A PKCι and PKCζ inhibitor
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CRT0066854

Item No. 28463

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2S)-3-phenyl-N1-[5,6,7,8-tetrahydro-2-(4-pyridinyl)[1]benzothieno[2,3-d]pyrimidin-4-yl]-1,2-propanediamine
CAS Number
1438881-19-6
Molecular Formula
C24H25N5S
Formula Weight
415.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 30 mg/ml
λmax
227, 254, 288, 350 nm
SMILES
N[C@@H](CC1=CC=CC=C1)CNC2=C3C(SC4=C3CCCC4)=NC(C5=CC=NC=C5)=N2
InChi Code
InChI=1S/C24H25N5S/c25-18(14-16-6-2-1-3-7-16)15-27-23-21-19-8-4-5-9-20(19)30-24(21)29-22(28-23)17-10-12-26-13-11-17/h1-3,6-7,10-13,18H,4-5,8-9,14-15,25H2,(H,27,28,29)/t18-/m0/s1
InChi Key
NRHASZRDWOUMFD-SFHVURJKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    CRT0066854 is an inhibitor of PKCι and PKCζ (IC50s = 132 and 639 nM, respectively).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kjær, S., Linch, M., Purkiss, A., et al. Adenosine-binding motif mimicry and cellular effects of a thieno[2,3-d]pyrimidine-based chemical inhibitor of atypical protein kinase C isoenzymes. Biochem. J. 451(2), 329-342 (2013).