DG013A formate
Based on 1 Customer Validation
DG013A formate is a zinc-dependent M1-aminopeptidase inhibitor that exhibits inhibitory activity against ERAP1 (IC50 = 33 nM) and ERAP2 (IC50 = 11 nM). DG013A formate enhances SRHFLAFSFR epitope presentation, rescues GSW11 peptide neoantigen presentation, reduces SIINFEKL presentation, modulates the immunopeptidome, decreases HLA-B27 free heavy chain expression, and reduces IL-17A secretion. DG013A formate exhibits antiproliferative activity. DG013A formate can be used for research on autoimmune diseases and melanoma.
For research use only. We do not sell to patients.
- Purity : 99.57%
- Formula: C30H43N4O10P
- Molecular Weight:650.66
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[2]|
IL-17A |
In Vitro
DG013A exhibits negligible passive permeability in Caco-2 cells, which is inconsistent with its use as a convertible intracellular chemical probe[1].
DG013A is a potent nanomolar ERAP1 inhibitor (IC50 = 33 nM) and ERAP2 inhibitor (IC50 = 11 nM), and it also inhibits IRAP and APN, with its binding to ERAP2 involving coordination of its phosphonic acid group with the active-site zinc ion[2].
DG013A is a potent inhibitor of recombinant ERAP1 with an IC50 of 43.5 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A375 human malignant melanoma cells
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Concentration:0-30 μM
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Incubation Time:48 h
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Result:Did not appear to be toxic to A375 cells up to a concentration of 30 μM.
Chemical Information
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Appearance Solid
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Molecular Weight 650.66
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Formula C30H43N4O10P
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Color White to off-white
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SMILES
O=P([C@@H](N)CCC1=CC=CC=C1)(O)C[C@@H](CC(C)C)C(N[C@H](C(N)=O)CC2=CNC3=CC=CC=C23)=O.O=CO.O=CO.O=CO
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (76.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 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
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. 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 |
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| DMSO | 1 mM | 1.5369 mL | 7.6845 mL | 15.3690 mL | 38.4225 mL |
| 5 mM | 0.3074 mL | 1.5369 mL | 3.0738 mL | 7.6845 mL | |
| 10 mM | 0.1537 mL | 0.7685 mL | 1.5369 mL | 3.8423 mL | |
| 15 mM | 0.1025 mL | 0.5123 mL | 1.0246 mL | 2.5615 mL | |
| 20 mM | 0.0768 mL | 0.3842 mL | 0.7685 mL | 1.9211 mL | |
| 25 mM | 0.0615 mL | 0.3074 mL | 0.6148 mL | 1.5369 mL | |
| 30 mM | 0.0512 mL | 0.2562 mL | 0.5123 mL | 1.2808 mL | |
| 40 mM | 0.0384 mL | 0.1921 mL | 0.3842 mL | 0.9606 mL | |
| 50 mM | 0.0307 mL | 0.1537 mL | 0.3074 mL | 0.7685 mL | |
| 60 mM | 0.0256 mL | 0.1281 mL | 0.2562 mL | 0.6404 mL |
DG013A formate Related Classifications
HY-139907B Related Classifications
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