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Daminozide/丁酰肼 {[allProObj[0].p_purity_real_show]}

货号:A252184 同义名: 丁酰肼(B9) / Alar; Succinic Acid

Daminozide is a histone demethylase KDM2/7 subfamily inhibitor (IC50 values are 0.55, 1.5 and 2.1 μM for PHF8, KDM2A and KDM7A respectively). Exhibits ≥ 60-fold selectivity for KDM2/7 demethylases over other histone demethylases and 2-oxoglurate oxygenases (IC50 > 100 μM).

Daminozide/丁酰肼 化学结构 CAS号:1596-84-5
Daminozide/丁酰肼 化学结构
CAS号:1596-84-5
Daminozide/丁酰肼 3D分子结构
CAS号:1596-84-5
Daminozide/丁酰肼 化学结构 CAS号:1596-84-5
Daminozide/丁酰肼 3D分子结构 CAS号:1596-84-5
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Daminozide/丁酰肼 纯度/质量文件 产品仅供科研

货号:A252184 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 KDM1 KDM2 KDM3 KDM4 KDM5 KDM6 其他靶点 纯度
OG-L002 +++

LSD1, IC50: 20 nM

99%+
ORY-1001 +++

LSD1, IC50: 20 nM

98%
SP-2509 ++++

LSD1, IC50: 13 nM

98+%
GSK2879552 2HCl +

LSD1, Ki: 1.7 μM

99%+
T-3775440 HCl ++++

LSD1, IC50: 2.1 nM

99%
GSK-LSD1 2HCl +++

LSD1, IC50: 16 nM

98%
Pulrodemstat benzenesulfonate 99%+
IOX1 +

KDM2A, IC50: 1.8 μM

+++

KDM3A, IC50: 0.1 μM

++

KDM4E, IC50: 2.3 μM

KDM4C, IC50: 0.6 μM

+

KDM5C, IC50: 19 μM

+

KDM6B, IC50: 1.6 μM

99%
PFI-90 99%+
ML324 +

JMJD2, IC50: 920 nM

99%+
NCGC00244536 ++++

KDM4, IC50: 10 nM

99%
KDM4D-IN-1 ++

KDM4D, IC50: 0.41 μM

99%+
GSK467 ++++

KDM5B, Ki: 10 nM

99%
GSK-J1 +++

JMJD3, IC50: 60 nM

99%+
(Z)-JIB-04 ++

JMJD2E, IC50: 340 nM

JMJD2A, IC50: 1100 nM

++

JARID1A, IC50: 230 nM

++

JMJD3, IC50: 855 nM

97%
CPI-455 ++++

KDM5A, IC50: 10 nM

++++

KDM5, IC50: 10 nM

98%
JIB-04 ++

JMJD2D, IC50: 290 nM

JMJD2E, IC50: 435 nM

++

JARID1A, IC50: 230 nM

++

JMJD3, IC50: 855 nM

98%
GSK-J4 HCl +++

JMJD3, IC50: 60 nM

98%
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。

Daminozide/丁酰肼 生物活性

描述 Daminozide, a plant growth regulator, selectively inhibits human KDM2/7 histone demethylases, with IC50 values of 0.55 μM for PHF8, 1.5 μM for KDM2A, and 2.1 μM for KIAA1718. It exhibits over 100-fold selectivity for the KDM2/7 subfamily compared to other demethylase subfamily members tested [1][2].
体内研究

Daminozide (200-20000 ppm) induces teratogenic and genotoxic effects in the model organism Drosophila melanogaster [2].

体外研究

Daminozide exhibits over 100-fold selectivity for the KDM2/7 subfamily compared to other demethylase subfamily members tested (IC50=127 μM for KDM3A, or greater against other demethylases)[1].

Daminozide/丁酰肼 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
NCT03172715 Tibial Fractures Not Applicable Recruiting June 2029 Finland ... 展开 >> Central Finland Hospital Recruiting Jyväskylä, Finland, 40620 Contact: Juha Paloneva, MD, PhD    +358 14 2693119       Contact: Valtteri Tapper, MD          Sub-Investigator: Alar Toom, MD, PhD          Sub-Investigator: Valtteri Tapper, MD, PhD          Principal Investigator: Juha Paloneva, MD, PhD          Sub-Investigator: Heikki Nurmi, MD, PhD          Sub-Investigator: Maija Pesola, MD, PhD          Sub-Investigator: Konsta Pamilo, MD, PhD          Kuopio University Hospital Not yet recruiting Kuopio, Finland Contact: Jussi Jalkanen, MD          Principal Investigator: Jussi Jalkanen, MD, PhD          Sub-Investigator: Tommi Kääriäinen, MD, PhD          Päijät-Häme Central Hospital Not yet recruiting Lahti, Finland Contact: Jussi Haapala, MD, PhD          Principal Investigator: Jussi Haapala, MD, PhD          Sub-Investigator: Sami Nurmi, MD          Oulu University Hospital Not yet recruiting Oulu, Finland Contact: Tuukka Niinimäki, MD, PhD          Principal Investigator: Tuukka Niinimäki, MD, PhD          Sub-Investigator: Tero Kortekangas, MD, PhD          Seinäjoki Central Hospital Not yet recruiting Seinäjoki, Finland Contact: Janne Jousmäki, MD, PhD          Principal Investigator: Janne Jousmäki, MD, PhD          Sub-Investigator: Ville Sumuvuori, MD, PhD          Coxa Joint Replacement Hospital Not yet recruiting Tampere, Finland Contact: Jyrki Nieminen, MD          Principal Investigator: Jyrki Nieminen, MD, PhD          Tampere University Hospital Not yet recruiting Tampere, Finland Contact: Minna Laitinen, MD, PhD          Principal Investigator: Ilari Pajamäki, MD          Turku University Hospital Not yet recruiting Turku, Finland Contact: Niko Strandberg, MD, PhD          Principal Investigator: Niko Strandberg, MD, PhD          Sub-Investigator: Mika Junnila, MD, PhD 收起 <<
NCT02188355 - Recruiting September 2019 -
NCT02336243 Premature Birth ... 展开 >> Preeclampsia Fetal Growth Retardation Stillbirth 收起 << Phase 3 Unknown April 2018 Chile ... 展开 >> Centro de Salud Familiar ANCORA Juan Pablo II Recruiting Santiago, Chile Contact: Francisco Arancibia, Matron          Contact    +56 2 2482 2400       Centro de Salud Familiar ANCORA Madre Teresa de Calcuta Recruiting Santiago, Chile Contact: Patricia Alar, Enf Matrona          Contact    +56 2 2851 5211       Centro de Salud Familiar ANCORA San Alberto Hurtado Recruiting Santiago, Chile Contact: Ghislaine Bustamante, Matrona          Contact    +56 2 2587 9300       Centro Medico Lira 85 Recruiting Santiago, Chile Contact: Cecilia Berrios, Enf Matrona          Contact    +56 2 2354 8077       Centro Medico San Joaquin Recruiting Santiago, Chile Contact: Veronica Nuñez, Enf Matrona          Contact    +56 2 2354 8540 收起 <<

Daminozide/丁酰肼 参考文献

[1]Rose NR, Woon EC, Tumber A, Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases. J Med Chem. 2012 Jul 26;55(14):6639-43.

[2]Roy SS, et, al. Exploration of teratogenic and genotoxic effects of fruit ripening retardant Alar (Daminozide) on model organism Drosophila melanogaster. Interdiscip Toxicol. 2018 May;11(1):27-37.

Daminozide/丁酰肼 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

6.24mL

1.25mL

0.62mL

31.22mL

6.24mL

3.12mL

62.43mL

12.49mL

6.24mL

Daminozide/丁酰肼 技术信息

CAS号1596-84-5
分子式C6H12N2O3
分子量 160.17
SMILES Code O=C(O)CCC(NN(C)C)=O
MDL No. MFCD00002787
别名 丁酰肼(B9) ;Alar; Succinic Acid; Kylar SADH; SADH; Kylar; DMASA; DIMG; B 995; Aminozide
运输蓝冰
InChI Key NOQGZXFMHARMLW-UHFFFAOYSA-N
Pubchem ID 15331
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

溶解方案

DMSO: 100 mg/mL(624.33 mM),配合水浴加热至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

H2O: 100 mg/mL(624.33 mM),配合低频超声助溶

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
配制的工作液建议现用现配,短期内尽快用完。 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
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