Table 1

RA306 selectivity profile

Eurofins panel (304 kinases)
P33 assays
IC50 (nM)IC50 ratioaATP (µM)
 CaMKIIγ (h)<3∼110
 CaMKIIδ (h)<3110
 CaMKIδ (h)12>415
 CaMKIIβ (h)17>615
 ACK1 (h)26>970
 MLK1 (h)89>3045
 SIK (h)149>5045
 PTK5 (h)216>72155
 Pyk2 (h)249>8390
 IRE1 (h)254>8515
 ULK2 (h)255>8515
 CaMKK2 (h)294>9890
 Others>300>100Km
CEREP panel (107 targets)
Binding, enzyme, and uptake assays 
I%–10 µMI%–1 µMIC50 (nM)
 CaMK2α (h)101NANA
 Sigma (1/2) (h)9673NA
 15-Lipoxygenase-2 (h)9673270
 M3 (h)90NANA
 IRK (h)74NANA
 Others<50NANA
Ion channels
Manual patch-clamp
RA306 IC50 (µM)KN93 IC50 (µM)IC50 ratiob
 ERG (h)>300.08>375
 Kv4.3 (h)>304>7.5
 Nav1.5 (h)>302.7>11
 Cav1.2 (h)140.915
Eurofins panel (304 kinases)
P33 assays
IC50 (nM)IC50 ratioaATP (µM)
 CaMKIIγ (h)<3∼110
 CaMKIIδ (h)<3110
 CaMKIδ (h)12>415
 CaMKIIβ (h)17>615
 ACK1 (h)26>970
 MLK1 (h)89>3045
 SIK (h)149>5045
 PTK5 (h)216>72155
 Pyk2 (h)249>8390
 IRE1 (h)254>8515
 ULK2 (h)255>8515
 CaMKK2 (h)294>9890
 Others>300>100Km
CEREP panel (107 targets)
Binding, enzyme, and uptake assays 
I%–10 µMI%–1 µMIC50 (nM)
 CaMK2α (h)101NANA
 Sigma (1/2) (h)9673NA
 15-Lipoxygenase-2 (h)9673270
 M3 (h)90NANA
 IRK (h)74NANA
 Others<50NANA
Ion channels
Manual patch-clamp
RA306 IC50 (µM)KN93 IC50 (µM)IC50 ratiob
 ERG (h)>300.08>375
 Kv4.3 (h)>304>7.5
 Nav1.5 (h)>302.7>11
 Cav1.2 (h)140.915

NA, not available.

a

Kinase IC50/CaMKIIδ IC50.

b

RA306 IC50/KN93 IC50.

Table 1

RA306 selectivity profile

Eurofins panel (304 kinases)
P33 assays
IC50 (nM)IC50 ratioaATP (µM)
 CaMKIIγ (h)<3∼110
 CaMKIIδ (h)<3110
 CaMKIδ (h)12>415
 CaMKIIβ (h)17>615
 ACK1 (h)26>970
 MLK1 (h)89>3045
 SIK (h)149>5045
 PTK5 (h)216>72155
 Pyk2 (h)249>8390
 IRE1 (h)254>8515
 ULK2 (h)255>8515
 CaMKK2 (h)294>9890
 Others>300>100Km
CEREP panel (107 targets)
Binding, enzyme, and uptake assays 
I%–10 µMI%–1 µMIC50 (nM)
 CaMK2α (h)101NANA
 Sigma (1/2) (h)9673NA
 15-Lipoxygenase-2 (h)9673270
 M3 (h)90NANA
 IRK (h)74NANA
 Others<50NANA
Ion channels
Manual patch-clamp
RA306 IC50 (µM)KN93 IC50 (µM)IC50 ratiob
 ERG (h)>300.08>375
 Kv4.3 (h)>304>7.5
 Nav1.5 (h)>302.7>11
 Cav1.2 (h)140.915
Eurofins panel (304 kinases)
P33 assays
IC50 (nM)IC50 ratioaATP (µM)
 CaMKIIγ (h)<3∼110
 CaMKIIδ (h)<3110
 CaMKIδ (h)12>415
 CaMKIIβ (h)17>615
 ACK1 (h)26>970
 MLK1 (h)89>3045
 SIK (h)149>5045
 PTK5 (h)216>72155
 Pyk2 (h)249>8390
 IRE1 (h)254>8515
 ULK2 (h)255>8515
 CaMKK2 (h)294>9890
 Others>300>100Km
CEREP panel (107 targets)
Binding, enzyme, and uptake assays 
I%–10 µMI%–1 µMIC50 (nM)
 CaMK2α (h)101NANA
 Sigma (1/2) (h)9673NA
 15-Lipoxygenase-2 (h)9673270
 M3 (h)90NANA
 IRK (h)74NANA
 Others<50NANA
Ion channels
Manual patch-clamp
RA306 IC50 (µM)KN93 IC50 (µM)IC50 ratiob
 ERG (h)>300.08>375
 Kv4.3 (h)>304>7.5
 Nav1.5 (h)>302.7>11
 Cav1.2 (h)140.915

NA, not available.

a

Kinase IC50/CaMKIIδ IC50.

b

RA306 IC50/KN93 IC50.

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