MilliporeSigma
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5.32978

Sigma-Aldrich

PLD2 Inhibitor, ML395

Synonym(s):
PLD2 Inhibitor, ML395, Phosppolipase D2 inhibitor, VU0468809, ML-395
Empirical Formula (Hill Notation):
C26H29N5O2
Molecular Weight:
443.54

Assay

≥97% (HPLC)

Quality Level

form

solid

potency

360 nM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 50 mg/mL

storage temp.

2-8°C

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PLD Inhibitor, FIPI The PLD Inhibitor, FIPI controls the biological activity of PLD. This small molecule/inhibitor is primarily used for Membrane applications.

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PLD Inhibitor, FIPI

PTP LYP Inhibitor The PTP LYP Inhibitor controls the biological activity of PTP LYP. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Sigma-Aldrich

540217

PTP LYP Inhibitor

assay

≥97% (HPLC)

assay

≥99% (HPLC)

assay

≥98% (HPLC)

assay

≥95% (HPLC)

form

solid

form

powder

form

solid

form

solid

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze

color

off-white

color

off-white

color

green-yellow

color

white

solubility

DMSO: 50 mg/mL

solubility

DMSO: 100 mg/mL

solubility

DMSO: 10 mg/mL

solubility

DMSO: 50 mg/mL

General description

A cell permeable, triazaspirone derivative that acts as a highly potent, selective, and direct allosteric inhibitor of phospholipase D2 (PLD2; IC50 = 360 nM in exogenous biochemical assay). Exhibits >80-fold selectivity over phospholipase D1 (PLD1; IC50 = 30 µM). Shown to permeate the blood-brain barrier. Protects A549 cells from multiple strains of influenza virus when cells were pre-treated with this compound. Exhibits excellent DMPK profile (hepatic microsomal clearance = 82.1 ml/min/kg in Sprague-Dawley rats) and conforms to Lipinski′s rule and has favorable lipophilicity. Also displays favorable cytochrome P450 profile (CYP3A4 IC50 = 3.9 µM, CYP2D6 IC50 =16.4 µM, CYP1A2 IC50>30 µM, and CYP2C9 IC50>30 µM).
A cell permeable, triazaspirone derivative that acts as a highly potent, selective, and direct allosteric inhibitor of phospholipase D2 (PLD2; IC50 = 360 nM in exogenous biochemical assay). Exhibits >80-fold selectivity over phospholipase D1 (PLD1; IC50 = 30 µM). Shown to permeate the blood-brain barrier. Protects A549 cells from multiple strains of influenza virus when cells were pre-treated with this compound. Exhibits excellent DMPK profile (hepatic microsomal clearance = 82.1 ml/min/kg in Sprague-Dawley rats) and conforms to Lipinski′s rule and has favorable lipophilicity. Also displays favorable cytochrome P450 profile (CYP3A4 IC50 = 3.9 µM, CYP2D6 IC50 =16.4 µM, CYP1A2 IC50>30 µM, and CYP2C9 IC50>30 µM).

Please note that the molecular weight for this compound is batch-specific due to variable water content.
ML395 is a cell permeable, highly potent, selective, and direct allosteric inhibitor of phospholipase D2 (PLD2; IC₅₀ = 360 nM) that exhibits >80-fold selectivity over PLD1.

Biochem/physiol Actions

Primary Target
PLD2
Reversible: yes

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C).

Other Notes

O′Reilly, M.C., et al. 2014. ChemMedChem9, 2633.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


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