Cat. No.: HY-103045

CMPD101

4 Cited Publications

Customer Review

Based on 4 publication(s) in Google Scholar

CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC₅₀ of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC₅₀s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure.

For research use only. We do not sell to patients.

Purity: 99.49%
CAS No.: 865608-11-3
Formula: C₂₄H₂₁F₃N₆O
Molecular Weight:466.46

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CMPD101 Chemical Structure

CAS No.: 865608-11-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (4)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

GRK2

18 nM (IC₅₀)

GRK3

5.4 nM (IC₅₀)

PKCα

8.1 μM (IC₅₀)

ROCK2

1.4 μM (IC₅₀)

All ROCK Isoforms :

All PKC Isoforms :

In Vitro

CMPD101 (100 μM; pre-20 mins) inhibit the internalization of β2AR, remarkably decreases the isoproterenol-induced formation of clathrin-coated vesicles and the β2AR-GFP fusion protein remained on the plasma membrane in HEK-B2 cell line^[1].
CMPD101 (3-30 μM; pre-30 minutes) produced a robust phosphorylation of Ser375, which is partially inhibited by pretreatment of cells for 30 minutes with 3 μM Cmpd101 and fully blocked by pretreatment with 30 μM Cmpd101. It also inhibits phosphorylation of MOPr at Thr370, Thr376, and Thr379 residues^[2].
CMPD101 (3-30 μM; pre-30 minutes) does not affect the DAMGO-induced increase in ERK1/2 and Elk-1 phosphorylation, at 30 μM, this compound produces a small increase in basal ERK1/2 phosphorylation in HEK 293 cells expressing HA-MOPrs^[2].

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

Western Blot Analysis^[2]

Cell Line:

HEK 293 cells stably expressing HA-tagged rat MOPr
Concentration:

3 μM, 30 μM
Incubation Time:

Pre-30 minutes
Result:

Surpressed Ser375 expression completely at a high dose.

Western Blot Analysis^[2]

Cell Line:

HEK 293 cells stably expressing HA-tagged rat MOPr
Concentration:

3 μM, 30 μM
Incubation Time:

Pre-30 minutes
Result:

Had no effect on DAMGO-induced p-ERK1/2 and p-Elk-1 expression.

Chemical Information

CAS No. 865608-11-3
Appearance Solid
Molecular Weight 466.46
Formula C₂₄H₂₁F₃N₆O
Color White to off-white
SMILES

O=C(C1=CC(NCC2=NN=C(C3=CC=NC=C3)N2C)=CC=C1)NCC4=CC=CC=C4C(F)(F)F
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

Publications (4)

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Journal Impact Factor

J Exp Clin Cancer Res

2,6-DMBQ is a novel mTOR inhibitor that reduces gastric cancer growth in vitro and in vivo. [Abstract]

2020 Jun 9;39(1):107. PMID: 32517736

CMPD101 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2020 Jun 9;39(1):107. [Abstract]

CMPD101 (0.1-30 μM) significantly reduced growth of gastric cancer cells.
Int J Mol Sci

Cellular Electrical Impedance as a Method to Decipher CCR7 Signalling and Biased Agonism. [Abstract]

2022 Aug 10;23(16):8903. PMID: 36012168

CMPD101 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Aug 10;23(16):8903. [Abstract]

CMPD101 (10 µM) significantly increased the maximal CI_[3-20] and AUC_[20-120].
Biomolecules

Ketamine Improves Desensitization of µ-Opioid Receptors Induced by Repeated Treatment with Fentanyl but Not with Morphine. [Abstract]

2022 Mar 10;12(3):426. PMID: 35327617

CMPD101 purchased from MedChemExpress. Usage Cited in: Biomolecules. 2022 Mar 10;12(3):426. [Abstract]

CMPD101 (0.001–10 μM) significantly cancelled the ketamine-induced improvement of the decrease in MOR activity in HEK293 cells evoked by repeated administration of 100 nM fentanyl.

CMPD101 purchased from MedChemExpress. Usage Cited in: Biomolecules. 2022 Mar 10;12(3):426. [Abstract]

CMPD101 (1-10 µM) significantly cancelled the ketamine-induced improvement in the rescue of cAMP in HEK293 cells caused by repeated administration of 100 nM fentanyl.

CMPD101 purchased from MedChemExpress. Usage Cited in: Biomolecules. 2022 Mar 10;12(3):426. [Abstract]

CMPD101 (1–10 µM) significantly cancelled the ketamine-induced enhancement of β-arrestin recruitment to MOR U2OS OPRM1 induced by the repeated administration of 100 nM fentanyl.
ACS Omega

Determination of Site-Specific Phosphorylation Occupancy Using Targeted Mass Spectrometry Reveals the Regulation of Human Apical Bile Acid Transporter, ASBT. [Abstract]

2024 Aug 30;9(37):38477-38489. PMID: 39310206

Solvent & Solubility

In Vitro:

DMSO : 175 mg/mL (375.17 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

2.1438 mL

10.7190 mL

21.4381 mL

5 mM

0.4288 mL

2.1438 mL

4.2876 mL

10 mM

0.2144 mL

1.0719 mL

2.1438 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, 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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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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: ≥ 2.08 mg/mL (4.46 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.46 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.46 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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)
Handling Instructions (2659 KB)

References

[1]. Okawa T, et al. Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure. J Med Chem. 2017 Aug 24;60(16):6942-6990. [Content Brief]

[2]. Yu Q, et al. Inhibition of prostatic smooth muscle contraction by the inhibitor of G protein-coupled receptor kinase 2/3, CMPD101.Eur J Pharmacol. 2018 Jul 15;831:9-19. [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, 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	2.1438 mL	10.7190 mL	21.4381 mL	53.5952 mL
	5 mM	0.4288 mL	2.1438 mL	4.2876 mL	10.7190 mL
	10 mM	0.2144 mL	1.0719 mL	2.1438 mL	5.3595 mL
	15 mM	0.1429 mL	0.7146 mL	1.4292 mL	3.5730 mL
	20 mM	0.1072 mL	0.5360 mL	1.0719 mL	2.6798 mL
	25 mM	0.0858 mL	0.4288 mL	0.8575 mL	2.1438 mL
	30 mM	0.0715 mL	0.3573 mL	0.7146 mL	1.7865 mL
	40 mM	0.0536 mL	0.2680 mL	0.5360 mL	1.3399 mL
	50 mM	0.0429 mL	0.2144 mL	0.4288 mL	1.0719 mL
	60 mM	0.0357 mL	0.1787 mL	0.3573 mL	0.8933 mL
	80 mM	0.0268 mL	0.1340 mL	0.2680 mL	0.6699 mL
	100 mM	0.0214 mL	0.1072 mL	0.2144 mL	0.5360 mL

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CMPD101

Bioactive Compound Library Max

Bioactive Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

GPCR/G Protein Compound Library

Kinase Inhibitor Library

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Anti-Cardiovascular Disease Compound Library

Cytoskeleton Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Extracellular Vesicles (EVs) Compound Library

Multi-Target Compound Library

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) CMPD101

All ROCK Isoforms

All PKC Isoforms

Biological Activity

Chemical Information

Publications (4)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

CMPD101 Related Classifications

HY-103045 Related Classifications