681245-85-2
Chemical Structure
A-800141
- CAS No.: 681245-85-2
- Formula:C24H30N2O4S
- Molecular Weight:442.57
IUPAC Name: (Z)-2-((2-(3-(diethylamino)prop-1-en-1-yl)phenyl)sulfonamido)-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid
InChIKey: GKLFXULRKHHGON-XFXZXTDPSA-N
SMILES: O=C(C1=C2CCCCC2=CC=C1NS(=O)(C3=CC=CC=C3/C=C\CN(CC)CC)=O)O
Biological Activity: A-800141 is an orally active, selective, sulfonamide-based MetAP2 inhibitor (IC50=12 nM) that binds reversibly to MetAP2 and interacts with its manganese ions. A-800141 induces the production of N-terminal methionine-unprocessed GAPDH variants, which in turn triggers G1-phase cell cycle arrest, elevates p21 levels, and reduces the levels of phosphorylated Rb and total cyclin A. A-800141 exhibits anti-angiogenic and tumor growth inhibitory effects, and produces synergistic effects when combined with cytotoxic inhibitors or BCL-2 inhibitors. A-800141 has been widely used in scientific research related to B-cell lymphoma, neuroblastoma, prostate cancer, colon cancer, melanoma and other fields[1][2][3].
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A-800141 | A-800141 is an orally active, selective, sulfonamide-based MetAP2 inhibitor (IC50=12 nM) that binds reversibly to MetAP2 and interacts with its manganese ions. A-800141 induces the production of N-terminal methionine-unprocessed GAPDH variants, which in turn triggers G1-phase cell cycle arrest, elevates p21 levels, and reduces the levels of phosphorylated Rb and total cyclin A. A-800141 exhibits anti-angiogenic and tumor growth inhibitory effects, and produces synergistic effects when combined with cytotoxic inhibitors or BCL-2 inhibitors. A-800141 has been widely used in scientific research related to B-cell lymphoma, neuroblastoma, prostate cancer, colon cancer, melanoma and other fields. | |||||||||||||||||||||
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References
- [1]. Wang J, et al. Correlation of tumor growth suppression and methionine aminopetidase-2 activity blockade using an orally active inhibitor. Proc Natl Acad Sci U S A. 2008;105(6):1838-1843. [Content Brief]
- [2]. Yin SQ, et al. The development of MetAP-2 inhibitors in cancer treatment. Curr Med Chem. 2012;19(7):1021-1035. [Content Brief]
- [3]. Mauriz JL, et al. Methionine aminopeptidases as potential targets for treatment of gastrointestinal cancers and other tumours. Curr Drug Targets. 2010;11(11):1439-1457. [Content Brief]
