PPI-2458

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PPI-2458 is a potent, orally active, selective and irreversible inhibitor of methionine aminopeptidase-2 (MetAP-2). PPI-2458 can be used for arthritis and lymphoma research.

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

PPI-2458 Chemical Structure

CAS No. : 431077-35-9

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Description

PPI-2458 is a potent, orally active, selective and irreversible inhibitor of methionine aminopeptidase-2 (MetAP-2). PPI-2458 can be used for arthritis and lymphoma research^[1]^[2].

In Vitro

PPI-2458 potently inhibits HUVEC proliferation with a GI₅₀ of 0.2 nM and a maximum inhibition of >95% at 1 nM^[1].
PPI-2458 (0-100 nM, 6 days) inhibits proliferation and MetAP-2 in SU-DHL-16 cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[2]

Cell Line:	SU-DHL-16 cells
Concentration:	0, 0.01, 0.1, 1, 10, and 100 nM
Incubation Time:	6 days
Result:	Inhibited SU-DHL-16 proliferation in a dose-dependent fashion with maximum inhibition of 60% achieved at the highest concentration (100 nmol/L) and GI₅₀ at 1.9 nmol/L.

In Vivo

PPI-2458 (0-50 mg/kg, Orally, qod) reverses joint swelling and inflammation in the PG-PS (25 mg/kg, i.p.)-induced arthritis model^[1].
PPI-2458 (0-3 mg/kg, Nasogastric intubation, qod) shows a decrease in germinal center lymphocytes in experimentally naive cynomolgus monkeys^[2].
PPI-2458 (0-100 mg/kg, Orally, qod) significantly suppresses tumor growth in a dose-dependent manner in severe combined immunodeficient mice with SR tumor xenografts ^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female Lewis rats (101–121 g, PG-PS (25 mg/kg, i.p.)-induced arthritis model)^[1]
Dosage:	0.25, 1, 5, and 50 mg/kg
Administration:	Orally (po), started at day 15 after the chronic destructive phase of the disease was established and terminated on day 31
Result:	Significantly and dose-dependently attenuated the chronic inflammatory response. Markedly attenuated paw swelling in a dose-dependent manner with maximal protection at an orally administered dose of 50 mg/kg at day 31.

Animal Model:	Forty-two experimentally naive cynomolgus monkeys^[2]
Dosage:	0.1 mg/kg (three males and three females), 0.3 mg/kg (three males and three females), 1.0 mg/kg (five males and five females), and 3.0 mg/kg (five males and five females)
Administration:	Nasogastric intubation every other day (QOD) for 13 days (total of seven treatments)
Result:	Exhibited a marked decrease in germinal center lymphocytes.

Animal Model:	60 female Fox Chase severe combined immunodeficient mice (SR lymphoma cells were injected s.c. above the right hind leg)^[2]
Dosage:	10, 30, or 100 mg/kg
Administration:	oral gavage, QOD
Result:	Significantly suppressed tumor growth in a dose-dependent manner. PPI-2458 administered at 100 mg/kg produced the greatest degree of tumor growth inhibition, which was 57% (P < 0.001) at the end of the study.

Clinical Trial

Molecular Weight

424.53

Formula

C₂₂H₃₆N₂O₆

CAS No.

431077-35-9

SMILES

O=C(O[C@H](CC1)[C@@H](OC)[C@H]([C@@]2(C)O[C@@H]2C/C=C(C)\C)[C@]31CO3)N[C@@H](C(N)=O)C(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Bernier SG, et al. A methionine aminopeptidase-2 inhibitor, PPI-2458, for the treatment of rheumatoid arthritis. Proc Natl Acad Sci U S A. 2004 Jul 20;101(29):10768-73. [Content Brief]

[2]. Cooper AC, et al. A novel methionine aminopeptidase-2 inhibitor, PPI-2458, inhibits non-Hodgkin's lymphoma cell proliferation in vitro and in vivo. Clin Cancer Res. 2006 Apr 15;12(8):2583-90. [Content Brief]

PPI-2458 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PPI-2458431077-35-9PPI2458PPI 2458MetAPMethionine AminopeptidaseHUVECarthritisinflammatoryorally activeNHL tumorSU-DHL-16SR lymphoma cellsInhibitorinhibitorinhibit

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