CRT 0066101

• Supplier: Tocris Bioscience
• Catalog: 3555
• Prices: $245.00
• Sizes: 10 mg
• Function Type: Inhibitor
• Cas Number: 1883545-60-5
• Chemical Name: 2-[4-[[(2R)-2-aminobutyl]amino]-2-pyrimidinyl]-4-(1-methyl-1H-pyrazol-4-yl)phenoldihydrochloride
• Formula: C18H22N6O.2HCl
• Molecular Weight: 411.33
• Purity: >98 %
• Description: Potent inhibitor of protein kinase D (PKD); inhibits all PKD isoforms (IC 50 values are 1, 2 and 2.5 nM for PKD1, PKD3 and PKD2 respectively). Exhibits selectivity for PKD against a panel of >90 protein kinases, including PKC α , MEK, ERK, c-Raf and c-Src. Reduces proliferation and cell viability of pancreatic cancer cells expressing moderate levels of endogenous PKD1/2. Orally bioavailable.

Product References

A novel small-molecule inhibitor of protein kinase D blocks pancreatic cancer - A novel small-molecule inhibitor of protein kinase D blocks pancreatic cancer

Harikumar KB, Kunnumakkara AB, Ochi N, Tong Z, Deorukhkar A, Sung B, Kelland L, Jamieson S, Sutherland R, Raynham T, Charles M, Bagherzadeh A, Foxton C, Boakes A, Farooq M, Maru D, Diagaradjane P, Matsuo Y, Sinnett-Smith J, Gelovani J, Krishnan S, Aggarwal BB, Rozengurt E, Ireson CR, Guha S. Mol Cancer Ther. 2010 May;9(5):1136-46.

PKD1 mediates negative feedback of PI3K/Akt activation in response to G - PKD1 mediates negative feedback of PI3K/Akt activation in response to G

Ni Y, Sinnett-Smith J, Young SH, Rozengurt E. PLoS One. 2013 Sep 9;8(9):e73149.