CMPD101
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.49%
- CAS. Nr.: 865608-11-3
- Formel: C24H21F3N6O
- Molecular Weight:466.46
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) CMPD101
More
Customer Validation & Images
-
Bio/Physico-chemical Assay
-
Cell Proliferation/Viability Assay
-
Bio/Physico-chemical Assay
-
Bio/Physico-chemical Assay
-
Cell Proliferation/Viability Assay
Biologische Aktivität
|
GRK2 |
GRK2 18 nM (IC50) |
GRK3 5.4 nM (IC50) |
PKCα 8.1 μM (IC50) |
ROCK2 1.4 μM (IC50) |
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.
-
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.
-
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. Nr. 865608-11-3
-
Appearance Solid
-
Molecular Weight 466.46
-
Formel 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
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
-
Journal Impact Factor
-
Most Recent
-
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
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
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.
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Reinheit & Dokumentation
-
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)
-
Handling Instructions (2659 KB)
Verweise
[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
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.
| 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
HY-103045 Related Classifications
Powered by Bioz