2. Metabolic Enzyme/Protease
  3. MetAP
  4. PPI-2458

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

PPI-2458 Chemical Structure

CAS No. : 431077-35-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

PPI-2458 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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.

PPI-2458 Related Antibodies

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.
Appearance

Solid

Color

White to off-white

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (235.55 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3555 mL 11.7777 mL 23.5555 mL
5 mM 0.4711 mL 2.3555 mL 4.7111 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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
DMSO 1 mM 2.3555 mL 11.7777 mL 23.5555 mL 58.8887 mL
5 mM 0.4711 mL 2.3555 mL 4.7111 mL 11.7777 mL
10 mM 0.2356 mL 1.1778 mL 2.3555 mL 5.8889 mL
15 mM 0.1570 mL 0.7852 mL 1.5704 mL 3.9259 mL
20 mM 0.1178 mL 0.5889 mL 1.1778 mL 2.9444 mL
25 mM 0.0942 mL 0.4711 mL 0.9422 mL 2.3555 mL
30 mM 0.0785 mL 0.3926 mL 0.7852 mL 1.9630 mL
40 mM 0.0589 mL 0.2944 mL 0.5889 mL 1.4722 mL
50 mM 0.0471 mL 0.2356 mL 0.4711 mL 1.1778 mL
60 mM 0.0393 mL 0.1963 mL 0.3926 mL 0.9815 mL
80 mM 0.0294 mL 0.1472 mL 0.2944 mL 0.7361 mL
100 mM 0.0236 mL 0.1178 mL 0.2356 mL 0.5889 mL
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PPI-2458 Related Classifications

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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