Inhibitor SourceBook™ Second Edition

Phosphorylation/Dephosphorylation
Product Cat. No. Comments Size Price
JAK Inhibitor I 420099 {2-(1,1-Dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one}
A potent inhibitor of Janus protein tyrosine Kinases (JAKs). Displays potent inhibitory
activity against JAK (IC 50 = 5 nM for murine JAK ), JAK2 (IC 50 = nM), JAK3 (K i =
5 nM), and Tyk2 (IC 50 = nM).
N InSolution JAK
Inhibitor I
420097 {2-(1,1-Dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one}
A 0 mM (500 mg/ 62 ml) solution of JAK Inhibitor I (Cat. No. 420099) in DMSO.
N JAK2 Inhibitor II 420132 (1,2,3,4,5,6-Hexabromocyclohexane)
A cell-permeable hexabromocyclohexane compound that acts as a specific and direct
inhibitor of JAK2 autophosphorylation (maximal inhibition at 50 mM in BSC-40 cells
overexpressing JAK2).
JAK3 Inhibitor I 420101 [4-(4´-Hydroxyphenyl)amino-6,7-dimethoxyquinazoline; WHI-P131]
A specific inhibitor of JAK3 (IC 50 = 78 mM). Does not affect the activity of JAK , JAK2,
ZAP/Syk, or Src tyrosine kinases.
JAK3 Inhibitor II 420104 {4-[(3´-Bromo-4´-hydroxyphenyl)amino]-6,7-dimethoxyquinazoline; WHI-P154}
A potent, cell-permeable inhibitor of JAK3 that is reported to kill glioblastoma cells
(IC 50 = 8 3 nM).
JAK3 Inhibitor III 420106 [4-(3´,5´-Dibromo-4-hydroxyphenyl)amino-6,7-dimethoxyquinazoline; WHI-P97]
A potent and specific inhibitor of JAK3 (IC 50 = mM).
JAK3 Inhibitor IV 420121 [2-Naphthyl-(N-isopropyl,N-benzyl)-b-aminoethylketone, HCI; ZM 39923]
A potent and selective ATP-competitive inhibitor of JAK3 (pIC 50 = 7. ). Weakly inhibits
other tyrosine kinases (pIC 50 = 5.6 for EGF-R; 4.4 for JAK ). In neutral buffer undergoes
a retro-Michael breakdown (t /2 = 36 min at 25˚C, pH 7.43) to the active analog 2-naphthylvinyl
ketone (Cat. No. 420 22) [pIC 50 = 6.8 for JAK3; 5.0 for EGF-R; 4.7 for JAK ].
JAK3 Inhibitor V 420122 [(2-Naphthylvinyl Ketone); ZM 449829]
A breakdown product of JAK3 Inhibitor-IV (Cat. No. 420 2 ) with similar inhibitory
activities (pIC 50 = 6.8 for JAK3; 5.0 for EGF-R; 4.7 for JAK ). Also inhibits STAT-5
phosphorylation and T-cell proliferation.
JAK3 Inhibitor VI 420126 A cell-permeable, potent inhibitor of JAK3 (IC 50 = 27 nM). Binds to the enzyme active
site and prevents IL-2-induced cellular phosphorylation of JAK3 and STAT5.
JAK3 Inhibitor, Negative
Control
420112 (4-Phenylamino-6,7-dimethoxyquinazoline; WHI-P258)
A useful negative control compound for JAK3 inhibitors.
Lavendustin A 428150 {5-Amino-[(N-2,5-dihydroxybenzyl)-N´-2-hydroxybenzyl]salicylic Acid; RG14355}
A potent inhibitor of EGFR kinase (IC 50 = nM) and p60 c-src (IC 50 = 500 nM).
Lavendustin B 428160 [5-Amino-(N,N´-bis-2-hydroxybenzyl)salicylic Acid]
A negative control for Lavendustin A (IC 50 = .3 mM for EGFR kinase).
Lavendustin C 234450 [Compound 5; 5-(N-2´,5´-Dihydroxybenzyl)aminosalicylic Acid]
Potent inhibitor of p60c-src (IC = 200 nM) and Ca 50 2+ /calmodulin-dependent kinase II
(IC = 200 nM).
50
N Lck Inhibitor 428205 A cell-permeable pyrrolopyrimidine compound that acts as a potent, selective and ATPcompetitive
inhibitor of Lck (IC at 5 mM of ATP = < nM, 2 nM, 70 nM, .57 mM, and
50
.98 mM for Lck Y 64-509 394 , lckcd pY394 , src, kdr, and tie-2, respectively; IC at mM of
50
ATP = 6 nM, 66 nM, 26 nM, 420 nM, and 5. 8 mM for Lck Y 64-509 394 , blk, fyn, lyn, and
csk, respectively). Only minimally affects the activities of other kinases (IC = 3.2 mM,
50
> 33 mM, > 50 mM, and > 50 mM for EGFR, PKC, CDC2/B, and ZAP-70, respectively).
N
Protein Tyrosine Kinase (PTK) Inhibitors, continued
LFM-A 435301 [a-Cyano-b-hydroxy-b-methyl-N-(3-fluorophenyl)propenamide]
A useful negative control (IC 50 ≥ 454 mM) for LFM-A 3.
LFM-A 2 435302 {a-Cyano-b-hydroxy-b-methyl-N-[4-(trifluoromethoxy)phenyl]propenamide}
A potent and specific inhibitor of EGFR kinase (IC 50 = .7 mM).
LFM-A 3 435300 [a-Cyano-b-hydroxy-b-methyl-N-(2,5-dibromophenyl)propenamide]
A potent and specific inhibitor of Bruton’s tyrosine kinase (BTK; IC 50 = 7.2 mM for human
BTK in vitro and IC 50 = 2.5 mM for recombinant BTK).
Met Kinase Inhibitor 448101 (3Z)-N-(3-Chlorophenyl)-3-((3,5-dimethyl-4-((4-methylpiperazin-1-yl)carbonyl)-1Hpyrrol-2-yl)methylene)-N-methyl-2-oxo-2,3-dihydro-1H-indole-5-sulfonamide;
SU11274
A cell-permeable pyrrole indolinone compound that acts as a potent, reversible, and
ATP-competitive inhibitor of Met kinase activity (IC = 20 nM).
50
500 mg $83
500 mg $83
25 mg $88
5 mg $ 8
5 mg $ 50
mg $ 27
0 mg $ 90
0 mg $ 68
5 mg $ 5
50 Orders Phone 800 854 34 7
Calbiochem • Inhibitor SourceBook
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500 mg
mg
500 mg
mg
500 mg
mg
$76
$ 27
mg $ 7
mg $ 7
mg $62
mg $82
$44
$75
$ 42
$230
5 mg $98
mg $85