MI-389
Based on 1 Customer Validation
MI-389 is a potent menin-MLL interaction inhibitor (IC50=25 nM) and a CRBN-recruiting, GSPT1-targeted PROTAC degrader. MI-389 upregulates myeloid differentiation-related genes that are lowly expressed in primitive hematopoietic progenitor cells, thereby inducing myeloid differentiation phenotypic changes in MLL-rearranged leukemia cells. MI-389 competitively blocks the MG-H1-RAGE interaction to interfere with the AGEs-RAGE pathway, thus alleviating AGEs-induced HUVEC injury. MI-389 can be used in studies related to MLL-rearranged acute leukemia.
(Pink: eRF3a/GSPT1 ligand (HY-76719); Blue: Cereblon ligand (HY-10984); Black: linker).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.34%
- CAS No.: 2222635-92-7
- 화학식: C35H35FN6O6
- 분자량:654.69
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보관:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
eRF3a/GSPT1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Kasumi 1 | EC50 |
21.3 nM
Compound: 18; MI-389
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Antiproliferative activity against human Kasumi 1 cells assessed as reduction in cell viability incubated for 72 hrs by Cell-titer glo luminescent assay
Antiproliferative activity against human Kasumi 1 cells assessed as reduction in cell viability incubated for 72 hrs by Cell-titer glo luminescent assay
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[PMID: 39094274] |
In Vitro
MI-389 potently inhibits the menin-MLL interaction in cell-free assays, with an IC50 of 25 nM and a Kd of 21 nM for binding to menin[1].
MI-389 (0.74-1.69 μM; 7 days) selectively inhibits the growth of MLL-rearranged leukemia cells (MV4;11, MOLM-13, MLL-AF9 BMCs) with GI50 values ranging from 0.74-1.69 μM, while showing no activity against non-MLL leukemia cells (Jurkat, HM-2 BMCs) after 7 days of treatment[1].
MI-389 (4 μM; 6 days) reverses the MLL fusion-driven gene expression signature in MV4;11 human MLL leukemia cells, downregulating oncogenic MLL target genes and upregulating differentiation-associated genes after 6 days of treatment with 4 μM MI-389[1].
MI-389 (2 μM; 6 days) downregulates oncogenic MLL target genes and upregulates the myeloid differentiation marker MNDA in MOLM-13 human MLL leukemia cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MLL-rearranged human leukemia cell lines (MV4;11, MOLM-13), MLL-AF9 transformed murine bone marrow cells (BMCs), non-MLL leukemia cell lines (Jurkat, HM-2 transformed BMCs)
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Concentration:0.74-1.69 μM (MLL-rearranged cells); >5 μM (non-MLL leukemia cells)
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Incubation Time:7 days
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Result:Inhibited growth of MV4;11 cells with a GI50 of 0.74 μM.
Inhibited growth of MOLM-13 cells with a GI50 of 1.69 μM.
Inhibited growth of MLL-AF9 transformed BMCs with a GI50 of 0.78 μM.
Showed no significant growth inhibition in Jurkat cells or HM-2 transformed BMCs (GI50 >5 μM for both).
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Cell Line:MOLM-13 human MLL leukemia cells
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Concentration:2 μM
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Incubation Time:6 days
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Result:Markedly downregulated expression of MLL fusion target genes: HOXA9, MEIS1, HOXA10, HOXA7, PBX3, DLX2, FLT3, and MEF2C.
Upregulated expression of MNDA, a myeloid differentiation marker, by approximately 7-fold relative to DMSO-treated controls.
Chemical Information
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CAS No. 2222635-92-7
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Appearance Solid
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분자량 654.69
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화학식 C35H35FN6O6
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Color Yellow to orange
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SMILES
O=C1C2=C(NCCCCCCNC(C3=C(C)NC(/C=C4C5=CC(F)=CC=C5NC/4=O)=C3C)=O)C=CC=C2C(N1C6C(NC(CC6)=O)=O)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
용액&용해도
In Vitro:
DMSO : 66.67 mg/mL (101.83 mM; Need ultrasonic; 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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[2]. Feng L, et al. Competitive binding between 4,4'-diphenylmethane-bis(methyl) carbamate and RAGE ligand MG-H1 on human umbilical vein endothelial cell by cell membrane chromatography. Journal of chromatography. B, Analytical technologies in the biomedical and life sciences. 2012 Jan 15;881-882:55-62. [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, 6 months; -20°C, 1 month (stored under nitrogen). 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 | 1.5274 mL | 7.6372 mL | 15.2744 mL | 38.1860 mL |
| 5 mM | 0.3055 mL | 1.5274 mL | 3.0549 mL | 7.6372 mL | |
| 10 mM | 0.1527 mL | 0.7637 mL | 1.5274 mL | 3.8186 mL | |
| 15 mM | 0.1018 mL | 0.5091 mL | 1.0183 mL | 2.5457 mL | |
| 20 mM | 0.0764 mL | 0.3819 mL | 0.7637 mL | 1.9093 mL | |
| 25 mM | 0.0611 mL | 0.3055 mL | 0.6110 mL | 1.5274 mL | |
| 30 mM | 0.0509 mL | 0.2546 mL | 0.5091 mL | 1.2729 mL | |
| 40 mM | 0.0382 mL | 0.1909 mL | 0.3819 mL | 0.9547 mL | |
| 50 mM | 0.0305 mL | 0.1527 mL | 0.3055 mL | 0.7637 mL | |
| 60 mM | 0.0255 mL | 0.1273 mL | 0.2546 mL | 0.6364 mL | |
| 80 mM | 0.0191 mL | 0.0955 mL | 0.1909 mL | 0.4773 mL | |
| 100 mM | 0.0153 mL | 0.0764 mL | 0.1527 mL | 0.3819 mL |
MI-389 Related Classifications
HY-136688 Related Classifications
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Keywords
- MI-389
- 2222635-92-7
- MI389
- MI 389
- PROTACs
- Eukaryotic Release Factor (eRF)
- Epigenetic Reader Domain
- menin-MLL interaction
- homeobox genes
- leukemogenesis-related genes
- MLL-rearranged leukemia cells
- MOLM-13
- menin-MLL fusion protein
- myeloid differentiation-associated genes
- MLL-AF9 BMCs
- primitive hematopoietic progenitor cells
- MV4;11
- Inhibitor
- inhibitor
- inhibit