Iadademstat 2HCl | ORY-1001 dihydrochloride | KDM1A Inhibitor

Iadademstat 2HCl {[allProObj[0].p_purity_real_show]}

货号：A474772 同义名： ORY-1001 dihydrochloride; RG6016 dihydrochloride

Iadademstat 2HCl是一种选择性的、不可逆的赖氨酸（K）特异性去甲基化酶1A（KDM1A/LSD1）抑制剂。

Iadademstat 2HCl 化学结构
CAS号：1431303-72-8

Iadademstat 2HCl 3D分子结构
CAS号：1431303-72-8

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Iadademstat 2HCl 纯度/质量文件产品仅供科研

货号：A474772 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 >

Iadademstat 2HCl 质控信息

组蛋白去甲基酶亚型比较

产品名称	KDM1 ↓ ↑	KDM2 ↓ ↑	KDM3 ↓ ↑	KDM4 ↓ ↑	KDM5 ↓ ↑	KDM6 ↓ ↑	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	++ KDM4C, IC50: 0.6 μM KDM4E, IC50: 2.3 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				++ JMJD2A, IC50: 1100 nM JMJD2E, IC50: 340 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。

Iadademstat 2HCl 生物活性

描述

ORY-1001 trans is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.

Iadademstat 2HCl 细胞实验

Cell Line NCI-H510A THP-1 MV(4;11) TF-1a LNCaP cells MV(4;11) cells THP-1 cells U2OS osteosarcoma cells A549 lung adenocarcinoma cells BT-474 cells MDA-MB-436 cells	Concentration	Treated Time	Description	References
NCI-H510A	0.002 to 2000 nM	10 days	Evaluate the effect of Iadademstat on NCI-H510A cell viability, EC50= 0.16 nM	ACS Pharmacol Transl Sci. 2021 Nov 12;4(6):1818-1834
THP-1	0.02 to 2000 nM	96 hours	Evaluate CD11b protein levels, Iadademstat significantly induced CD11b expression	ACS Pharmacol Transl Sci. 2021 Nov 12;4(6):1818-1834
MV(4;11)	2000, 200, 20, 2 nM	24 hours	Assess LSD1 target engagement, Iadademstat showed the highest LSD1 target engagement	ACS Pharmacol Transl Sci. 2021 Nov 12;4(6):1818-1834
TF-1a	0.002 to 2000 nM	96 hours	Evaluate the effect of Iadademstat on TF-1a cell viability, EC50 in subnanomolar range	ACS Pharmacol Transl Sci. 2021 Nov 12;4(6):1818-1834
LNCaP cells	5 nM	96 hours	To evaluate KDM1A target engagement, results showed that free KDM1A was reduced by ~80% after treatment with 5 nM ORY-1001	J Biol Chem. 2019 May 17;294(20):8311-8322
MV(4;11) cells	5 nM	96 hours	To evaluate KDM1A target engagement, results showed that free KDM1A was reduced by ~80% after treatment with 5 nM ORY-1001	J Biol Chem. 2019 May 17;294(20):8311-8322
THP-1 cells	5 nM	96 hours	To evaluate KDM1A target engagement, results showed that free KDM1A was reduced by ~80% after treatment with 5 nM ORY-1001	J Biol Chem. 2019 May 17;294(20):8311-8322
U2OS osteosarcoma cells	50 nM	24 h	Inhibition of KDM1A, leading to accumulation of H3K9 methylation and loss of H3K9 acetylation	Epigenetics Chromatin. 2023 May 13;16(1):18
A549 lung adenocarcinoma cells	50 nM	24 h	Inhibition of KDM1A, leading to accumulation of H3K9 methylation and loss of H3K9 acetylation	Epigenetics Chromatin. 2023 May 13;16(1):18
BT-474 cells	10 µmol/L	48 hours	Evaluate the inhibitory effect of iadademstat on SOX2 enhancer-driven transcriptional activation, showing a dose-dependent reduction in reporter activity	Aging (Albany NY). 2020 Mar 18;12(6):4794-4814
MDA-MB-436 cells	3.98 µmol/L (IC50)	6 days	Evaluate the inhibitory effect of iadademstat on CSC-driven mammosphere formation, showing a dose-dependent decrease in mammosphere number	Aging (Albany NY). 2020 Mar 18;12(6):4794-4814

Cell Line

Concentration

Treated Time

Description

References

NCI-H510A

0.002 to 2000 nM

10 days

Evaluate the effect of Iadademstat on NCI-H510A cell viability, EC50= 0.16 nM

ACS Pharmacol Transl Sci. 2021 Nov 12;4(6):1818-1834

THP-1

0.02 to 2000 nM

96 hours

Evaluate CD11b protein levels, Iadademstat significantly induced CD11b expression

ACS Pharmacol Transl Sci. 2021 Nov 12;4(6):1818-1834

MV(4;11)

2000, 200, 20, 2 nM

24 hours

Assess LSD1 target engagement, Iadademstat showed the highest LSD1 target engagement

ACS Pharmacol Transl Sci. 2021 Nov 12;4(6):1818-1834

TF-1a

0.002 to 2000 nM

96 hours

Evaluate the effect of Iadademstat on TF-1a cell viability, EC50 in subnanomolar range

ACS Pharmacol Transl Sci. 2021 Nov 12;4(6):1818-1834

LNCaP cells

5 nM

96 hours

To evaluate KDM1A target engagement, results showed that free KDM1A was reduced by ~80% after treatment with 5 nM ORY-1001

J Biol Chem. 2019 May 17;294(20):8311-8322

MV(4;11) cells

5 nM

96 hours

To evaluate KDM1A target engagement, results showed that free KDM1A was reduced by ~80% after treatment with 5 nM ORY-1001

J Biol Chem. 2019 May 17;294(20):8311-8322

THP-1 cells

5 nM

96 hours

To evaluate KDM1A target engagement, results showed that free KDM1A was reduced by ~80% after treatment with 5 nM ORY-1001

J Biol Chem. 2019 May 17;294(20):8311-8322

U2OS osteosarcoma cells

50 nM

24 h

Inhibition of KDM1A, leading to accumulation of H3K9 methylation and loss of H3K9 acetylation

Epigenetics Chromatin. 2023 May 13;16(1):18

A549 lung adenocarcinoma cells

50 nM

24 h

Inhibition of KDM1A, leading to accumulation of H3K9 methylation and loss of H3K9 acetylation

Epigenetics Chromatin. 2023 May 13;16(1):18

BT-474 cells

10 µmol/L

48 hours

Evaluate the inhibitory effect of iadademstat on SOX2 enhancer-driven transcriptional activation, showing a dose-dependent reduction in reporter activity

Aging (Albany NY). 2020 Mar 18;12(6):4794-4814

MDA-MB-436 cells

3.98 µmol/L (IC50)

6 days

Evaluate the inhibitory effect of iadademstat on CSC-driven mammosphere formation, showing a dose-dependent decrease in mammosphere number

Aging (Albany NY). 2020 Mar 18;12(6):4794-4814

Iadademstat 2HCl 动物实验

Species Rats	Animal Model Sprague-Dawley rats	Administration	Dosage	Frequency	Description	References
Rats	Sprague-Dawley rats	Oral	2.5 μg/kg and 15 μg/kg	Single dose or 5 consecutive days	To evaluate the pharmacokinetics and pharmacodynamics relationship of ORY-1001, results showed maximum target engagement in PBMCs at 24 h after single dose and 6 h after repeated administration for 5 days, and target inhibition persisted after plasma levels returned to baseline	J Biol Chem. 2019 May 17;294(20):8311-8322

Species

Rats

Animal Model

Sprague-Dawley rats

Administration

Dosage

Frequency

Description

References

Rats

Sprague-Dawley rats

Oral

2.5 μg/kg and 15 μg/kg

Single dose or 5 consecutive days

To evaluate the pharmacokinetics and pharmacodynamics relationship of ORY-1001, results showed maximum target engagement in PBMCs at 24 h after single dose and 6 h after repeated administration for 5 days, and target inhibition persisted after plasma levels returned to baseline

J Biol Chem. 2019 May 17;294(20):8311-8322

Iadademstat 2HCl 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.30mL

0.66mL

0.33mL

16.49mL

3.30mL

1.65mL

32.97mL

6.59mL

3.30mL

Iadademstat 2HCl 技术信息

CAS号	1431303-72-8
分子式	C₁₅H₂₄Cl₂N₂
分子量	303.27
SMILES Code	N[C@@H]1CC[C@](N[C@H]2[C@H](C3=CC=CC=C3)C2)([H])CC1.[H]Cl.[H]Cl
MDL No.	N/A

别名	ORY-1001 dihydrochloride; RG6016 dihydrochloride; RO 7051790 dihydrochloride; Iadademstat dihydrochloride
运输	蓝冰

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：

H₂O: 55 mg/mL(181.36 mM)

动物实验：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

Iadademstat 2HCl {[allProObj[0].p_purity_real_show]}

Iadademstat 2HCl 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Iadademstat 2HCl 质控信息

Iadademstat 2HCl 生物活性

Iadademstat 2HCl 细胞实验

Iadademstat 2HCl 动物实验

Iadademstat 2HCl 实验方案

Iadademstat 2HCl 技术信息

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Iadademstat 2HCl 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Iadademstat 2HCl 质控信息

Iadademstat 2HCl 生物活性

Iadademstat 2HCl 细胞实验

Iadademstat 2HCl 动物实验

Iadademstat 2HCl 实验方案

Iadademstat 2HCl 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

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