1. Anti-infection
  2. Fungal
  3. NPPM 6748-481

NPPM 6748-481 is a potent and selective yeast Sec14 inhibitor with a yeast Sec14 IC50 of 211 nM. NPPM 6748-481 disrupts membrane trafficking, impairing trans-Golgi network-endosomal transport and endocytic transport. NPPM 6748-481 impairs Snc1 v-SNARE recycling, secretory invertase trafficking, and vacuolar carboxypeptidase Y processing. NPPM 6748-481 can be used for research on yeast infection.

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NPPM 6748-481

NPPM 6748-481 Chemical Structure

CAS No. : 432020-20-7

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10 mM * 1 mL in DMSO
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Description

NPPM 6748-481 is a potent and selective yeast Sec14 inhibitor with a yeast Sec14 IC50 of 211 nM. NPPM 6748-481 disrupts membrane trafficking, impairing trans-Golgi network-endosomal transport and endocytic transport. NPPM 6748-481 impairs Snc1 v-SNARE recycling, secretory invertase trafficking, and vacuolar carboxypeptidase Y processing. NPPM 6748-481 can be used for research on yeast infection[1].

In Vitro

NPPM 6748-481 (30 min) potently and selectively inhibits purified yeast Sec14-catalyzed [3H]PtdIns transfer in vitro with an IC50 of 211 nM, and does not inhibit related yeast Sfh1-Sfh5 PITPs at concentrations up to 40 μM[1].
NPPM 6748-481 (10-16 h) inhibits growth of WT haploid Saccharomyces cerevisiae with an IC50 of 2.87 μM, and sensitivity to the compound directly correlates with cellular Sec14 levels[1].
NPPM 6748-481 (30 min) has drastically reduced inhibitory sensitivity against purified yeast Sec14 with mutations in specific residues (Y111, Y151, S201, S173) in vitro, with Sec14S173C showing >736-fold resistance[1].
NPPM 6748-481 (20-40 μM; 48 h) does not inhibit growth of Saccharomyces cerevisiae expressing NPPM-resistant Sec14S173C, and "bypass Sec14" cki1Δ and kes1Δ mutants are also resistant to the compound, confirming Sec14 as the sole essential cellular target[1].
NPPM 6748-481 (20 μM; 3 h) selectively disrupts TGN-endosomal PtdIns-4-P pools in WT Saccharomyces cerevisiae without affecting plasma membrane PtdIns-4-P pools, phenocopying genetic Sec14 inactivation[1].
NPPM 6748-481 (20 μM) does not interfere with Sfh4-dependent PtdSer decarboxylation to PtdEtn in Saccharomyces cerevisiae psd1Δ mutants, demonstrating selective inhibition of Sec14-dependent versus Sfh4-dependent PtdIns-4-P signaling in TGN-endosomes[1].

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

Molecular Weight

363.77

Formula

C17H15ClFN3O3

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=CC=C(Cl)C([N+]([O-])=O)=C1)N2CCN(C3=CC=CC=C3F)CC2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (274.90 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7490 mL 13.7449 mL 27.4899 mL
5 mM 0.5498 mL 2.7490 mL 5.4980 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Purity: 99.60%

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 (stored under nitrogen). 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 2.7490 mL 13.7449 mL 27.4899 mL 68.7247 mL
5 mM 0.5498 mL 2.7490 mL 5.4980 mL 13.7449 mL
10 mM 0.2749 mL 1.3745 mL 2.7490 mL 6.8725 mL
15 mM 0.1833 mL 0.9163 mL 1.8327 mL 4.5816 mL
20 mM 0.1374 mL 0.6872 mL 1.3745 mL 3.4362 mL
25 mM 0.1100 mL 0.5498 mL 1.0996 mL 2.7490 mL
30 mM 0.0916 mL 0.4582 mL 0.9163 mL 2.2908 mL
40 mM 0.0687 mL 0.3436 mL 0.6872 mL 1.7181 mL
50 mM 0.0550 mL 0.2749 mL 0.5498 mL 1.3745 mL
60 mM 0.0458 mL 0.2291 mL 0.4582 mL 1.1454 mL
80 mM 0.0344 mL 0.1718 mL 0.3436 mL 0.8591 mL
100 mM 0.0275 mL 0.1374 mL 0.2749 mL 0.6872 mL
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Product Name:
NPPM 6748-481
Cat. No.:
HY-15784
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