CMPD101

Name: CMPD101
Brand: MedChemExpress
SKU: HY-103045
Rating: 5.0 (4 reviews)

Cat. No.: HY-103045 Purity: 98.96%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

CAS No. : 865608-11-3

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of CMPD101:

CMPD101 hydrochloride Get quote
CMPD101 (Standard) Get quote

4 Publications Citing Use of MCE CMPD101

Cell Proliferation/Viability Assay

Bio/Physico-chemical Assay

: CMPD101 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Aug 10;23(16):8903.; CMPD101 (10 µM) significantly increased the maximal CI_[3-20] and AUC_[20-120].

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

: 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.

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ROCK ROCK1 ROCK2

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

GRK2

18 nM (IC₅₀)

GRK3

5.4 nM (IC₅₀)

PKCα

8.1 μM (IC₅₀)

ROCK2

1.4 μM (IC₅₀)

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.

Molecular Weight

466.46

Formula

C₂₄H₂₁F₃N₆O

CAS No.

865608-11-3

Appearance

Solid

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

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (535.95 mM; Need ultrasonic; 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	2.1438 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

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.96%

Select Batch:

Data Sheet (283 KB) SDS (254 KB)

COA (255 KB) RP-HPLC (259 KB) MS (69 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]

Complete Stock Solution Preparation Table

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

CMPD101 Related Classifications

Cardiovascular Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CMPD101865608-11-3CMPD 101CMPD-101ROCKG Protein-coupled Receptor Kinase (GRK)PKCRho-associated protein kinaseRho-associated kinaseRho-kinaseROKProtein kinase CNeuronheartfailuredesensitizationInhibitorinhibitorinhibit

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CMPD101

Customer Review

Other Forms of CMPD101:

CMPD101 Related Antibodies

4 Publications Citing Use of MCE CMPD101

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All ROCK Isoform Specific Products:

View All PKC Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

CMPD101 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

CMPD101 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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