PF-4800567 is a selective, ATP competitive casein kinase 1ε inhibitor with IC50 values of 32 and 711 nM for CK1ε and CK1δ respectively. Casein kinase 1 epsilon (CK1epsilon) and casein kinase 1 delta (CK1delta) are closely related Ser-Thr protein kinases that serve as key clock regulators as demonstrated by mammalian mutations in each that dramatically alter the circadian period. PF-4800567 displays 22-fold greater potency towards CK1ε than CK1δ. PF-4800567 completely blocks CK1epsilon-mediated PER3 nuclear localization and PER2 degradation.
 |
Source | Oncogene (2011). Figure 5. PF-4800567 |
| Method | cell proliferation assay | |
| Cell Lines | HEK293 and HT1080 cell | |
| Concentrations | 1 μM | |
| Incubation Time | 24 h | |
| Results | We confirmed that PF480 selectively inhibited CK1ɛ using the in vivo autophosphorylation assay. PF480 was less effective than PF670 at inhibition of Wnt/β-catenin signaling |
| Cell Experiment | |
|---|---|
| Cell lines | COS-7 cells |
| Preparation method | Nuclear Translocation. CK1ϵ- and CK1δ-dependent PER3 nuclear translocation was run as described previously for CK1ϵ (Badura et al., 2007), with alterations as indicated below. CK1δ-dependent PER3 nuclear translocation was performed with human full-length CKIδ-pcDNA4/HisA cotransfected into COS-7 cells with the GFP-tagged murine PER3. The sensitivity of the assay was increased by incorporating an anti-GFP antibody-staining step. After the plates were fixed with 4% paraformaldehyde and washed in PBS, cells were blocked and permeabilized in PBS with 4% goat serum and 0.1% Triton X-100 for 1 h at room temperature. Blocking buffer was then replaced with a polyclonal anti-GFP antibody (Invitrogen), diluted 1:1000 in blocking buffer, and incubated for 2 h. After three washes in PBS, goat anti-rabbit Alexa Fluor 488 secondary antibody (Invitrogen), diluted 1:1000 in Hoechst staining solution, was added and incubated for 1 h before three final washes in PBS. |
| Concentrations | 0, 0.01, 0.1, 1, 10μM |
| Incubation time | 1~2 hr |
| Animal Experiment | |
|---|---|
| Animal models | C57BL/6J mice |
| Formulation | 20% hydroxypropyl β-cyclodextrin |
| Dosages | 100 mg/kg daily for 3 days |
| Administration | s.c. |
| Molecular Weight | 359.81 |
| Formula | C17H18ClN5O2 |
| CAS Number | 1188296-52-7 |
| Solubility (25°C) | DMSO ≥30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Casein Kinase Products |
|---|
| ON 108600
ON 108600 is an inhibitor of CK2 (Casein Kinase2)/TNIK/DYRK1 with IC50 values of 0.016 μm/0.007 μM, 0.028 μM, 0.05 μM/0.005 μM, and 0.005 μM for DYRK1A/DYRKB, DYRK2, CK2α1/CK2α2, and TNIK, respectively. 0.005 μM. It has anti-tumor activity. |
| (R)-DRF053 dihydrochloride
(R)-DRF053 dihydrochloride is a potent inhibitor of casein kinase 1 (CK1), CDK1/cyclin B, and CDK5/p25, with IC50s of 14 nM, 220 nM, and 80 nM, respectively.(R)-DRF053 dihydrochloride prevented the production of CK1-dependent amyloid-β in cellular models. In addition, (R)-DRF053 dihydrochloride prevented the production of CK1-dependent amyloid-β in cell models. |
| Casein kinase 1δ-IN-5
Casein kinase 1δ-IN-5 is a potent and selective protein kinase CK-1δ inhibitor with an IC50 of 47 nM, which has neuroprotective and anti-inflammatory properties in vitro. It has neuroprotective and anti-inflammatory properties in vitro. It can be used in studies related to neurodegenerative diseases. |
| CK2-IN-1
CK2-IN-1 is a CK2 inhibitor with an IC50 value of 150 nM. |
| SR-1277
SR-1277 is a potent, selective and ATP-competitive CK1δ/ε inhibitor with IC50 values of 49 nM and 260 nM, respectively.In addition, SR-1277 inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3, and CDK9/cyclin K with IC50 values of 305 nM, 1340 nM, 311 nM, and 109 nM, respectively. 1340 nM, 311 nM and 109 nM, respectively, and can be used in cancer research. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
