CRT0066854

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CRT0066854

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Cat No: 28463

Biochemicals - Kinase Inhibitors

CRT0066854 is an inhibitor of PKCι and PKCζ (IC50s = 132 and 639 nM, respectively).{46388} It also inhibits the Rho-associated kinase II (ROCK2) kinase domain (IC50 = 620 nM). It is selective for these atypical PKCs and ROCK2 over typical PKCs and 98 ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

(2S)-3-phenyl-N1-[5,6,7,8-tetrahydro-2-(4-pyridinyl)[1]benzothieno[2,3-d]pyrimidin-4-yl]-1,2-propanediamine

Correlated keywords:

CRT-0066854 PKC-? ? ROCKII LLGL-2 HEK-293 A-549 NRK49F 49-F NRK49

Product Overview:
CRT0066854 is an inhibitor of PKCι and PKCζ (IC50s = 132 and 639 nM, respectively).{46388} It also inhibits the Rho-associated kinase II (ROCK2) kinase domain (IC50 = 620 nM). It is selective for these atypical PKCs and ROCK2 over typical PKCs and 98 other kinases in a panel at 1 µM. CRT0066854 decreases phosphorylation of the atypical PKC substrate lethal giant larvae 2 (LLGL2) in HEK293 cells expressing PKCι and LLGL2. It decreases viability of A549 lung carcinoma cells (IC50 = 3.47 µM) and decreases colony formation in HeLa cells by 65% when used at a concentration of 1 µM. CRT0066854 impairs lumen formation in MDCK cells in a Matrigel™ assay and migration of NRK-49F cells in a wound assay.

Size	1 mg
Shipping	dry ice
CAS Number	1438881-19-6
Molecular Formula	C₂₄H₂₅N₅S
SMILES	N[C@@H](CC1=CC=CC=C1)CNC2=C3C(SC4=C3CCCC4)=NC(C5=CC=NC=C5)=N2
Molecular Weight	415,6
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.39
UNSPSC code	12352100

Technical File

MSDS

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Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

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ISO Guide 34:2009

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