Identification | Back Directory | [Name]
3-(1-(3-([1,1'-biphenyl]-4-ylamino)-3-oxopropyl)-1H-1,2,3-triazol-4-yl)-6-hydroxy-1-methyl-2-phenyl-1H-indole-5-carboxylic acid | [CAS]
1143579-78-5 | [Synonyms]
II-B08 3-(1-(3-([1 FAP1 Inhibitor LMWPTP Inhibitor CD45 Inhibitor V Lyp Inhibitor III 1'-biphenyl]-4-ylamino)-3-oxopropyl)-1H-1 3-triazol-4-yl)-6-hydroxy-1-methyl-2-phenyl-1H-indole-5-carboxylic acid 3-(1-(3-([1,1'-biphenyl]-4-ylamino)-3-oxopropyl)-1H-1,2,3-triazol-4-yl)-6-hydroxy-1-methyl-2-phenyl-1H-indole-5-carboxylic acid | [Molecular Formula]
C33H27N5O4 | [MDL Number]
MFCD32645102 | [MOL File]
1143579-78-5.mol | [Molecular Weight]
557.599 |
Hazard Information | Back Directory | [Description]
II-B08, also known as PTP Inhibitor XXXI, is a cell-permeable SHP2 inhibitor (IC50 = 5.5 μM). II-B08 blocks growth factor stimulated ERK1/2 activation and hematopoietic progenitor proliferation, providing supporting evidence that chemical inhibition of SHP2 may be therapeutically useful for anticancer and antileukemia treatment. X-ray crystallographic analysis of the structure of SHP2 in complex with 9 reveals molecular determinants that can be exploited for the acquisition of more potent and selective SHP2 inhibitors. | [Uses]
II-B08 is a reversible and noncompetitive SHP2 inhibitor (IC50: 5.5 μM, 15.7, 14.3 μM for SHP2, SHP1, PTP1B). II-B08 can be used for cancer research[1]. | [References]
[1] Zeng LF, et al. Therapeutic potential of targeting the oncogenic SHP2 phosphatase. J Med Chem. 2014 Aug 14;57(15):6594-609. DOI:10.1021/jm5006176 [2] Zhang X, et al. Salicylic acid based small molecule inhibitor for the oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2). J Med Chem. 2010 Mar 25;53(6):2482-93. DOI:10.1021/jm901645u |
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