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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
43 Results for "
GRK2
" in MedChemExpress (MCE) Product Catalog:
Products (43)
43 Results for "GRK2" in MCE Product Catalog:
6
6 Cited Publications
Cat. No.: HY-18990
CAS No.: 817194-38-0
Research Areas:
GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
5
5 Cited Publications
Cat. No.: HY-18991
CAS No.: 1813527-81-9
Research Areas:
CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, GRK5 and GRK1, respectively.
4
4 Cited Publications
Research Areas:
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 .
3
3 Cited Publications
Cat. No.: HY-47573
CAS No.: 2750414-35-6
Research Areas:
CCG273441 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) with an IC50 value of 3.8 nM. CCG273441 is highly selective to GRK5 over GRK2 (IC50=4.8 μM) by binding Cys474, a GRK5 subfamily-specific residue, as a covalent handle .
3
Research Areas:
Locostatin (UIC-1005) is a potent RKIP inhibitor. Locostatin binds Raf kinase inhibitor RKIP protein and disrupts the interaction of RKIP with Raf-1 kinase and G protein-coupled receptor kinase 2. Locostatin inhibits cell proliferation and migration. Locostatin can be used to synthesize chemical probes toward PEBP-proteins. Locostatin aggravates thioacetamide (HY-Y0698)-induced acute liver failure in mice [2] .
1
1 Cited Publications
Research Areas:
GRK2 Inhibitor 2 is an orally active and selective G protein-coupled receptor kinase 2 (GRK) inhibitor with an IC50 of 19 nM. GRK2 Inhibitor 2 also inhibits Aurora-A with an IC50 of 137 nM. GRK2 Inhibitor 2 can be used in the study of congestive heart failure (HF) .
1
Research Areas:
CCG258208 (GRK2-IN-1) hydrochloride is a potent and selective GRK2 (G protein-coupled receptor kinase 2) inhibitor (IC50=30 nM) while maintaining 230-fold selectivity over GRK5 (IC50=7.09 μM) and more than 2500-fold selectivity over GRK1 (IC50=87.3 μM), PKA, and ROCK1. CCG258208 hydrochloride can be used in heart failure research .
1
1 Cited Publications
Target:
Opioid Receptor G Protein-coupled Receptor Kinase (GRK) Mas-related G-protein-coupled Receptor (MRGPR)
Research Areas:
CCG258747 is a selective GRK2 inhibitor (IC50 = 18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, > 5500, and > 550-fold, respectively). CCG258747 also blocks the internalization of the µ-opioid receptor (MOR). CCG258747 attenuates IgE mediated anaphylaxis by inhibiting GRK2 and FcεRI signaling pathway but activates mast cells via MRGPRX2 and MRGPRB2. CCG258747 can be used to study diseases related to overexpression of GRK2 (such as heart failure, opioid tolerance) [2].
1
1 Cited Publications
Cat. No.: HY-P1396A
Research Areas:
Cat. No.: HY-112779
CAS No.: 70323-44-3
Target:
Research Areas:
Pertussis Toxin is a protein-based AB5-type exotoxin produced by the bacterium Bordetella pertussis, which causes whooping cough. Pertussis Toxin inhibits G protein-coupled receptor (GPR) signaling through Gi proteins [2] .
Research Areas:
GRK2 Inhibitor 1 (methyl 5-[2-(5-nitro-2-furyl)vinyl]-2-furoate) is a dual GRK2/β-ARK1 inhibitor that induces dopamine (DA) inhibition reversal (DIR). GRK2 Inhibitor 1 can also block serotonin-induced or neurotensin-induced DIR reversal. Note: DIR refers to the phenomenon in which neurons in addiction-related brain pathways become less sensitive to DA inhibition when exposed to moderate concentrations of DA for a long time .
Cat. No.: HY-P1396
CAS No.: 148505-03-7
Research Areas:
Cat. No.: HY-RS05813
Research Areas:
GRK2 Human Pre-designed siRNA Set A contains three designed siRNAs for GRK2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-177948
CAS No.: 3052947-04-0
Research Areas:
GRK2 degrader-1 (compound 1) is a potent and orally active GRK2 degrader. GRK2 degrader-1 degrades GRK2 via the ubiquitin-proteasome pathway. GRK2 degrader-1 inhibits right ventricular remodeling and elevation of pulmonary artery pressure in a pulmonary artery hypertension (PAH) mouse model. GRK2 degrader-1 can be used for PAH research .
Cat. No.: HY-109562
CAS No.: 2055990-90-2
Synonyms: GRKs-IN-1
Research Areas:
CCG258208 (GRK2-IN-1) is a potent and selective GRK2 (G protein-coupled receptor kinase 2) inhibitor (IC50=30 nM) while maintaining 230-fold selectivity over GRK5 (IC50=7.09 μM) and more than 2500-fold selectivity over GRK1 (IC50=87.3 μM), PKA, and ROCK1. CCG258208 can be used in heart failure research .
Cat. No.: HY-RS23286
Research Areas:
Grk2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Grk2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-RS16845
Research Areas:
Grk2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Grk2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-183057
CAS No.: 2234900-83-3
Research Areas:
GRK2 modulator 1 is an orally active, brain-penetrant and selective GRK2 modulator. GRK2 modulator 1 enhances the active, non-phosphorylated GRK2 and prevents mitochondrial GRK2 and TOMM6 aggregation. GRK2 modulator 1 enhances the non-amyloidogenic processing of APP and prevent PHF-tau, neurodegeneration, and neuronal loss. GRK2 modulator 1 decreases the senescence marker, UPAR, reduces the Alzheimer disease (AD)-related mortality, and prolongs survival. GRK2 modulator 1 exerts neuroprotection by inhibiting HDAC6, and counteracts age-related cardiac dysfunction. GRK2 modulator 1 can be used for research on AD .
Cat. No.: HY-B0492S1
CAS No.: 2714485-95-5
Synonyms: BRL29060-d4 hydrochloride; BRL29060A-d4
Cat. No.: HY-168971
CAS No.: 1390658-79-3
Synonyms: CP-25
Target:
IFNAR STAT TNF Receptor Interleukin Related CXCR JAK G Protein-coupled Receptor Kinase (GRK)
Research Areas:
Paeoniflorin-6′-O-benzene sulfonate (CP-25) is the inhibitor for G protein-coupled receptor kinase 2 (GRK2) that inhibits the translocation of GRK2 to the cell membrane, inhibits JAK1/STAT3 signaling pathway. Paeoniflorin-6′-O-benzene sulfonate inhibits IL-17A/CXCL2-induced proliferation of HaCaT. Paeoniflorin-6′-O-benzene sulfonate reduces the levels of inflammatory factors and chemokines such as IL-17A, IL-17F, IFN-γ, TNF-α, IL-22, IL-23, CXCL2, CXCL3 and CXCL9, alleviates Imiquimod (HY-B0180)-induced psoriasis in mouse model .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
