MMRi62
Based on 1 Customer Validation
MMRi62, a ferroptosis inducer targeting MDM2-MDM4 (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. MMRi62 inducesferroptosis, resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12.
For research use only. We do not sell to patients.
- Purity: 99.59%
- CAS No.: 352693-80-2
- Formula: C21H15Cl2N3O
- Molecular Weight:396.27
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | CC50 |
>100 μM
Compound: GNF-Pf-5250
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NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
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[PMID: 18579783] |
MMRi62 inhibits proliferation, clonogenic, and spheroid growth of pancreatic ductal adenocarcinoma cell (PDAC) by induction of cell death[1].
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MMRi62 (3 nM-100 μM;4 h) binds to RING–RINGheterodimers of MDM2 and MDM4 withthe Kd value of 1.39 μM[2].
MMRi62 (10 nM-1 μM;72 h) induces apoptosis and inhibits leukemic cells with IC50sof 0.34 μM (HL60) and 0.22 μM (HL60VR)[2].
MMRi62 (5 μM and 10μM; 24 h) decreases MDM2B autoubiquitination, increasesMDM4 ubiquitination in a dose-dependent manner[2].
MMRi62 is an E3 ligase modifier capable ofswitching substrate preference from MDM2 to MDM4[2].
MMRi62 (5 μM; 24and 72 h) induces apoptosis in a p53-independent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:WT-p53 bearing MV4-11 cells; 293cells transfected with MDM2B and MDM4
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Concentration:2, 2.5, 5, 10, 40, 80, 160 μM
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Incubation Time:24 hours
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Result:Increased cleaved PARP protein and activatedcaspase 3 level in wt-p53 bearing MV4-11 cells at 2 μM for 24 h.
Decreased MDM2B autoubiquitination, increasedMDM4 ubiquitination at 5 μM and 10 μM for 24 h.
Induced MDM2-dependent degradation of MDM4protein at 5 μM in NALM6 cells.
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Cell Line:Primary AML patient cells, NALM6cells and NALM6shp53 cells
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Concentration:1, 10, 25, and 50 µM
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Incubation Time:24 hours and 72 hours
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Result:Induced NALM6 cells apoptosis at 24 hand induced Primary AML patient cells at 72 h.
MMRi62 also completely abrogates metastasis of orthotopic tumors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 352693-80-2
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Appearance Solid
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Molecular Weight 396.27
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Formula C21H15Cl2N3O
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Color White to off-white
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SMILES
OC1=C2N=CC=CC2=CC=C1C(C3=CC=CC(Cl)=C3Cl)NC4=NC=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 62.5 mg/mL (157.72 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)
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 (protect from light). 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 (protect from light). 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)
Purity & Documentation
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Data Sheet (280 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
[1]. Li J, et al. Small-Molecule MMRi62 Induces Ferroptosis and Inhibits Metastasis in Pancreatic Cancer via Degradation of Ferritin Heavy Chain and Mutant p53. Mol Cancer Ther. 2022 Apr 1;21(4):535-545. [Content Brief]
[2]. Lama R, et al. Small molecule MMRi62 targets MDM4 for degradation and induces leukemic cell apoptosis regardless of p53 status. Front Oncol. 2022 Aug 5;12:933446. [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 (protect from light). 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 | 2.5235 mL | 12.6177 mL | 25.2353 mL | 63.0883 mL |
| 5 mM | 0.5047 mL | 2.5235 mL | 5.0471 mL | 12.6177 mL | |
| 10 mM | 0.2524 mL | 1.2618 mL | 2.5235 mL | 6.3088 mL | |
| 15 mM | 0.1682 mL | 0.8412 mL | 1.6824 mL | 4.2059 mL | |
| 20 mM | 0.1262 mL | 0.6309 mL | 1.2618 mL | 3.1544 mL | |
| 25 mM | 0.1009 mL | 0.5047 mL | 1.0094 mL | 2.5235 mL | |
| 30 mM | 0.0841 mL | 0.4206 mL | 0.8412 mL | 2.1029 mL | |
| 40 mM | 0.0631 mL | 0.3154 mL | 0.6309 mL | 1.5772 mL | |
| 50 mM | 0.0505 mL | 0.2524 mL | 0.5047 mL | 1.2618 mL | |
| 60 mM | 0.0421 mL | 0.2103 mL | 0.4206 mL | 1.0515 mL | |
| 80 mM | 0.0315 mL | 0.1577 mL | 0.3154 mL | 0.7886 mL | |
| 100 mM | 0.0252 mL | 0.1262 mL | 0.2524 mL | 0.6309 mL |
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