1G244
Based on 6 publication(s) in Google Scholar
1G244 is a potent DPP8/9 inhibitor with IC50s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.50%
- CAS. Nr.: 847928-32-9
- Formel: C29H30F2N4O2
- Molecular Weight:504.57
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Speicherung:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Apoptosis Compound Library
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Publications Citing Use of MedChemExpress (MCE) 1G244
More
Biologische Aktivität
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DPP-4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>100 μM
Compound: 2; 1G244
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Inhibition of BALB/c mouse 5'-His6-tagged 3'-FLAG-tagged FAP fused with ECD expressed in HEK293 cells using Ala-Pro-p-nitroanilide as substrate preincubated for 15 mins followed by substrate addition measured for 10 mins by spectrofluorimetry
Inhibition of BALB/c mouse 5'-His6-tagged 3'-FLAG-tagged FAP fused with ECD expressed in HEK293 cells using Ala-Pro-p-nitroanilide as substrate preincubated for 15 mins followed by substrate addition measured for 10 mins by spectrofluorimetry
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10.1039/C5MD00454C |
| Sf9 | IC50 |
0.012 μM
Compound: 2; 1G244
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Inhibition of full length human DPP8 expressed in baculovirus infected sf9 cells using Ala-Pro-p-nitroanilide as substrate preincubated for 15 mins followed by substrate addition measured for 10 mins by spectrofluorimetry
Inhibition of full length human DPP8 expressed in baculovirus infected sf9 cells using Ala-Pro-p-nitroanilide as substrate preincubated for 15 mins followed by substrate addition measured for 10 mins by spectrofluorimetry
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10.1039/C5MD00454C |
1G244 (0-100 μM; 72 hours; Delta47, U266 , KMS-5, RPMI8226, or MM.1 S cells) treatment dose-dependently decreases viable cell number of five multiple myeloma cell lines[1].
1G244 (50 μM; 0-48 hours; MM.1 S cells) treatment induces apoptosis, as cleaved forms of both caspase-3 and PARP are detected[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Delta47, U266 , KMS-5, RPMI8226, or MM.1 S cells
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Concentration:0 μM, 1 μM, 5 μM, 10 μM, 50 μM, or 100 μM
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Incubation Time:72 hours
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Result:Dose-dependently decreased viable cell number of five multiple myeloma cell lines.
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Cell Line:MM.1 S cells
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Concentration:50 μM
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Incubation Time:0 hour, 3 hours, 6 hours, 12 hours, 24 hours, 48 hours
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Result:Decreased caspase-3 and PARP protein.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/Shi-scid IL-2Rγnull (NOG) female mice (6-7 weeks; 19-21 g) injected with MM.1 S cells[1]
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Dosage:30 mg/kg
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Administration:Subcutaneous injection; once-a-week; for 3 weeks
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Result:Apparently suppressed the subcutaneous growth of MM.1 S cells in murine xenograft model.
Chemical Information
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CAS. Nr. 847928-32-9
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Appearance Solid
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Molecular Weight 504.57
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Formel C29H30F2N4O2
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Color Off-white to light yellow
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SMILES
O=C(N1CC2=C(C=CC=C2)C1)[C@@H](N)CC(N3CCN(C(C4=CC=C(F)C=C4)C5=CC=C(F)C=C5)CC3)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (6)
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Journal Impact Factor
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Most Recent
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Nature
2025 Jun;642(8066):222-231. PMID: 40205054 -
Cell
2024 Feb 29;187(5):1223-1237.e16. PMID: 38428396 -
Nat Chem Biol
2023 Apr;19(4):431-439. PMID: 36357533 -
Int J Biol Macromol
Z-VAD(OMe)-FMK suppresses Seneca Valley Virus replication by targeting the active sites of the 3C protease. [Abstract]2025 May;306(Pt 3):141587. PMID: 40032110 -
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Lösungsmittel & Löslichkeit
DMSO : 250 mg/mL (495.47 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 (sealed storage, away from moisture and 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.12 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (278 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)
Verweise
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 (sealed storage, away from moisture and 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 | 1.9819 mL | 9.9094 mL | 19.8189 mL | 49.5471 mL |
| 5 mM | 0.3964 mL | 1.9819 mL | 3.9638 mL | 9.9094 mL | |
| 10 mM | 0.1982 mL | 0.9909 mL | 1.9819 mL | 4.9547 mL | |
| 15 mM | 0.1321 mL | 0.6606 mL | 1.3213 mL | 3.3031 mL | |
| 20 mM | 0.0991 mL | 0.4955 mL | 0.9909 mL | 2.4774 mL | |
| 25 mM | 0.0793 mL | 0.3964 mL | 0.7928 mL | 1.9819 mL | |
| 30 mM | 0.0661 mL | 0.3303 mL | 0.6606 mL | 1.6516 mL | |
| 40 mM | 0.0495 mL | 0.2477 mL | 0.4955 mL | 1.2387 mL | |
| 50 mM | 0.0396 mL | 0.1982 mL | 0.3964 mL | 0.9909 mL | |
| 60 mM | 0.0330 mL | 0.1652 mL | 0.3303 mL | 0.8258 mL | |
| 80 mM | 0.0248 mL | 0.1239 mL | 0.2477 mL | 0.6193 mL | |
| 100 mM | 0.0198 mL | 0.0991 mL | 0.1982 mL | 0.4955 mL |
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