Inhibitor SourceBook™ Second Edition

Protein Tyrosine Kinase (PTK) Inhibitors, continued
Calbiochem • Inhibitor SourceBook
Phosphorylation/Dephosphorylation
Product Cat. No. Comments Size Price
Cucurbitacin I, Cucumis
sativus L.
Curcumin, Curcuma
longa L.
238590 (JSI-124)
A cell-permeable, potent, and highly selective inhibitor of Janus kinase/signal
transducer and activator of transcription 3 (JAK/STAT3) signaling pathway. Suppresses
STAT3 tyrosine phosphorylation in v-Src-transformed NIH 3T3 cells and human lung
adenocarcinoma A549 cells (IC 50 = 500 nM).
239802 [1,7-Bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione]
Inhibits the intrinsic kinase activity of EGFR. Induces apoptosis in both androgendependent
and androgen-independent prostate cancer cells.
Daidzein 251600 (4´,7-Dihydroxyisoflavone)
Inactive analog of Genistein that is also reported to inhibit casein kinase II activity.
Damnacanthal 251650 (3-Hydroxy-1-methoxyanthraquinone-2-aldehyde)
Most potent and selective inhibitor of p56 lck tyrosine kinase and p56 lck
autophosphorylation (IC 50 = 7 nM). Inhibition is competitive with respect to
peptide binding site and mixed non-competitive with the ATP binding site.
Daphnetin 268295 (7,8-Dihydroxy-2H-1-benzopyran-2-one; 7,8-Dihydroxycoumarin)
A broad-spectrum inhibitor of protein kinases. Inhibits EGFR kinase (IC 50 = 7.67 mM),
PKA (IC 50 = 9.33 mM), and PKC (IC 50 = 25 mM).
5´-Deoxy-5´methylthioadenosine
260585 (MeSAdo; MTA)
Inhibits FGF-2 receptor tyrosine kinase and S49 cell-derived high affinity cAMP
phosphodiesterase (K i = 62 mM) in vitro.
DMBI 317200 {(Z)-3-[4-(Dimethylamino)benzylidenyl]indolin-2-one}
Inhibitor of the tyrosine activity of b-PDGFR (IC 50 = 4 mM in PAC- cells) and
FGFR (IC 50 = 5 mM).
EGFR/ErbB-2 Inhibitor 324673 [4557W; 4-(4-Benzyloxyanilino)-6,7-dimethoxyquinazoline]
A cell-permeable, potent, reversible, and ATP competitive inhibitor of EGFR and c-erbB2
(IC 50 = 20 nM and 80 nM, respectively).
Emodin 324694 (6-Methyl-1,3,8-trihydroxyanthraquinone)
Inhibitor of p56 lck (IC 50 = 8.5 mM). Suppresses HER2/neu tyrosine kinase activity
in HER2/neu overexpressing cancer cells.
Erbstatin Analog 324930 (2,5-Dihydroxymethylcinnamate)
Cell-permeable stable analog of Erbstatin. Competitive inhibitor of EGFR kinase activity
(IC 50 = 780 nM). Inhibits the activation of v-Abl tyrosine kinase activity.
Geldanamycin,
Streptomyces
hygroscopicus
345805 Inhibitor of p60 c-src tyrosine kinase activity. Binds Hsp90 and induces degradation of
tyrosine kinases.
Genistein 345834 (4´,5,7-Trihydroxyisoflavone)
A tyrosine kinase inhibitor that also blocks the autophosphorylation of EGFR kinase
(IC 50 = 2.6 mM). Also acts as an inhibitor of p60 v-src (IC 50 = 25 mM).
Genistin 345836 (Genistein, 7-O-b-D-Glucopyranoside)
An inactive analog of the PTK inhibitor Genistein (Cat. No. 345834) and can be used as a
negative control for Genistein. Reported to reduce bone loss in ovarectomized rats.
GTP- 4564 371806 (3-Phenyl-1H-benzofuro[3,2-c]pyrazole; 1-Phenyl-3-H-8-oxa-2,3-diazacyclopenta[a]inden)
A cell-permeable, potent, and specific inhibitor of class III receptor tyrosine kinases
(IC = 300 nM for c-fms, c-kit, wt-FLT3, and ITD-FLT3; .0 mM for PDGFRb).
50
Herbimycin A,
Streptomyces sp.
mg $ 57
00 mg $35
25 mg $47
mg $ 4
0 mg $50
50 mg $73
0 mg $62
mg $84
50 mg $69
mg $44
00 mg $ 80
20 mg
50 mg
$73
$ 46
5 mg $ 06
5 mg $84
375670 An inhibitor of p60 c-src (IC 50 = 900 nM). Reversibly binds to the thiol groups of the kinase. 00 mg $ 48
HNMPA-(AM) 3 397100 (Hydroxy-2-naphthalenylmethylphosphonic Acid Trisacetoxymethyl Ester; Pro-drug II)
Cell-permeable inhibitor of insulin receptor tyrosine kinase (IC 50 = 00 mM).
IGF- R Inhibitor, PPP 407247 (Insulin-like Growth Factor-1 Receptor Inhibitor; Picropodophyllin)
A cell-permeable, potent and specific inhibitor of IGF- R both in vitro
(IC 50 = nM in cell-free kinase assay; 60 nM and < 50 nM for cell viability and
receptor autophosphorylation, respectively, in melanoma cell lines) and in vivo
(complete inhibition of IGF- R-dependent tumor cell growth at 20 mg/kg/ 2 hr s.c.
in SCID mice) with minimum toxic effect (LD 50 > 500 mg/kg). Exhibits little effect
towards IR, FGFR, PDGFR and EGFR.
5 mg $ 3
mg $95
Technical Support
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E-mail calbiochem@emdbiosciences.com
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