152121-30-7 Usage
Description
SB 202190 is a selective, potent, cell-permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC50 values of 50 and 100 nM, respectively. When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases (ERKs, JNKs). Pyridinyl imidazole inhibitors, including this compound, directly bind p38 MAP kinases in the ATP binding pocket. Recently, SB 202190 has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-induced receptor expression, and HIV-mediated depressive disorder.
Uses
Different sources of media describe the Uses of 152121-30-7 differently. You can refer to the following data:
1. SB 202190 is a DFG inhibitor used in the treatment of colorectal cancer. It is a highly selective, potent inhibitor of p38 MAP kinase. SB-202190 is able to promote proliferation of C6 cells in lower c
oncentration but induced apoptosis in higher levels. Studies show that SB202190 can protect neural function from ischemia/reperfusion injury and regulate the activation of Bcl-2 and Bax protein after
ischemia/reperfusion in rat.
2. SB 202190 is a DFG inhibitor used in the treatment of colorectal cancer. It is a highly selective, potent inhibitor of p38 MAP kinase. SB-202190 is able to promote proliferation of C6 cells in lower concentration but induced apoptosis in higher levels. Studies show that SB202190 can protect neural function from ischemia/reperfusion injury and regulate the activation of Bcl-2 and Bax protein after ischemia/reperfusion in rat.
Definition
ChEBI: A member of the class of imidazoles that is 1H-imidazole in which the hydrogens at positions 2, 4, and 5 are replaced by 4-hydroxyphenyl, pyridin-4-yl, and 4-fluorophenyl groups, respectively. It is a widely used inhibitor of mitogen-act
vated protein kinase (MAPK) alpha and beta.
General Description
A potent, reversible, competitive, and cell-permeable inhibitor of p38 MAP kinase. Inhibits p38 phosphorylation of myelin basic protein (MBP) with no effect on the activity of the ERK or JNK MAP kinase subgroups. Also inhibits the kinase activity of p38β (Ki = 16 nM; IC50 = 350 nM) and p38 phosphorylation of activating transcription factor 2 (ATF-2; IC50 = 280 nM). Blocks LPS-induced TNF-α and interleukin biosynthesis. Reported to induce LDL receptor expression in Hep52 cells. A 1 mg/ml solution of SB 202190 (Cat. No. 559397) in anhydrous DMSO is also available.
Biological Activity
A highly selective, potent and cell-permeable inhibitor of p38 MAP kinase. Binds within the ATP pocket of the active kinase (K d = 38 nM, as measured in recombinant human p38), and selectively inhibits the p38 α and β isoforms (IC 50 = 50 and 100 nM at SAPK2a/p38 and SAPK2b/p38 β 2 respectively). Also available as part of the MAPK Inhibitor Tocriset? .
Biochem/physiol Actions
Cell permeable: yes
References
1) Young et al. (1997), Pyridinyl imidazole inhibitors of p38 mitogen-activated protein kinase bind in the ATP site; J. Biol. Chem., 272 12116
2) Davies et al. (2000), Specificity and mechanism of action of some commonly used protein kinase inhibitors; Biochem. J., 351 95
3) Manthey et al. (1998), SB202190, a selective inhibitor of p38 mitogen-activated protein kinase, is a powerful regulator of LPS-induced mRBAs in monocytes; J. Leukoc. Biol., 64 409
4) Nemoto et al. (1998), Induction of apoptosis by SB202190 through inhibition of p38β mitogen-activated protein kinase; J. Biol. Chem., 273 16415
Check Digit Verification of cas no
The CAS Registry Mumber 152121-30-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,5,2,1,2 and 1 respectively; the second part has 2 digits, 3 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 152121-30:
(8*1)+(7*5)+(6*2)+(5*1)+(4*2)+(3*1)+(2*3)+(1*0)=77
77 % 10 = 7
So 152121-30-7 is a valid CAS Registry Number.
InChI:InChI=1/C20H14FN3O/c21-16-5-1-13(2-6-16)18-19(14-9-11-22-12-10-14)24-20(23-18)15-3-7-17(25)8-4-15/h1-12,23-24H
152121-30-7Relevant articles and documents
Treatment for CNS injuries
-
, (2008/06/13)
The present invention is directed to the use of 2,4,5-trisubstituted imidazole compounds and compositions in the treatment of CNS injuries to the brain.
Substituted imidazoles as glucagon receptor antagonists
Chang, Linda L.,Sidler, Kelly L.,Cascieri, Margaret A.,De Laszlo, Stephen,Koch, Greg,Li, Bing,MacCoss, Malcolm,Mantlo, Nathan,O'Keefe, Stephen,Pang, Margaret,Rolando, Anna,Hagmann, William K.
, p. 2549 - 2553 (2007/10/03)
A modestly active, nonselective triarylimidazole lead was optimized for binding affinity with the human glucagon receptor. This led to the identification of a 2- and/or 4-alkyl or alkyloxy substituent on the imidazole C4-aryl group as a structural determinant for significant enhancement in binding with the glucagon receptor (e.g., 41, IC50 = 0.053 μM) and selectivity (> 1000 ×) over p38 MAP kinase in this class of compounds.
Pyridyl imidazoles
-
, (2008/06/13)
Novel 2,4,5-triaryl imidazole compounds and compositions for use in therapy.
