Chemical Structure : CRT0066854
CAS No.:
1438881-19-6
CRT0066854
(CRT 0066854)
Catalog No.: PC-20701Not For Human Use, Lab Use Only.
CRT0066854 is a potent and selective chemical inhibitor of atypical PKC (protein kinase C) isoforms PKCζ and PKCι with IC50 of 639 nM and 132 nM, respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
CRT0066854 is a potent and selective chemical inhibitor of atypical PKC (protein kinase C) isoforms PKCζ and PKCι with IC50 of 639 nM and 132 nM, respectively.
CRT0066854 shows little to no acitvity agianst nPKCϵ (IC50=7.21 uM).
CRT0066854 is approximately 20-fold more potent for PKCζk and over 60-fold more potent for PKCιk than BIM-1.
CRT0066854 is a potent and selective chemical tool to modulate aPKC activity both in vitro and in cells, with no effect on PKCα or PKCϵ.
CRT0066854 inhibits the LLGL2 (lethal giant larvae 2) phosphorylation in HEK-293 cells (IC50=0.87 uM) and exhibits IC50 of 3.47 uM for A549 lung carcinoma cell viability.
CRT0066854 (3-12 uM) impedes directed migration of NRK cells.
Physicochemical Properties
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M.Wt
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415.56
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Formula
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C24H25N5S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(S)-3-phenyl-N1-(2-(pyridin-4-yl)-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-yl)propane-1,2-diamine
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References
1. Kjær S, et al. Biochem J. 2013 Apr 15;451(2):329-42.
2. Linch M, et al. Carcinogenesis. 2014 Feb;35(2):396-406.
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