1. Metabolic Enzyme/Protease
    Apoptosis
  2. Dipeptidyl Peptidase
    Apoptosis
  3. 1G244

1G244 

Cat. No.: HY-116304 Purity: >98.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

1G244 Chemical Structure

1G244 Chemical Structure

CAS No. : 847928-32-9

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25 mg USD 1233 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

IC50 & 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.
Molecular Weight

504.57

Formula

C₂₉H₃₀F₂N₄O₂

CAS No.

847928-32-9

SMILES

O=C(N1CC2=C(C=CC=C2)C1)[[email protected]@H](N)CC(N3CCN(C(C4=CC=C(F)C=C4)C5=CC=C(F)C=C5)CC3)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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)

References

Purity: >98.0%

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Keywords:

1G244Dipeptidyl PeptidaseApoptosisDPPDipeptidylpeptidasesDPP8DPP9anti-myelomaapoptosiscelldeathcaspases-3PARPInhibitorinhibitorinhibit

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1G244
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