Iadademstat dihydrochloride
Based on 9 publication(s) in Google Scholar
Iadademstat (ORY-1001) dihydrochloride is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.96%
- No. CAS: 1431303-72-8
- Fòrmula: C15H24Cl2N2
- Peso molecular:303.27
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Iadademstat dihydrochloride
More- Oncogene. 2021 Apr;40(15):2711-2724. [Abstract]
- EMBO Mol Med. 2025 Aug 29. [Abstract]
- J Med Chem. 2025 Apr 21. [Abstract]
- J Med Chem. 2024 Nov 14;67(21):19874-19888. [Abstract]
- Cell Biosci. 2022 Aug 30;12(1):140 [Abstract]
- Bioorg Chem. 2026 Oct 5:181:110366.
- J Appl Toxicol. 2023 Nov;43(11):1748-1760. [Abstract]
- Biomed Pharmacother. 2026 Sep:202:119803.
- bioRxiv. 2025 Oct 15:2025.10.13.681683. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Flow Cytometry
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In Vivo Imaging
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Flow Cytometry
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Cell Migration/Invasion Assay
Actividad biológica
Descripciòn
IC50 & Target
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KDM1/LSD1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| AGS | IC50 |
>50 μM
Compound: ORY-1001
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Antiproliferative activity against human AGS cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human AGS cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
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[PMID: 33957387] |
| BGC-823 | IC50 |
>50 μM
Compound: ORY-1001
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Antiproliferative activity against human BGC-823 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human BGC-823 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
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[PMID: 33957387] |
| MKN-1 | IC50 |
>50 μM
Compound: ORY-1001
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Antiproliferative activity against human MKN-1 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human MKN-1 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
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[PMID: 33957387] |
| MKN-45 | IC50 |
>50 μM
Compound: ORY-1001
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Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
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[PMID: 33957387] |
| MM1.S | EC50 |
>10 μM
Compound: ORY-1001
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Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability after 144 hrs
Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability after 144 hrs
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[PMID: 33359604] |
| NCI-N87 | IC50 |
>50 μM
Compound: ORY-1001
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Antiproliferative activity against human NCI-N87 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human NCI-N87 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
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[PMID: 33957387] |
| SNU1 | IC50 |
>50 μM
Compound: ORY-1001
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Antiproliferative activity against human SNU1 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human SNU1 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
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[PMID: 33957387] |
| THP-1 | IC50 |
>20 μM
Compound: ORY-1001
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Antiproliferative activity against human THP1 cells after 8 days by MTS assay
Antiproliferative activity against human THP1 cells after 8 days by MTS assay
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[PMID: 30448189] |
In Vitro
Iadademstat dihydrochloride is a KDM1A inhibitor that inactivate KDM1A by irreversible binding to the flavin adenine nucleotide (FAD) cofactor. Iadademstat has very high selectivity for KDM1A over the MAO enzymes, high selectivity over KDM1B and unrivaled subnanomolar cellular activity in differentiation and colony formation assays on mixed lineage leukemia (MLL)-translocated acute myeloid leukemia (AML) cell lines. Iadademstat provokes a time and dose-dependent induction of the Cd11b differentiation marker in MLL-AF9 cells, which interestingly preceeds changes in H3K4me2 levels. While MLL-translocated cells are especially sensitive, other acute leukemia (AL) cell lines also respond to Iadademstat[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1431303-72-8
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Appearance Solid
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Peso molecular 303.27
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Fòrmula C15H24Cl2N2
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Color White to off-white
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SMILES
N[C@@H]1CC[C@@H](N[C@H]2[C@H](C3=CC=CC=C3)C2)CC1.[H]Cl.[H]Cl
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Synonyms
ORY-1001 dihydrochloride; RG6016 dihydrochloride; RO 7051790 dihydrochloride
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (9)
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Journal Impact Factor
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Most Recent
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Oncogene
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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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.
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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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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.
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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 -
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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 -
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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
Solvente y solubilidad
In Vitro:
H2O : 57.75 mg/mL (190.42 mM; Need ultrasonic and warming)
DMSO : 0.69 mg/mL (2.28 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (329.74 mM); Clear solution; Need ultrasonic
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Maes T, et al. KDM1 histone lysine demethylases as targets for treatments of oncological and neurodegenerative disease. Epigenomics. 2015;7(4):609-26. doi: 10.2217/epi.15.9. [Content Brief]
[2]. Tamara Maes, et al. ORY-1001, a Potent and Selective Covalent KDM1A Inhibitor, for the Treatment of Acute Leukemia. Cancer Cell. 2018 Mar 12;33(3):495-511.e12. [Content Brief]
Complete Stock Solution Preparation Table
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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 3.2974 mL | 16.4870 mL | 32.9739 mL | 82.4348 mL |
| H2O | 5 mM | 0.6595 mL | 3.2974 mL | 6.5948 mL | 16.4870 mL |
| 10 mM | 0.3297 mL | 1.6487 mL | 3.2974 mL | 8.2435 mL | |
| 15 mM | 0.2198 mL | 1.0991 mL | 2.1983 mL | 5.4957 mL | |
| 20 mM | 0.1649 mL | 0.8243 mL | 1.6487 mL | 4.1217 mL | |
| 25 mM | 0.1319 mL | 0.6595 mL | 1.3190 mL | 3.2974 mL | |
| 30 mM | 0.1099 mL | 0.5496 mL | 1.0991 mL | 2.7478 mL | |
| 40 mM | 0.0824 mL | 0.4122 mL | 0.8243 mL | 2.0609 mL | |
| 50 mM | 0.0659 mL | 0.3297 mL | 0.6595 mL | 1.6487 mL | |
| 60 mM | 0.0550 mL | 0.2748 mL | 0.5496 mL | 1.3739 mL | |
| 80 mM | 0.0412 mL | 0.2061 mL | 0.4122 mL | 1.0304 mL | |
| 100 mM | 0.0330 mL | 0.1649 mL | 0.3297 mL | 0.8243 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Iadademstat dihydrochloride Related Classifications
HY-12782T Related Classifications
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