CS640 shows potent activity on CAMK1D IC50 of 8 nM (ADP-Glow assay) and 11 nM (pCAMK1D phosphorylation assay).
CS640 shows excellent selectivity in a Eurofins DiscoverX screen (468 Kinases). Only minor activity outside the CAMK1 subfamily found. Other possible off-targets from Discover X screen were not confirmed in nanoBRET or WesternBlot assays.
Potency Against Target Family
Kinase
|
Percent of control(%)
|
RB IC50 (nM)
|
NanoBRET IC50 (nM)
|
CAMK1D
|
0.9
|
8
|
29
|
CAMK1B
|
0
|
3
|
8.2
|
CAMK1A
|
0
|
1
|
23
|
CAMK1G
|
0
|
1
|
55
|
Selectivity
CS640 shows potent activity on CAMK1D IC50 of 8 nM (ADP-Glow assay) and 11 nM (pCAMK1D phosphorylation assay).
CS640 shows excellent selectivity in a Eurofins DiscoverX screen (468 Kinases). Only minor activity outside the CAMK1 subfamily found. Other possible off-targets from DX screen were not confirmed in orthogonal assay such as nanoBRET or Western Blot.
The negative control CS640s was tested in an in house kinase DSF Panel, showing no Tm shift on any kinase.

Dosage
To minimize the chance of off-target effects, we recommend a concentration of no higher than 1 µM for cell-based assays. Some toxicity was found at conc. of 10 µM at some cell lines. For in vivo studies the probe was tested up to 40 mg/kg in in Diet-Induced Obesity in vivo mouse models.
Cellular based Activity
In NanoBRET assay using HEK293T cells CS640 binds all Kinase from the CAMK1 subfamily:
CAMK1A IC50 = 23 nM, CAMK1B IC50 = 8.2 nM, CAMK1D IC50 = 29 nM, CAMK1G IC50 = 55 nM