Cat. No.: HY-101354

R-IMPP

Name: R-IMPP
Brand: MedChemExpress
SKU: HY-101354
Price: 52.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: PF-00932239)

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R-IMPP (PF-00932239) is a PCSK9 translation inhibitor and a selective 80S ribosome binder. R-IMPP inhibits the KRAS/MEK/ERK signaling cascade. R-IMPP reduces LPS-induced nuclear translocation of NFkB P65. R-IMPP increases LDL-R levels in cells, promotes LDL-C uptake, and does not alter the secretion of transferrin or albumin. R-IMPP inhibits the growth of colorectal cancer (CRC) cells, organoids and xenografts carrying APC/KRAS mutations, as well as the number and burden of spontaneous mouse tumors. R-IMPP can be used in research related to colorectal cancer with APC/KRAS mutations, hepatic ischemia-reperfusion injury and hypercholesterolemia.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Pureté: 99.93%
CAS No.: 2133832-83-2
Formule: C₂₄H₂₇N₃O₂
Masse moléculaire:389.49

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

R-IMPP Chemical Structure

CAS No.: 2133832-83-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Voir tous les produits spécifiques à Isoform Ras :

Voir tous les produits spécifiques à Isoform MEK :

Voir tous les produits spécifiques à Isoform ERK :

Voir tous les produits spécifiques à Isoform NF-κB :

Cellular Effect

Cell Line	Type	Value	Description	References
Bone marrow cell	IC₅₀	>20 μM Compound: 1; PF-00932239	Cytotoxicity against rat bone marrow cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay Cytotoxicity against rat bone marrow cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 29878763]
CHO-K1	IC₅₀	<10 μM Compound: 1; R-IMPP, PF-00932239	Inhibition of human recombinant full length ProLabel-tagged PCSK9 expressed in CHO-K1 cells incubated overnight and measured after 3 days by chemiluminescence assay Inhibition of human recombinant full length ProLabel-tagged PCSK9 expressed in CHO-K1 cells incubated overnight and measured after 3 days by chemiluminescence assay	[PMID: 30448414]
CHO-K1	IC₅₀	>10 μM Compound: 1; R-IMPP, PF-00932239	Cytotoxicity against CHOK1 cells expressing human recombinant full length ProLabel-tagged PCSK9 after overnight incubation by CellTiter blue assay Cytotoxicity against CHOK1 cells expressing human recombinant full length ProLabel-tagged PCSK9 after overnight incubation by CellTiter blue assay	[PMID: 30448414]
CHO-K1	IC₅₀	>10 μM Compound: 1; R-IMPP, PF-00932239	Inhibition of human recombinant PCSK9 expressed in CHO-K1 cells assessed as alkaline phosphatase secretion incubated overnight and measured after 3 days by HTS assay Inhibition of human recombinant PCSK9 expressed in CHO-K1 cells assessed as alkaline phosphatase secretion incubated overnight and measured after 3 days by HTS assay	[PMID: 30448414]
CHO-K1	IC₅₀	4.8 μM Compound: 1; R-IMPP, PF-00932239	Inhibition of human recombinant full length ProLabel-tagged PCSK9 expressed in CHO-K1 cells incubated overnight and measured after 3 days by HTS assay Inhibition of human recombinant full length ProLabel-tagged PCSK9 expressed in CHO-K1 cells incubated overnight and measured after 3 days by HTS assay	[PMID: 30448414]
CHO-K1	IC₅₀	4.8 μM Compound: Fig 8, Cpd 80S	Inhibition of 80s ribosome in CHOK1 cells assessed as reduction in PL-tagged PCSK9 expression incubated for over night by EFC kit method Inhibition of 80s ribosome in CHOK1 cells assessed as reduction in PL-tagged PCSK9 expression incubated for over night by EFC kit method	[PMID: 31673315]
HeLa	IC₅₀	8.04 μM Compound: 1; PF-00932239	Binding affinity to 80S ribosome in human HeLa cells lysates using human full length PCSK9 encoding mRNAs assessed as inhibition of PCSK9 mRNA translation after 45 mins by Steady-Glo luciferase reporter gene assay Binding affinity to 80S ribosome in human HeLa cells lysates using human full length PCSK9 encoding mRNAs assessed as inhibition of PCSK9 mRNA translation after 45 mins by Steady-Glo luciferase reporter gene assay	[PMID: 30482620]
Huh-7	IC₅₀	2.2 μM Compound: 13; R-IMPP	Inhibition of PCSK9 expression in human HuH7 cells after overnight incubation by ELISA Inhibition of PCSK9 expression in human HuH7 cells after overnight incubation by ELISA	[PMID: 29519739]
Huh-7	IC₅₀	2.63 μM Compound: 1; PF-00932239	Binding affinity to 80S ribosome in human HuH7 cells harboring pCMV-truncated human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay Binding affinity to 80S ribosome in human HuH7 cells harboring pCMV-truncated human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay	[PMID: 29878763]
Huh-7	IC₅₀	2.63 μM Compound: 1; PF-00932239	Binding affinity to 80S ribosome in human HuH7 cells harboring human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay Binding affinity to 80S ribosome in human HuH7 cells harboring human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay	[PMID: 30482620]
Huh-7	IC₅₀	8.37 μM Compound: 1; PF-00932239	Binding affinity to 80S ribosome in human HuH7 cells assessed as inhibition of PCSK9 mRNA translation after overnight incubation by ELISA Binding affinity to 80S ribosome in human HuH7 cells assessed as inhibition of PCSK9 mRNA translation after overnight incubation by ELISA	[PMID: 29878763]

In Vitro

R-IMPP (30-60 μM) inhibits the KRAS/MEK/ERK pathway by reducing the protein levels of p-ERK and cyclin D3 in three APC/KRAS-mutant colorectal cancer cell lines, HCT116, LOVO and SW1116^[1].
R-IMPP (40 μM) inhibits the expression of active KRAS protein in SW1116 APC/KRAS mutant colorectal cancer cells^[1].
R-IMPP (72 h) inhibits cell viability, with stronger inhibitory potency against APC/KRAS mutant colorectal cancer cell lines (72-hour IC₅₀: 17.6-41.8 μM). In comparison, the 72-hour IC₅₀ is 84.8 μM for wild-type 1CT cells and 57.5 μM for normal NCM460 colon cells^[1].
R-IMPP (30-60 μM; 24 h) potently inhibits the expression of PCSK9 protein in AML12 hepatocytes^[2].
R-IMPP (60 μM; 24 h) impairs the mitochondrial membrane potential of AML12 hepatocytes, while no such effect is observed at the concentration of 30 μM^[2].
R-IMPP attenuates hypoxia/reoxygenation-induced apoptosis of AML12 hepatocytes^[2].
R-IMPP potently inhibits PCSK9 secretion in CHO-K1 cells expressing recombinant ProLabel-tagged PCSK9, with an IC₅₀ of 4.8 μM. Meanwhile, it exhibits only extremely low cytotoxicity and no non-universal secretion inhibitory effect^[3].
R-IMPP (3-30 μM; overnight pre-treatment) promotes the uptake of AF-LDL by Huh7 cells, with a 47.5% increase in uptake at the concentration of 30 μM^[3].

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

Cell Viability Assay^[1]

Cell Line:

NCM460 (normal colonic epithelial cells), 1CT (wildtype colonic cells), 1CT-AK, DLD1, HCT116, LOVO, SW1116 (APC/KRAS-mutant CRC cell lines)
Concentration:

Various concentrations
Incubation Time:

72 h
Result:

Exhibited 72-hour IC₅₀ values of 57.5 μM for NCM460, 84.8 μM for 1CT, 41.8 μM for 1CT-AK, 22.5 μM for DLD1, 17.6 μM for HCT116, 26.4 μM for LOVO, and 26.9 μM for SW1116.
Rendered APC/KRAS-mutant CRC cells more sensitive than wildtype or normal colonic cells.

Western Blot Analysis^[3]

Cell Line:

human hepatoma Huh7 cells
Concentration:

10 μM, 30 μM
Incubation Time:

overnight
Result:

Caused a dose-dependent increase in LDL-R levels at 10 μM and 30 μM.
Caused a dose-dependent decrease in both pro-PCSK9 and mature PCSK9 levels in cell lysates at 10 μM and 30 μM.

In Vivo

R-IMPP (100 mg/kg; i.p.) suppresses the growth of SW1116 APC/KRAS-mutant CRC xenografts in NOD/SCID mice^[1].
R-IMPP (50 mg/kg; i.p.; 3 times/week) suppresses tumor development in the spontaneous APC/KRAS-mutant CRC mouse model^[1].
R-IMPP (50 mg/kg; i.p.) synergizes with Simvastatin (HY-17502) to induce regression of SW1116 APC/KRAS-mutant CRC xenografts in nude mice^[1].

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

Animal Model:

NOD/SCID^[1]
Dosage:

100 mg/kg
Administration:

i.p.
Result:

Suppressed growth of SW1116 xenografts, with decreased tumor volume and weight.
Caused no significant decrease in body weight.

Animal Model:

Apc^{Min/+}Kras^{G12D/+}Villin-Cre^[1]
Dosage:

50 mg/kg
Administration:

i.p.; 3 times/week
Result:

Significantly suppressed tumor number and tumor load.

Animal Model:

Nude^[1]
Dosage:

50 mg/kg
Administration:

i.p.
Result:

Triggered tumor regression compared to control or single agent treatments, and reduced tumor weight.
Down-regulated PCSK9 protein and GGPP levels in xenograft tumors.

Chemical Information

CAS No. 2133832-83-2
Appearance Solid
Masse moléculaire 389.49
Formule C₂₄H₂₇N₃O₂
Color Light yellow to yellow
SMILES

O=C(N(C1=NC=CC2=C1C=CC=C2)[C@H]3CNCCC3)CCC4=CC=C(OC)C=C4
Synonyms

PF-00932239
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (256.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5675 mL

12.8373 mL

25.6746 mL

5 mM

0.5135 mL

2.5675 mL

5.1349 mL

10 mM

0.2567 mL

1.2837 mL

2.5675 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (6.42 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Wong CC, et al. The cholesterol uptake regulator PCSK9 promotes and is a therapeutic target in APC/KRAS-mutant colorectal cancer. Nature communications. 2022 Jul 08;13(1):3971.

[2]. Zhang Y, et al. Blockade of Hepatocyte PCSK9 Ameliorates Hepatic Ischemia-Reperfusion Injury by Promoting Pink1-Parkin-Mediated Mitophagy. Cellular and molecular gastroenterology and hepatology. 2024;17(1):149-169. [Content Brief]

[3]. Petersen DN, et al. A Small-Molecule Anti-secretagogue of PCSK9 Targets the 80S Ribosome to Inhibit PCSK9 Protein Translation. Cell Chem Biol. 2016 Nov 17;23(11):1362-1371. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5675 mL	12.8373 mL	25.6746 mL	64.1865 mL
	5 mM	0.5135 mL	2.5675 mL	5.1349 mL	12.8373 mL
	10 mM	0.2567 mL	1.2837 mL	2.5675 mL	6.4187 mL
	15 mM	0.1712 mL	0.8558 mL	1.7116 mL	4.2791 mL
	20 mM	0.1284 mL	0.6419 mL	1.2837 mL	3.2093 mL
	25 mM	0.1027 mL	0.5135 mL	1.0270 mL	2.5675 mL
	30 mM	0.0856 mL	0.4279 mL	0.8558 mL	2.1396 mL
	40 mM	0.0642 mL	0.3209 mL	0.6419 mL	1.6047 mL
	50 mM	0.0513 mL	0.2567 mL	0.5135 mL	1.2837 mL
	60 mM	0.0428 mL	0.2140 mL	0.4279 mL	1.0698 mL
	80 mM	0.0321 mL	0.1605 mL	0.3209 mL	0.8023 mL
	100 mM	0.0257 mL	0.1284 mL	0.2567 mL	0.6419 mL

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CAS No.:
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R-IMPP

PF-06446846 hydrochloride

SBC-110736

SBC-115076

Cetraxate hydrochloride

WNK463

Laroprovstat

Pep2-8

SBC-110736 (Standard)

PF-06446846

Benzamidine hydrochloride

Upamostat

PCSK9-IN-10

Voir tous les produits spécifiques à Isoform Ras

Voir tous les produits spécifiques à Isoform MEK

Voir tous les produits spécifiques à Isoform ERK

Voir tous les produits spécifiques à Isoform NF-κB

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

R-IMPP

PF-06446846 hydrochloride

SBC-110736

SBC-115076

Cetraxate hydrochloride

WNK463

Laroprovstat

Pep2-8

SBC-110736 (Standard)

PF-06446846

Benzamidine hydrochloride

Upamostat

PCSK9-IN-10

Voir tous les produits spécifiques à Isoform Ras

Voir tous les produits spécifiques à Isoform MEK

Voir tous les produits spécifiques à Isoform ERK

Voir tous les produits spécifiques à Isoform NF-κB

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

R-IMPP Related Classifications

HY-101354 Related Classifications

Bioz