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).
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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。 |
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]. |
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 << |
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 |
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 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
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