Tacedinaline | N-acetyldinaline;CI-994;CI994, CI-994, CI 994, PD123654, PD-123654, PD 123654, Tacedinaline, acetyldinaline;Acetyldinaline;PD-123654;Goe-5549 | HDAC

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乙酰地那林 /Tacedinaline {[allProObj[0].p_purity_real_show]}

货号：A132717 同义名： N-acetyldinaline;CI-994

CI-994 is an inhibitor of HDAC1 with IC50 of 0.57 μM with anti-tumor effect. It can cause G1 cell cycle arrest.

Tacedinaline 化学结构
CAS号：112522-64-2

Tacedinaline 3D分子结构
CAS号：112522-64-2

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Tacedinaline 纯度/质量文件产品仅供科研

货号：A132717 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。

Tacedinaline 生物活性

靶点	HDAC3 HDAC3, IC50:1.2 μM HDAC2 HDAC2, IC50:0.9 μM HDAC1 HDAC1, IC50:0.9 μM
描述	The histone deacetylase (HDAC) is responsible for the regulation of reversible histone acetylation. CI-994 is an aminophenyl benzamide-type inhibitor of HDAC with IC50 values of 0.9, 0.9, and 1.2 µM for HDAC1, 2, and 3, respectively. It also showed whole-cell HDAC inhibitory activity in 293T cells with an IC50 value of 6 µM and anti-proliferative activity in human cancer cell line HCT116 with an IC50 value of 4 µM^[3]. In non-small cell lung cancer cells, the combination of CI-994 (40 µM) and antineoplastic agents (i.e. 0.01 µM gemcitabine, 0.001 µM docetaxel) caused a marked synergism of action at 48 and 72 h after the treatment^[4]. The administration of CI-994 (10 or 30 mg/kg) for 14 days increased acetylation of histone H3 in mice following spinal cord injury compared to the vehicle-treated group^[5].
作用机制	CI-994 is an HDAC inhibitor that exerts antitumor effects probably through the inhibition of histone deacetylation and cell cycle arrest^[4].

Tacedinaline 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
293T cells		Function assay		Inhibition of HDAC in 293T cells, IC50=6 μM	17941625
human HCT116 cells		Cytotoxic assay		Cytotoxicity against human HCT116 cells by MTT assay, IC50=4 μM	17941625
human LNCap		Proliferation assay		Antiproliferative activity against human LNCap by MTT assay， IC50=7.4 μM	18166465
human MDA-MB-231 cells		Growth inhibition assay	5 days	Growth inhibition of human MDA-MB-231 cells after 5 days by MTT assay, GI50=0.17 μM	18543902

Tacedinaline 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00004861	Pancreatic Cancer	Phase 2	Completed	-	United States, California ... 展开 >> Cedars-Sinai Comprehensive Cancer Center Los Angeles, California, United States, 90048 United States, Florida H. Lee Moffitt Cancer Center and Research Institute Tampa, Florida, United States, 33612 United States, Maryland Sinai Hospital of Baltimore Baltimore, Maryland, United States, 21225 United States, Michigan William Beaumont Hospital Royal Oak, Michigan, United States, 48073 United States, North Carolina Raleigh Hematology/Oncology Associates - Wake Practice Raleigh, North Carolina, United States, 27609 United States, Ohio Jewish Hospital of Cincinnati, Inc. Cincinnati, Ohio, United States, 45236 Ireland Cancer Center Cleveland, Ohio, United States, 44106-5065 United States, Tennessee West Clinic, P.C. Memphis, Tennessee, United States, 38117 Sarah Cannon-Minnie Pearl Cancer Center Nashville, Tennessee, United States, 37203 United States, Texas Tyler Cancer Center Tyler, Texas, United States, 75702 United States, Virginia Northern Virginia Oncology Group Fairfax, Virginia, United States, 22031 Canada, Manitoba St. Boniface General Hospital Winnipeg, Manitoba, Canada, R2H 2A6 Canada, Nova Scotia Nova Scotia Cancer Centre Halifax, Nova Scotia, Canada, B3H 1V7 Canada, Ontario Cancer Care Ontario-London Regional Cancer Centre London, Ontario, Canada, N6A 4L6 Ottawa Regional Cancer Center - General Division Ottawa, Ontario, Canada, K1H 8L6 Canada, Quebec Centre Hospitalier de l'Universite de Montreal Montreal, Quebec, Canada, H2L-4M1 收起 <<
NCT00005093	Lung Cancer	Phase 3	Completed	-	United States, California ... 展开 >> Cedars-Sinai Comprehensive Cancer Center Los Angeles, California, United States, 90048 United States, Florida H. Lee Moffitt Cancer Center and Research Institute Tampa, Florida, United States, 33612 United States, Massachusetts New England Medical Center Hospital Boston, Massachusetts, United States, 02111 United States, Michigan University of Michigan Comprehensive Cancer Center Ann Arbor, Michigan, United States, 48109-0752 Barbara Ann Karmanos Cancer Institute Detroit, Michigan, United States, 48201 United States, North Carolina Raleigh Hematology/Oncology Associates - Wake Practice Raleigh, North Carolina, United States, 27609 United States, Ohio Arthur G. James Cancer Hospital - Ohio State University Columbus, Ohio, United States, 43210 United States, Tennessee West Clinic, P.C. Memphis, Tennessee, United States, 38117 United States, Texas Southwest Regional Cancer Center Austin, Texas, United States, 78705 Canada, Alberta Cross Cancer Institute Edmonton, Alberta, Canada, T6G 1Z2 Canada, British Columbia British Columbia Cancer Agency - Fraser Valley Cancer Centre Surrey, British Columbia, Canada, V3V 1Z2 BC Cancer Agency Vancouver, British Columbia, Canada, V5Z 4E6 British Columbia Cancer Agency - Vancouver Island Cancer Centre Victoria, British Columbia, Canada, V8R 1J8 Canada, Ontario Ottawa Regional Cancer Center - General Division Ottawa, Ontario, Canada, K1H 8L6 Mount Sinai Hospital - Toronto Toronto, Ontario, Canada, M5G 1X5 Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 收起 <<
NCT00005624	Multiple Myeloma	Phase 2	Completed	-	United States, Florida ... 展开 >> H. Lee Moffitt Cancer Center and Research Institute Tampa, Florida, United States, 33612 收起 <<

Tacedinaline 参考文献

[1]Moradei OM, Mallais TC, et al. Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity. J Med Chem. 2007 Nov 15;50(23):5543-6.

[2]Loprevite M, Tiseo M, et al. In vitro study of CI-994, a histone deacetylase inhibitor, in non-small cell lung cancer cell lines. Oncol Res. 2005;15(1):39-48.

[3]Moradei OM, Mallais TC, Frechette S, et al. Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity. J Med Chem. 2007;50(23):5543-5546. doi:10.1021/jm701079h

[4]Loprevite M, Tiseo M, Grossi F, et al. In vitro study of CI-994, a histone deacetylase inhibitor, in non-small cell lung cancer cell lines. Oncol Res. 2005;15(1):39-48. doi:10.3727/096504005775082066

[5]Zhang S, Fujita Y, Matsuzaki R, Yamashita T. Class I histone deacetylase (HDAC) inhibitor CI-994 promotes functional recovery following spinal cord injury. Cell Death Dis. 2018;9(5):460. Published 2018 May 1. doi:10.1038/s41419-018-0543-8

Tacedinaline 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.71mL

0.74mL

0.37mL

18.57mL

3.71mL

1.86mL

37.13mL

7.43mL

3.71mL

Tacedinaline 技术信息

CAS号	112522-64-2
分子式	C₁₅H₁₅N₃O₂
分子量	269.298

别名	N-acetyldinaline;CI-994;CI994, CI-994, CI 994, PD123654, PD-123654, PD 123654, Tacedinaline, acetyldinaline;Acetyldinaline;PD-123654;Goe-5549
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

DMSO: 50 mg/mL(185.67 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

5% DMSO+40% PEG 300+water 5 mg/mL

乙酰地那林 /Tacedinaline {[allProObj[0].p_purity_real_show]}

Tacedinaline 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Tacedinaline 质控信息

Tacedinaline 生物活性

Tacedinaline 细胞研究

Tacedinaline 临床研究

Tacedinaline 参考文献

Tacedinaline 实验方案

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HDAC3	HDAC3, IC50:1.2 μM
HDAC2	HDAC2, IC50:0.9 μM
HDAC1	HDAC1, IC50:0.9 μM

乙酰地那林 /Tacedinaline {[allProObj[0].p_purity_real_show]}

Tacedinaline 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Tacedinaline 质控信息

Tacedinaline 生物活性

Tacedinaline 细胞研究

Tacedinaline 临床研究

Tacedinaline 参考文献

Tacedinaline 实验方案

Tacedinaline 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

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Tacedinaline 纯度/质量文件产品仅供科研