Art. -Nr.: HY-109117

Iadademstat

Name: Iadademstat
Brand: MedChemExpress
SKU: HY-109117
Price: 110.00 USD
Availability: InStock
Rating: 5 (7 reviews)

(Synonyms: ORY-1001)

7 Cited Publications

Kundenbewertung

Based on 7 publication(s) in Google Scholar

Iadademstat (ORY-1001) is a highly potent, orally active and selective LSD1 (KDM1A) inhibitor with antileukemic activity. Iadademstat can be used for relapsed or refractory acute myeloid leukemia research.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.82%
CAS. Nr.: 1431304-21-0
Formel: C₁₅H₂₂N₂
Molecular Weight:230.35

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Iadademstat Chemical Structure

CAS. Nr.: 1431304-21-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (7)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

LSD1

Alle Histone Demethylase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Leukemia cell	EC₅₀	0.1 nM Compound: ORY-1001	Antitumor activity against human Leukemia cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antitumor activity against human Leukemia cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 38214982]
MV4-11	IC₅₀	>20 μM Compound: 2; ORY-1001	Antiproliferative activity against human MV4-11 cells after 3 days by MTS assay Antiproliferative activity against human MV4-11 cells after 3 days by MTS assay	[PMID: 29031059]
MV4-11	IC₅₀	0.03 μM Compound: 2; ORY-1001	Antiproliferative activity against human MV4-11 cells after 10 days by MTS assay Antiproliferative activity against human MV4-11 cells after 10 days by MTS assay	[PMID: 29031059]
RPMI-8226	IC₅₀	>20 μM Compound: 2; ORY-1001	Antiproliferative activity against human RPMI8226 cells after 10 days by MTS assay Antiproliferative activity against human RPMI8226 cells after 10 days by MTS assay	[PMID: 29031059]
RPMI-8226	IC₅₀	>20 μM Compound: 2; ORY-1001	Antiproliferative activity against human RPMI8226 cells after 3 days by MTS assay Antiproliferative activity against human RPMI8226 cells after 3 days by MTS assay	[PMID: 29031059]
THP-1	IC₅₀	>50 μM Compound: ORY-1001	Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo assay Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by celltiter glo assay	[PMID: 37086699]

In Vitro

Iadademstat (80-160 μM, 24 h-15 days) inhibits the proliferation of cancer cells H1299 and A549, arrests the cell cycle at G1 phase, induces apoptosis and inhibits the colony formation of H1299 and A549^[2].
Iadademstat (80-160 μM, 24 h) decreases glycolysis in H1299 and A549 cells by reducing HK2 protein levels^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[2]

Cell Line:

H1299 and A549
Concentration:

80-160 μM
Incubation Time:

1-4 days
Result:

Inhibited cell proliferation.

Apoptosis Analysis^[2]

Cell Line:

H1299 and A549
Concentration:

80-160 μM
Incubation Time:

24 h
Result:

Induced apoptosis.

Cell Cycle Analysis^[2]

Cell Line:

H1299 and A549
Concentration:

80-160 μM
Incubation Time:

48 h
Result:

Arrested the cell cycle at G1 phase.

In Vivo

Iadademstat (400 µg/kg, po, every 7 days for 28 days) exhibits antitumor activity in glioblastoma xenograft mouse model^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Glioblastoma xenograft mouse model^[3]
Dosage:

400 µg/kg
Administration:

po, every 7 days for 28 days
Result:

Inhibited the growth of tumors, increased the survival rate.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1431304-21-0
Appearance Solid
Molecular Weight 230.35
Formel C₁₅H₂₂N₂
Color White to off-white
SMILES

N[C@@H]1CC[C@@](CC1)([H])N[C@H]2[C@H](C3=CC=CC=C3)C2
Synonyms

ORY-1001
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (7)

All Cell Proliferation/Viability AssayCell Migration/Invasion AssayFlow CytometryIn Vivo ImagingWB

Sort by:

Journal Impact Factor

Oncogene

BRD4 inhibition sensitizes cervical cancer to radiotherapy by attenuating DNA repair. [Abstract]

2021 Apr;40(15):2711-2724. PMID: 33712705
EMBO Mol Med

Dual targeting of CDK6 and LSD1 is synergistic and overcomes differentiation blockade in AML. [Abstract]

2025 Aug 29. PMID: 40883610

Iadademstat purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2025 Aug 29. [Abstract]

MV4-11 cells cocultured with HS-5 stromal cells were incubated with CDK6 inhibitor ribociclib at 1 μM, with ORY-1001 (ORY, Iadademstat dihydrochloride) at 0.5 nM, or with the combination of ribociclib and ORY-1001 (Combo) for 96 h. After the treatment, leukemic cells were seeded in equal numbers in methylcellulose for 10 days.

Iadademstat purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2025 Aug 29. [Abstract]

MV4-11 cells transfected with control (Ctrl) or CDK6 siRNAs were incubated with 5 μM TCP or 0.5 nM ORY-1001 (ORY, Iadademstat dihydrochloride), as indicated, for 4 days. The percentage of CD11b-expressing cells was assessed by flow cytometry (left panel).

Iadademstat purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2025 Aug 29. [Abstract]

Bioluminescent imaging of NSG mice at day 24, post-xenotransplantation of 2 × 10⁵ luciferase-labeled MOLM-14 cells. Mice were treated by intraperitoneal injections of either palbociclib (25 mg/kg), Iadademstat dihydrochloride (ORY-1001, ORY, 0.0125 mg/kg), the combination of the two molecules or vehicle control, for 4 weeks.

Iadademstat purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2025 Aug 29. [Abstract]

Quantification of hCD45 + hCD33+ leukemic blast cells in NSG mice transplanted with primary AML patient cells. Treatment with the combination of palbociclib and Iadademstat dihydrochloride (ORY-1001, ORY, 0.0125 mg/kg; i.p.) was initiated once the engraftment was confirmed by the appearance of blast cells in the bloodstream, and were administered for 3–6 weeks until an endpoint was reached. The percentage of human myeloid cells was assessed by flow cytometry in the bone marrow. PDX#1 p < 0.0001 ; PDX#2 p < 0.0001 ; PDX#3 p = 0.3301 ; PDX#4 p = 0.0033 ; PDX#5 p = 0.0368.
J Med Chem

The Exploration of Indole-Based LSD1-Targeted Inhibitors for Enhanced Immune Response in Gastric Cancer via the PD-L1/PD-1 Axis. [Abstract]

2025 Apr 21. PMID: 40257403

Iadademstat purchased from MedChemExpress. Usage Cited in: J Med Chem. 2025 Apr 21. [Abstract]

Iadademstat dihydrochloride (ORY-1001, 2 μM; 2 days) inhibited the invasion of MKN-45 cells.

Iadademstat purchased from MedChemExpress. Usage Cited in: J Med Chem. 2025 Apr 21. [Abstract]

Iadademstat dihydrochloride (ORY-1001, 2 μM) inhibited the migration of MKN-45 cells.

Iadademstat purchased from MedChemExpress. Usage Cited in: J Med Chem. 2025 Apr 21. [Abstract]

Iadademstat dihydrochloride (ORY-1001, 2 μM; 5 days) significantly reduced PD-L1 protein levels in MKN-45 and MFC cell lines.

Iadademstat purchased from MedChemExpress. Usage Cited in: J Med Chem. 2025 Apr 21. [Abstract]

Iadademstat dihydrochloride (ORY-1001, 2 μM; 5 days) reduced membrane PD-L1 levels in MKN-45 and MFC cell lines.
J Med Chem

Target Ligand Separation and Identification of Isoforsythiaside as a Histone Lysine-Specific Demethylase 1 Covalent Inhibitor Against Breast Cancer Metastasis. [Abstract]

2024 Nov 14;67(21):19874-19888. PMID: 39499621
Cell Biosci

Motoneurons innervation determines the distinct gene expressions in multinucleated myofibers. [Abstract]

2022 Aug 30;12(1):140 PMID: 36042463
J Appl Toxicol

Influences of lysine-specific demethylase 1 inhibitors on NO synthase-Kruppel-like factor pathways in human endothelial cells in vitro and zebrafish (Danio rerio) larvae in vivo. [Abstract]

2023 Nov;43(11):1748-1760. PMID: 37408164
bioRxiv

Co-targeting menin and LSD1 dismantles oncogenic programs and restores differentiation in MLL-rearranged AML. [Abstract]

2025 Oct 15:2025.10.13.681683. PMID: 41279447

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (108.53 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.3412 mL

21.7061 mL

43.4122 mL

5 mM

0.8682 mL

4.3412 mL

8.6824 mL

10 mM

0.4341 mL

2.1706 mL

4.3412 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (10.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (10.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (10.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Olga Salamero, et al. First-in-Human Phase I Study of Iadademstat (ORY-1001): A First-in-Class Lysine-Specific Histone Demethylase 1A Inhibitor, in Relapsed or Refractory Acute Myeloid Leukemia. J Clin Oncol. 2020 Dec 20;38(36):4260-4273. [Content Brief]

[2]. Lu Z, et al., ORY-1001 Suppresses Cell Growth and Induces Apoptosis in Lung Cancer Through Triggering HK2 Mediated Warburg Effect. Front Pharmacol. 2018 Dec 4;9:1411. [Content Brief]

[3]. Yang H, et al., [ORY-1001 inhibits glioblastoma cell growth by downregulating the Notch/HES1 pathway via suppressing lysine-specific demethylase 1 expression]. Nan Fang Yi Ke Da Xue Xue Bao. 2024 Aug 20;44(8):1620-1630. Chinese. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	4.3412 mL	21.7061 mL	43.4122 mL	108.5305 mL
	5 mM	0.8682 mL	4.3412 mL	8.6824 mL	21.7061 mL
	10 mM	0.4341 mL	2.1706 mL	4.3412 mL	10.8530 mL
	15 mM	0.2894 mL	1.4471 mL	2.8941 mL	7.2354 mL
	20 mM	0.2171 mL	1.0853 mL	2.1706 mL	5.4265 mL
	25 mM	0.1736 mL	0.8682 mL	1.7365 mL	4.3412 mL
	30 mM	0.1447 mL	0.7235 mL	1.4471 mL	3.6177 mL
	40 mM	0.1085 mL	0.5427 mL	1.0853 mL	2.7133 mL
	50 mM	0.0868 mL	0.4341 mL	0.8682 mL	2.1706 mL
	60 mM	0.0724 mL	0.3618 mL	0.7235 mL	1.8088 mL
	80 mM	0.0543 mL	0.2713 mL	0.5427 mL	1.3566 mL
	100 mM	0.0434 mL	0.2171 mL	0.4341 mL	1.0853 mL

Bioz

Keywords

Iadademstat

7 Cited Publications

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Iadademstat

Publications Citing Use of MedChemExpress (MCE) Iadademstat

Alle Histone Demethylase Isoform-spezifische Produkte anzeigen