847928-32-9
847928-32-9 structure
- Name: 1G244
- Chemical Name: 1G244
- CAS Number: 847928-32-9
- Molecular Formula: C29H30F2N4O2
- Molecular Weight: 504.57
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2020-01-23 10:50:51
- Modify Date: 2024-01-06 08:36:30
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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[1][2].
| Name | 1G244 |
|---|
| Description | 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[1][2]. |
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| Related Catalog | |
| Target |
IC50: 12 nM (DPP8), 84 nM (DPP9)[2] |
| In Vitro | 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]. Cell Viability Assay[1] Cell Line: Delta47, U266 , KMS-5, RPMI8226, or MM.1 S cells Concentration: 0 μM, 1 μM, 5 μM, 10 μM, 50 μM, or 100 μM Incubation Time: 72 hours Result: Dose-dependently decreased viable cell number of five multiple myeloma cell lines. Western Blot Analysis[1] Cell Line: MM.1 S cells Concentration: 50 μM Incubation Time: 0 hour, 3 hours, 6 hours, 12 hours, 24 hours, 48 hours Result: Decreased caspase-3 and PARP protein. |
| In Vivo | 1G244 (30 mg/kg; subcutaneous injection; once-a-week; for 3 weeks; NOG female mice) treatment apparently suppresses the subcutaneous growth of MM.1 S cells in murine xenograft model[1]. Animal Model: NOD/Shi-scid IL-2Rγnull (NOG) female mice (6-7 weeks; 19-21 g) injected with MM.1 S cells[1] Dosage: 30 mg/kg Administration: Subcutaneous injection; once-a-week; for 3 weeks Result: Apparently suppressed the subcutaneous growth of MM.1 S cells in murine xenograft model. |
| References |
| Molecular Formula | C29H30F2N4O2 |
|---|---|
| Molecular Weight | 504.57 |