58mL

2.79mL

Pracinostat 技术信息

CAS号	929016-96-6
分子式	C₂₀H₃₀N₄O₂
分子量	358.478

别名	SB939
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 250 mg/mL(697.39 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

动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 10 mg/mL clear

PO 0.5% CMC-Na 38 mg/mL suspension

Pracinostat {[allProObj[0].p_purity_real_show]}

Pracinostat 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Pracinostat 质控信息

Pracinostat 生物活性

Pracinostat 细胞研究

Pracinostat 动物研究

Pracinostat 参考文献

Pracinostat 实验方案

Pracinostat 技术信息

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HDAC8	HDAC8, IC50:140 nM
HDAC10	HDAC10, IC50:40 nM
HDAC3	HDAC3, IC50:43 nM
HDAC4	HDAC4, IC50:56 nM
HDAC6	HDAC6, IC50:1.008 μM
HDAC9	HDAC9, IC50:70 nM
HDAC11	HDAC11, IC50:93 nM
HDAC7	HDAC7, IC50:137 nM
HDAC5	HDAC5, IC50:47 nM
HDAC2	HDAC2, IC50:96 nM
HDAC1	HDAC1, IC50:49 nM

Pracinostat {[allProObj[0].p_purity_real_show]}

Pracinostat 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Pracinostat 质控信息

Pracinostat 生物活性

Pracinostat 细胞研究

Pracinostat 动物研究

Pracinostat 参考文献

Pracinostat 实验方案

Pracinostat 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

细胞研究

临床研究

确认信息

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Pracinostat 纯度/质量文件产品仅供科研