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CMPD101

CAT: 0804-HY-103045-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-103045-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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[1].
CAS Number
865608-11-3
UNSPSC
12352005
Target
G Protein-coupled Receptor Kinase (GRK) ; PKC; ROCK
Type
Reference compound
Related Pathways
Cell Cycle/DNA Damage; Cytoskeleton; Epigenetics; GPCR/G Protein; Stem Cell/Wnt; TGF-beta/Smad
Applications
COVID-19-anti-virus
Field of Research
Cardiovascular Disease
Assay Protocol
https://www.medchemexpress.com/cmpd101.html
Concentration
10mM
Purity
98.95
Solubility
DMSO : 250 mg/mL (ultrasonic)
Smiles
O=C(C1=CC(NCC2=NN=C(C3=CC=NC=C3)N2C)=CC=C1)NCC4=CC=CC=C4C(F)(F)F
Molecular Formula
C24H21F3N6O
Molecular Weight
466.46
References & Citations
[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.|[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
GRK2; PKCα; ROCK2

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