Target Validation Information
Target ID T89529
Target Name mRNA of Protein tyrosine phosphatase-1B
Target Type
Successful
Drug Potency against Target USNIC ACID Drug Info IC50 = 16400 nM [529326]
16-alphaH,17-isovaleryloxy-ent-kauran-19-oic acid Drug Info IC50 = 7100 nM [528088]
EVANS BLUE Drug Info IC50 = 1300 nM [527017]
TRYPAN BLUE Drug Info IC50 = 3900 nM [527017]
Abyssinone-VI-4-O-methyl ether Drug Info IC50 = 14800 nM [528537]
DYSIDINE Drug Info IC50 = 6700 nM [529869]
Ohioensin G Drug Info IC50 = 5600 nM [529192]
Mulberrofuran W Drug Info IC50 = 2700 nM [530464]
PHELLIGRIDIN I Drug Info IC50 = 3000 nM [528656]
Abyssinone-IV Drug Info IC50 = 16000 nM [528537]
Abyssinoflavanone VI Drug Info IC50 = 18900 nM [528828]
USIMINE A Drug Info IC50 = 15000 nM [529326]
BURTTINONE Drug Info IC50 = 18900 nM [529806]
CAULERPIN Drug Info IC50 = 3770 nM [528096]
FORMYLCHROMONE Drug Info Ki = 4300 nM [531033]
Oxalylaminobenzoic acid Drug Info Ki = 18 nM [531033]
OLEANOLIC_ACID Drug Info IC50 = 4200 nM [530332]
Isoxazolecarboxylic acid Drug Info Ki = 5700 nM [531033]
Oleanonic acid Drug Info IC50 = 3500 nM [529697]
ALBAFURAN A Drug Info IC50 = 9200 nM [530464]
URSOLIC ACID Drug Info IC50 = 3600 nM [530454]
NEORAUTENOL Drug Info IC50 = 7600 nM [530454]
Abyssinin II Drug Info IC50 = 17300 nM [528828]
Sigmoidin F Drug Info IC50 = 14200 nM [528828]
Kuwanon L Drug Info IC50 = 16900 nM [527927]
LICOAGROCHALCONE A Drug Info IC50 = 16900 nM [528828]
Ohioensin F Drug Info Ki = 1500 nM [529192]
24-hydroxyursolic acid Drug Info IC50 = 12800 nM [529697]
Erysubin E Drug Info IC50 = 8800 nM [530454]
Erybreadin D Drug Info IC50 = 6400 nM [530454]
3,9-Dihydroxy-4-prenyl-[6aR,11aR]pterocarpan Drug Info IC50 = 19500 nM [530454]
Isochroman mono-carboxylic acid Drug Info IC50 = 51.63 nM [531033]
Kuwanon R Drug Info IC50 = 8200 nM [530464]
Spathodic acid Drug Info IC50 = 18800 nM [529697]
Kuwanon V Drug Info IC50 = 13800 nM [530464]
5-deoxyabyssinin II Drug Info IC50 = 19200 nM [528828]
Abyssinoflavanone VII Drug Info IC50 = 15700 nM [528828]
SIGMOIDIN A Drug Info IC50 = 14400 nM [528828]
3alpha,24-dihydroxyolean-12-en-27-oic acid Drug Info IC50 = 11700 nM [528115]
3beta-acetoxyolean-12-en-27-oic acid Drug Info IC50 = 8500 nM [528115]
3beta-hydroxyurs-12-en-27-oic acid Drug Info IC50 = 4900 nM [528115]
3beta,6beta-dihydroxyolean-12-en-27-oic acid Drug Info IC50 = 12800 nM [528115]
3-oxoolean-12-en-27-oic acid Drug Info IC50 = 6800 nM [528115]
18beta-Glycyrrhetic acid Drug Info IC50 = 13800 nM [528115]
Methyl3beta-hydroxyolean-12-en-27-oate Drug Info IC50 = 16000 nM [528115]
ERYTHRIBYSSIN A Drug Info IC50 = 19300 nM [530454]
Pomolic acid Drug Info IC50 = 3900 nM [529697]
SIGMOIDIN B Drug Info IC50 = 19400 nM [528828]
Augustic acid Drug Info IC50 = 4930 nM [530467]
3-epi-masilinic acid Drug Info IC50 = 14330 nM [530467]
Sanggenon C Drug Info IC50 = 2600 nM [527927]
OHIOENSIN A Drug Info IC50 = 4300 nM [529192]
ERTIPROTAFIB Drug Info IC50 = 1400 nM [529004]
3beta-hydroxyolean-12-en-27-oic acid Drug Info IC50 = 5200 nM [528115]
18alpha-Glycyrrhetic acid Drug Info IC50 = 15600 nM [528115]
Mulberrofuran D Drug Info IC50 = 4300 nM [530464]
Ohioensin C Drug Info IC50 = 7600 nM [529192]
1,2,3,4,6-penta-O-galloyl-D-glucopyranose Drug Info IC50 = 4800 nM [531140]
RK-682 Drug Info IC50 = 4400 nM [531115]
3-(4,5-Bis-biphenyl-4-yl-1H-imidazol-2-yl)-phenol Drug Info IC50 = 8600 nM [526334]
Kuwanon J Drug Info IC50 = 2700 nM [530464]
Methyl 3beta-hydroxyolean-12-en-28-oate Drug Info IC50 = 14200 nM [528115]
Rotungenic acid Drug Info IC50 = 10900 nM [529697]
Abyssinin I Drug Info IC50 = 18200 nM [528828]
4'-((2-butylbenzofuran-3-yl)methyl)biphenyl-4-ol Drug Info IC50 = 1190 nM [530028]
4-(p-toluidino)-3-isopropylnaphthalene-1,2-dione Drug Info IC50 = 19590 nM [527986]
1,2-NAPHTHOQUINONE Drug Info IC50 = 1640 nM [526377]
LICOAGROCHACONE A Drug Info IC50 = 19100 nM [530275]
Sanggenon G Drug Info IC50 = 1600 nM [527927]
3-isopropyl-4-(phenylthio)naphthalene-1,2-dione Drug Info IC50 = 13660 nM [527986]
MASLINIC ACID Drug Info IC50 = 5930 nM [530467]
4'-(2-butylbenzofuran-3-yl)biphenyl-4-ol Drug Info IC50 = 740 nM [530028]
Mulberrofuran C Drug Info IC50 = 4900 nM [527927]
ERYBREADIN B Drug Info IC50 = 4200 nM [530454]
UVAOL Drug Info IC50 = 15600 nM [529697]
19alpha,24-dihydroxyurs-12-en-3-on-28-oic acid Drug Info IC50 = 8100 nM [529697]
CHROMOTROPATE Drug Info IC50 = 9700 nM [527017]
FOLITENOL Drug Info IC50 = 7800 nM [530454]
Erybreadin C Drug Info IC50 = 7300 nM [530454]
Action against Disease Model ISIS 113715 In cultured monkey hepatocytes, ISIS 113715 treatment dose-dependently reduced PTP-1B mRNA expression, with an IC 50 of less than 10 nM. [552912] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations Although heterozygous loss of PTP1B has no effect on t uMorigenesis,homozygous PTP1B deficiency dramatically delays or prevents the onset of MMTV-NeuNT-evoked breast t uMors. The effects of PTP1B deficiency correlate with defective extracellular signal-regulated kinase activation in preneoplastic mammary glands from compound mutant mice.In contrast,PTP1B deficiency has no effect on MMTV-polyoma middle T t uMorigenesis. Our data raise the possibility that PTP1B inhibitors may be chemopreventative for some forms of breast cancer. [552912]
References
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Ref 527927Bioorg Med Chem Lett. 2006 Mar 1;16(5):1426-9. Epub 2005 Dec 13.Protein tyrosine phosphatase 1B inhibitors from Morus root bark.
Ref 530454Bioorg Med Chem Lett. 2009 Dec 1;19(23):6745-9. Epub 2009 Oct 1.Cytotoxic and PTP1B inhibitory activities from Erythrina abyssinica.
Ref 529697J Nat Prod. 2008 Oct;71(10):1775-8. Epub 2008 Sep 18.Triterpenoids from the leaves of Diospyros kaki (persimmon) and their inhibitory effects on protein tyrosine phosphatase 1B.
Ref 529697J Nat Prod. 2008 Oct;71(10):1775-8. Epub 2008 Sep 18.Triterpenoids from the leaves of Diospyros kaki (persimmon) and their inhibitory effects on protein tyrosine phosphatase 1B.
Ref 527017Bioorg Med Chem Lett. 2004 Apr 19;14(8):1923-6.Evans Blue and other dyes as protein tyrosine phosphatase inhibitors.
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Ref 530454Bioorg Med Chem Lett. 2009 Dec 1;19(23):6745-9. Epub 2009 Oct 1.Cytotoxic and PTP1B inhibitory activities from Erythrina abyssinica.

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