R-IMPP

Catalog No.S8420 Batch:S842001

Technical Data

Formula	C₂₄H₂₇N₃O₂
Molecular Weight	389.49	CAS No.	2133832-83-2
Solubility (25°C)*	In vitro	DMSO	77 mg/mL (197.69 mM)
		Ethanol	77 mg/mL (197.69 mM)
		Water	7 mg/mL (17.97 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

R-IMPP is an inhibitor of PCSK9 secretion, half maximal inhibitory concentration [IC50] = 4.8 μM.

Targets

PCSK9 ^[1]

In vitro

R-IMPP promotes uptake of LDL-C in hepatoma cells by increasing LDL-R levels, without altering levels of secreted transferrin. R-IMPP does not decrease PCSK9 transcription or increase PCSK9 degradation, but instead causes transcript-dependent inhibition of PCSK9 translation. R-IMPP is discovered that exhibited weak PCSK9 anti-secretagogue activity (half maximal inhibitory concentration [IC50] = 4.8 μM), but does not affect intracellular ATP levels in the recombinant CHO-K1 cells, a measure of cytotoxicity, nor decrease secretion of a control protein, secreted alkaline phosphatase, a measure of relative selectivity. The inhibitory response of R-IMPP is stereospecific^[1].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Huh7 cells Concentrations 10, 30 μM Incubation Time 24 h Method Huh7 cells are plated at 150,000 cells per well and transfected with the full-length and truncation mutants. After 24 hr, cells are treated with vehicle, 30 μMR-IMPP, or 30 μM S-IMPP. At 48 hr post-transfection, cells are washed three times with TBS +2 mg/mL BSA and lysed with 100 mL of RIPA buffer per well. Protein lysates are subjected to SDS-PAGE and western blot analysis for PCSK9 (V5) and b-actin.

Cell Assay:^{^[1]}

Cell lines
Huh7 cells
Concentrations
10, 30 μM
Incubation Time
24 h
Method
Huh7 cells are plated at 150,000 cells per well and transfected with the full-length and truncation mutants. After 24 hr, cells are treated with vehicle, 30 μMR-IMPP, or 30 μM S-IMPP. At 48 hr post-transfection, cells are washed three times with TBS +2 mg/mL BSA and lysed with 100 mL of RIPA buffer per well. Protein lysates are subjected to SDS-PAGE and western blot analysis for PCSK9 (V5) and b-actin.

References

[1] Petersen DN, et al. Cell Chem Biol. 2016, 23(11):1362-1371.

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SHIPPING AND STORAGE
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