GRK6 inhibitor 18

  Cat. No.:  DC70442   Featured
Chemical Structure
2677786-61-5
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Field of application
GRK6 inhibitor 18 is a potent, and selective GRK6 inhibitor with IC50 of 8 nM.GRK6 inhibitor 18 displays >1,000-fold selectivity over Aurora A, as well as high selectivity against a panel of 85 kinases.GRK6 inhibitor 18 has potent cellular target engagement and antiproliferative activity against MM cells (IC50=0.4-0.46 uM) and is synergistic with bortezomib.
Cas No.: 2677786-61-5
Chemical Name: GRK6 inhibitor 18
SMILES: COC1=CC=CC2=NC(NCC3=CC=C(Cl)C=C3OC)=NC(NC4=NNC(CC)=C4)=C12
Formula: C22H23ClN6O2
M.Wt: 438.916
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: 1. David E Uehling, et al. J Med Chem. 2021 Aug 12;64(15):11129-11147.
Description: GRK6 inhibitor 18 is a potent, and selective GRK6 inhibitor with IC50 of 8 nM. GRK6 inhibitor 18 displays >1,000-fold selectivity over Aurora A, as well as high selectivity against a panel of 85 kinases. GRK6 inhibitor 18 has potent cellular target engagement and antiproliferative activity against MM cells (IC50=0.4-0.46 uM) and is synergistic with bortezomib.
References: 1. David E Uehling, et al. J Med Chem. 2021 Aug 12;64(15):11129-11147.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC70442 GRK6 inhibitor 18 GRK6 inhibitor 18 is a potent, and selective GRK6 inhibitor with IC50 of 8 nM.GRK6 inhibitor 18 displays >1,000-fold selectivity over Aurora A, as well as high selectivity against a panel of 85 kinases.GRK6 inhibitor 18 has potent cellular target engagement and antiproliferative activity against MM cells (IC50=0.4-0.46 uM) and is synergistic with bortezomib.
DC11955 Takeda compound 101 Compound 101 (GRK2 inhibitor 101, Takeda compound 101, Cmpd101) is a novel membrane-permeable, small-molecule inhibitor of GRK2 and GRK3.
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