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 Protein Kinase Inhibitor Specificity Table
Enzyme Explorer
 

Selecting an appropriate protein kinase inhibitor can pose a challenge due to the complexity of the protein kinase family. Factors such as inhibitor specificity and cell permeability should be considered. The table below is based on currently available data. For specific information on specific inhibitors, consult the citations. Specific kinetic data for inhibitors marked with an "X" was not available. References may be viewed by clicking in the reference column or scrolling down past the product table.

Prod No. Ref No. Product Description    PKA       PKC       PKG    CAM
Kinase		  MLCK  Casein Kinase  PTK  Notes & MAPK, CDK, Other Kinases
A1651-5Adenosine 3',5'-cyclic-Monophosphothioate, RP-Isomer 11µM        
A7410 6Amiloride HCl        EGFR 
A3145 7-9Apigenin 10µM     FGFR(20µM) 
A8186 10 Arg-Lys-Arg-Ala-Arg-Lys-GLu350-460µM  85-100µM      
A4308 11Autocamtide 2-Related Inhibitory Peptide   CAMKII(40nM)    
B6292 12Bisindolylmaleimide I Hydrochloride (GF 109203X)2.0µM14nM       
B178 13-15Butein>500µM>500µM    See NotesEGFR(16µM); p60c-src(65µM)
P1431 18-19Calmodulin        GRK 2&3(2µM) GRK5(40nM) & GRK6
C630320-21Calphostin C>50µM50nM    >50µM  
C2932 23Chelerythrine chloride 0.66µM       
C240 24 Rp-8-[(4Chlorophenyl)thio]-cGMPS Triethylamine  0.5µM      
D7802 25Daidzein       CKII Does not inhibit MAP2Kinase
D3768 27Dequalinium Chloride 8-15µM      β1 (8-15µM), I,II,III (11µM)
D1916295,6-Dichlorobenzimidazole riboside      CKII(4-10µM)  
D4681 30-32L-threo-Dihydrosphingosine X       
D266733,34 2,5-Dihydroxycinnamic Acid Methyl Ester       EGFR  
E2250 36Ellagic Acid2µM8µM       
E788137-39 Emodin>200µM>200µM    CKII(2µM)   
E3645 40rac-2-Ethoxy-3-Hexadecanamido-1-Propyl Phosphocholine  X     ID50=2.32µM for Leukemic HL60 cells
E3770 40rac-2-Ethoxy-3-Octadecanamido-1-Propyl Phosphocholine  X      ID50=1.64µM for Leukemic HL60 cells
G3381 41-43Geldanamycin        erbB, EGFR, v-src  
G6649
G6776		44-50Genistein>100µM15µM     See NotesEGFR(2.6µM)insulin(41µM)V-src(26µM) V-abl(39µM)
G0897 51Genistin        Neg. Control 
G2911 12GF 109203X (Bisindolylmaleimide I Hydrochloride)2.0µM10nM       
I7016 52,53H-7 Dihydrochloride (1-(5-Isoquinolinesulfonyl)-2-methylpiperazine Dihydrochloride)3.0µM6.0µM5.8µM 97µMCKI(100µM) KII(780µM)  
I6891 52,53H-7 Free Base (1-(5-Isoquinolinesulfonyl)-2-methylpiperazine) 3.0µM6.0µM5.8µM 97µM CKI(100µM) CKII(780µM)   
M9656 52H-8, N-(2-[Methylamino]ethyl)-5-isoquinolinesulfonamide Hydrochloride1.2µM 14.4µM0.48µM 68µM CKI(133µM) CKII(950µM)  
B1427 54-57H-89 48nM14µM340nMCAMKII(11µM)39µMCKI(34µM), CKII(124µM)   
I1392 59HA-100 8µM12µM4µM  240µM   
G1274 59-65HA-10042.3µM40µM1.3µM CAMKII(13µM)150µM    
H139 66HA-1077 2HCL1.6µM  1.6µM 36µM   
H664967-69Herbimycin A        p210bcr-abl 
H5257 71Hispidin  X      
H7904 72Hydroxytamoxifen 88µM      
H925273,74 Hypericin>50µM3.3µM       
I040475 Indirubin 3'-monoxime        Glycogen synthase Kinase (5-50nM)& CDK(5-100nM)
I214276-82KN-62 >100µM>100µM  CAMKII(0.3-1.8µM)>100µM    
K112 81-86KN-92    Neg.Control     
K138583KN-93          
K376187KT5720 60nM 2.4nM      
L240088-91Lavendustin A        EGFR(4.4ng/ml) 
L502592 Leflunomide       BTK 
M227293,94Melittin  1-4µM   0.08-1.4µM    
M7795 40rac-2-Methoxy-3-Hexadecanamido-1-Propyl phosphocholine  X      
M804540rac-2-Methoxy-3-Octadecanamido-1-Propyl phosphocholine  X       
I276495-97 ML-7 21µM42µM   300nM   
C117297-103 ML-9    XX    
M6760104-105 Myricetin 27.5µM12.1µM   1.7µMCKI(9µM), CKII(0.6µM) pp130fps(1.8µM), insulin receptor(2.6) 
N161 106NPC-15437 DiHCl  X       
O0886107Olomoucine         CDK Inhibitor
P4509108-109 Palmitoyl-DL-Carnitine Chloride 34µM        
P215 110-112PD 098,059         prevents the activation of MAPKK1 by Raf or MEK kinase
P7912113 Phloretin ~5µM       
P0453114-118Piceatannol 3µM8µM   12µM  See notesTyrosine kinases Syk, p40(15µM), p56lck(66µM) and p72. CDK(19µM)
P1004119Polymyxin B Sulfate  ~10µM       
P6062120 Protein kinase A inhibitor fragment 6-22 amide1.6nM        
P8462 121Protein Kinase C Fragment 19-36423µM147nM  24µM    
P0393122-125Protein Kinase Inhibitor from porcine heartX        
P0300123-125Protein Kinase Inhibitor Rabbit Sequence2.3nM        
P5015123-125Protein Kinase Inhibitor from rabbit muscleX        
Q0125105,126,
127		Quercetin  20-40µM   CKG(220nM), CKI(45µM), CKII(100nM)See NotesEGF Receptor(410nM), I, IIA, IIB(10µM), III(10µM), Mg++ Dep., P60v-src(50µM)
R2146128-133 Radicicol       src(0.1µg/ml) 
R0395134-135Rapamycin       p70s6k, p33cdk2 and p34cdc2. mTOR
R136 136-139Ro 31-8220 (Bisindolylmaleimide IX)1.5µM 7.6nM  CAMKII(17µM)   GRK5, GSK3
R137 136,140,
141		Ro 32-0432         10-fold selectivity for PKCα; 4-fold selectivity for PKCβI over PKCε. GRK5 inhibitor; less potent inhibitor of GRK2 or GRK3
R7772142,143Roscovitine         p34cdc2(0.45µM), CDK2
R5648144 Rottlerin See notes  CAMKIII(5.3µM)   PKCδ 3-6 µM; PKCα, PKCβ, PKCγ 30-42 µM
S8307145SB 203580        p38 MAPK (0.5µM)
S7049 146-148D-Sphingosine  53µM  CAMKIII(20µM)   Also Inhibits MAPK
S4400 73,105,
149-155		Staurosporine6nM 2.7-5.5nM8.5nMCAMKII(20nM) 21nM C-src(10nM), EGFR(600nM), Insulin(60nM)V-Src(6nM)V-abl(80nM) Inhibits CDK 1,2&5
T5648 157,158Tamoxifen Free Base 5-15µM      
T9262157,158Tamoxifen Citrate 5µM       
T3126160(+)-a-Tocopherol Acid Succinate X       
T7254 105 N a-p-Tosyl-L-lysine chloromethyl ketone Hydrochloride  1mM      
T7040 161Tyrphostin 1       EGFR >1250µMNegative Control
T7165 161Tyrphostin 23       EGFR 35µM 
T7665 161Tyrphostin 51        EGFR 0.8µM 
T7790 161Tyrphostin 63        EGFR 6500µMNegative Control
T182 162,163Tyrphostin A9        PDGFR(0.5µM), EGFR(460µM) 
T9177 164Tyrphostin AG 126      XBlocks TNFα and NO production in macrophages
T3434 51,165,
166		Tyrphostin AG 490       Jak-2 
T2067 167Tyrphostin AG 879      pp140c-trk(10µM) 
T4057 168Tyrphostin AG 1296        PDGFR 
T5317161Tyrphostin AG 1433        PDGR & VEGFRPDGFβ receptor(5 µM); VEGFreceptor(9.3µM)
T4182 169Tyrphostin AG 1478        EGFR  
T4192161Tyrphostin SU 1498        VEGFR(700nM) 
U120 170-172U0126         MEK1(72nM), MEK2(58nM)
W1628173,174 Wortmannin     200nM  PI3Kinase(3nM)


 No.  References
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