CRT0066101 dihydrochloride

Research use only, not for human use.

A potent, specific, orally active pan-PKD (protein kinase D) inhibitor.

A potent, specific, orally active pan-PKD (protein kinase D) inhibitor with biochemical IC50 of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively; shows selectivity against a panel of > 90 protein kinases including PKCα/PKBα/MEK/ERK/c-Raf/c-Src/c-Abl; reduces bromodeoxyuridine incorporation, increases apoptosis, blocks neurotensin-induced PKD1/2 activation and reduces neurotensin-induced, PKD-mediated Hsp27 phosphorylation, attenuated PKD1-mediated NF-kappaB activation in pancreatic cancer cells; potently blocks tumor growth in vivo.

——

——

CRT-0066101 | CRT 0066101

Apoptosis

PKD

PKD

——

——

1883545-60-5

411.33

C18H22N6O.2HCl

>98% (HPLC)

DMSO : ≥ 25 mg/mL 66.69 mM

OC1=CC=C(C2=CN(C)N=C2)C=C1C3=NC=CC(NC[C@H](N)CC)=N3.[H]Cl.[H]Cl

2-[4-[[(2R)-2-aminobutyl]amino]-2-pyrimidinyl]-4-(1-methyl-1H-pyrazol-4-yl)phenol dihydrochloride

(-20℃)

With Ice Pack

≥ 2 years