Inhibitor SourceBook™ Second Edition

Phosphorylation/Dephosphorylation
MAP Kinase Inhibitors, continued
Product Cat. No. Comments Size Price
Hymenialdisine, Stylissa
damicornis
400085 {4-(2-Amino-4-oxo-2-imidazolidin-5-ylidene)-2-bromo-4,5,6,7-tetrahydropyrrolo
[2,3-c]azepin-8-one; HD; 10Z-Hymenialdisine}
A potent, ATP-competitive inhibitor of GSK-3b (IC 50 = 0 nM). Also inhibits several other
protein kinases, including MEK- (IC 50 = 6 nM), Cdks (IC 50 = 22 nM for Cdk /cyclin B,
40 nM for Cdk2/cyclin E, and 28 nM for Cdk5/p35), and casein kinase (IC 50 = 35 nM).
5-Iodotubercidin 407900 {4-Amino-5-iodo-7-(b-D-ribofuranosyl)pyrrolo[2,3-d]pyrimidine; ITU}
A potent inhibitor of adenosine kinase (K i = 30 nM) and Ser/Thr-specific kinases that also
acts as a potent, and competitive inhibitor of ERK2 (K i = 530 nM).
N MEK Inhibitor I 444937 A cell-permeable pyridine-containing vinylogous cyanamide compound that acts
as a potent and selective inhibitor of MEK (IC 50 = 2 nM) with little activity towards
MKK3 and MKK4 (IC 50 > mM). The inhibition is noncompetitive with respect to ERK
and the compound displays significant affinity only towards ATP-bound MEK
(i.e., noncompetitive with respect to ATP). Exhibits superior potency, solubility, and
stability compared to U0 26 (Cat. No. 662005) in aqueous solutions.
MEK /2 Inhibitor 444939 [Z-& E-a-(Amino-((4-aminophenyl)thio)methylene)-2-(trifluoromethyl)
benzeneacetonitrile; SL327]
A cell-permeable, selective inhibitor of MEK (IC = 80 nM) and MEK2 (IC = 220 nM).
50 50
Inhibits ERK , MKK3/p38, MKK4, JNK, and PKC activities only at higher concentrations
(IC > 0 mM).
50
MEK Inhibitor II 444938 [2-Chloro-3-(N-succinimidyl)-1,4-naphthoquinone]
A cell-permeable, potent, and selective inhibitor of MEK (IC 50 = 380 nM for MEK ).
N MK2a Inhibitor 475863 [CMPD1; 4-(2´-Fluorobiphenyl-4-yl)-N-(4-hydroxyphenyl)-butyramide; Mitogen-activated
protein kinase-activated protein kinase 2a Inhibitor]
A p-amidophenolic compound that selectively inhibits the phosphorylation of MK2a
app (mitogen-activated protein kinase-activated protein kinase 2a; K = 330 nM) by p38a
i
in a non-ATP-competitive manner. Does not block the kinase activity of p38a towards
the other two known p38 substrates, MBP and ATF-2.
InSolution ML 3 63 475800 {4-[5-(4-Fluorophenyl)-2-(4-methanesulfinyl-benzylsulfanyl)-3H-imidazol-4-yl]pyridine}
Supplied as a 0 mM ( mg/236 ml) solution in DMSO. A cell-permeable inhibitor that
combines the structural features of cytokine release inhibitors SKF-86002 (Cat. No.
567305) and p38 MAP kinase inhibitor SB 203580 (Cat. No. 559389). Occupies the ATP
binding site of p38 MAP kinase and inhibits its activity (IC 50 = 4.0 mM).
p38 MAP Kinase
Inhibitor
p38 MAP Kinase
Inhibitor III
N InSolution p38 MAP
Kinase Inhibitor III
506126 [2-(4-Chlorophenyl)-4-(4-fluorophenyl)-5-pyridin-4-yl-1,2-dihydropyrazol-3-one]
A potent p38 MAP kinase inhibitor (IC 50 = 35 nM).
506121 {(RS)-{4-[5-(4-Fluorophenyl)-2-methylsulfanyl-3H-imidazol-4-yl]pyridin-2-yl}-
(1-phenylethyl)amine]; ML3403}
A cell-permeable, potent, selective, and ATP-competitive inhibitor of p38 MAP kinase
(IC = 380 nM for p38a).
50
506148 A 0 mM ( mg/247 ml) solution of p38 MAP Kinase Inhibitor III (Cat. No. 506 2 )
in DMSO.
NPPB 484100 5-Nitro-2-(3-phenylpropylamino)benzoic Acid
Blocks phosphorylation and activation of ERK /2 and JNK/SAPK, but not p38.
PD 98059 513000 (2´-Amino-3´-methoxyflavone)
A potent and selective MEK inhibitor. It selectively blocks the activation of MEK,
thus preventing its phosphorylation by c-Raf or MEK kinase (IC 50 = 2–7 mM).
PD 693 6 513030 [4-(4-Fluorophenyl)-2-(4-nitrophenyl)-5-(4-pyridyl)-1H-imidazole]
A potent and selective p38 MAP kinase inhibitor (IC 50 = 89 nM).
SB 202 90 559388 [FHPI; 4-(4-Fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)1H-imidazole]
A potent, selective, and cell-permeable p38 MAP kinase inhibitor (IC 50 = 50 nM for
SAPK2a/p38 and 00 nM for SAPK2b/p38b2).
500 mg $207
mg $ 5
26 Orders Phone 800 854 34 7
Calbiochem • Inhibitor SourceBook
Fax 800 776 0999
Web www.emdbiosciences.com/calbiochem
mg
5 mg
mg
5 mg
$95
$335
$84
$294
5 mg $79
5 mg $ 63
mg $ 0
500 mg $98
mg $ 2
mg $ 2
0 mg $62
5 mg $88
mg $98
mg $98
InSolution SB 202 90 559397 A mg/ml solution of SB 202 90 (Cat. No. 559388) in anhydrous DMSO. ml $ 04
SB 202 90,
Immobilized
559403 An immobilized form of the p38 MAP kinase inhibitor (Cat. No. 559388) covalently
attached to hydrophilic acrylic beads via a 3-carbon spacer. Useful for affinityprecipitation
of p38 MAP kinase and other functionally related proteins from cell
or tissue extracts.
set $ 32