2.7.11.30 (1'R,5'S,6'S)-2-(3',5'-dibromo-1',6'-dihydroxy-4'-oxocyclohex-2'-enyl) acetonitrile the small dibromotyrosine derivative purified from Pseudoceratina sp. suppresses TGF-beta responsiveness by inhibiting TGF-beta type I receptor serine/threonine kinase activity. The compound inhibits the TGF-beta-stimulated transcriptional activations of 3TP-Lux and decreases phosphorylated Smad2/3 levels and the nuclear translocation of Smad2/3 increased by TGF-beta. The compound inhibits TGF-beta-induced EMT and wound healing of A-549 cells and is a potential therapeutic agent for fibrotic disease and cancer treatment. The compound has no effects on TGF-beta receptor synthesis but attenuates TGF-beta-induced transcriptional activation in Mv1Lu cells and TGF-beta-induced expression of fibronectin and PAI-1 in A549 and NMuMG cells and TGF-beta-induced cell migration 217786 2.7.11.30 1-(1,3-benzodioxol-5-yl)-2-(6-ethylpyridin-2-yl)ethanone - 146099 2.7.11.30 1-(1,3-benzodioxol-5-yl)-2-(6-methylpyridin-2-yl)ethanone - 146100 2.7.11.30 1-(1,3-benzodioxol-5-yl)-2-bromo-2-(6-ethylpyridin-2-yl)ethanone - 146101 2.7.11.30 1-(1,3-benzodioxol-5-yl)-2-bromo-2-(6-methylpyridin-2-yl)ethanone - 146102 2.7.11.30 1-(1,3-benzodioxol-5-yl)-2-bromo-2-pyridin-2-ylethanone - 146103 2.7.11.30 1-(1,3-benzodioxol-5-yl)-2-pyridin-2-ylethanone - 146104 2.7.11.30 2,6-lutidine i.e. 2,6-dimethylpyridine 146944 2.7.11.30 2-(6-ethylpyridin-2-yl)-1-quinoxalin-6-ylethanone - 146168 2.7.11.30 2-(6-methylpyridin-2-yl)-1-quinoxalin-6-ylethanone - 146169 2.7.11.30 2-bromo-2-(6-ethylpyridin-2-yl)-1-quinoxalin-6-ylethanone - 146206 2.7.11.30 2-bromo-2-(6-methylpyridin-2-yl)-1-quinoxalin-6-ylethanone - 146207 2.7.11.30 2-bromo-2-pyridin-2-yl-1-quinoxalin-6-ylethanone - 146208 2.7.11.30 2-picoline - 146223 2.7.11.30 2-pyridin-2-yl-1-quinoxalin-6-ylethanone - 146224 2.7.11.30 3-((4-(6-methylpyridin-2-yl)-5-(quinolin-6-yl)-1H-imidazol-2-yl)methyl)benzamide IN-1233, inhibitor specifically inhibits TGF-beta signaling via ALK-5 by acting as a competitive inhibitor of the ATP-binding site, inhibition of activin receptor-like kinase-5 signaling in vivo with the selective small-molecule inhibitor prevents pulmonary arterial hypertension, right ventricular hypertrophy, and vascular remodeling after monocrotaline injection and inhibits the progression of established pulmonary arterial hypertension in this model 77903 2.7.11.30 3-([[4-(1,3-benzodioxol-5-yl)-5-(6-ethylpyridin-2-yl)-1,3-thiazol-2-yl]amino]methyl)benzamide - 146227 2.7.11.30 3-([[4-(1,3-benzodioxol-5-yl)-5-(6-ethylpyridin-2-yl)-1,3-thiazol-2-yl]amino]methyl)benzonitrile - 146228 2.7.11.30 3-([[4-(1,3-benzodioxol-5-yl)-5-(6-methylpyridin-2-yl)-1,3-thiazol-2-yl]amino]methyl)benzamide - 146229 2.7.11.30 3-([[4-(1,3-benzodioxol-5-yl)-5-(6-methylpyridin-2-yl)-1,3-thiazol-2-yl]amino]methyl)benzonitrile - 146230 2.7.11.30 3-([[4-(1,3-benzodioxol-5-yl)-5-pyridin-2-yl-1,3-thiazol-2-yl]amino]methyl)benzamide - 146231 2.7.11.30 3-([[4-(1,3-benzodioxol-5-yl)-5-pyridin-2-yl-1,3-thiazol-2-yl]amino]methyl)benzonitrile - 146232 2.7.11.30 3-([[5-(6-ethylpyridin-2-yl)-4-quinoxalin-6-yl-1,3-thiazol-2-yl]amino]methyl)benzonitrile - 146233 2.7.11.30 3-([[5-(6-methylpyridin-2-yl)-4-quinoxalin-6-yl-1,3-thiazol-2-yl]amino]methyl)benzonitrile - 146234 2.7.11.30 3-[[(5-pyridin-2-yl-4-quinoxalin-6-yl-1,3-thiazol-2-yl)amino]methyl]benzamide - 146246 2.7.11.30 3-[[(5-pyridin-2-yl-4-quinoxalin-6-yl-1,3-thiazol-2-yl)amino]methyl]benzonitrile - 146247 2.7.11.30 3-[[5-(6-ethylpyridin-2-yl)-4-(quinoxalin-6-yl)thiazol-2-ylamino]methyl]benzamide - 146248 2.7.11.30 3-[[5-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)thiazol-2-ylamino]methyl]benzamide - 146249 2.7.11.30 4(quinolin-4-yl)-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole derivatives IC50 of 0.00005-0.0013 mM 23716 2.7.11.30 4(quinolin-4-yl)-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole derivatives IC50 of 0.00015-0.0051 mM, overview 23716 2.7.11.30 4-(1,3-benzodioxol-5-yl)-5-(6-ethylpyridin-2-yl)-1,3-thiazol-2-amine - 146262 2.7.11.30 4-(1,3-benzodioxol-5-yl)-5-(6-methylpyridin-2-yl)-1,3-thiazol-2-amine - 146263 2.7.11.30 4-(1,3-benzodioxol-5-yl)-5-pyridin-2-yl-1,3-thiazol-2-amine - 146264 2.7.11.30 4-([[4-(1,3-benzodioxol-5-yl)-5-(6-ethylpyridin-2-yl)-1,3-thiazol-2-yl]amino]methyl)benzonitrile - 146255 2.7.11.30 4-([[4-(1,3-benzodioxol-5-yl)-5-(6-methylpyridin-2-yl)-1,3-thiazol-2-yl]amino]methyl)benzonitrile - 146256 2.7.11.30 4-([[4-(1,3-benzodioxol-5-yl)-5-pyridin-2-yl-1,3-thiazol-2-yl]amino]methyl)benzonitrile - 146257 2.7.11.30 4-([[5-(6-ethylpyridin-2-yl)-4-quinoxalin-6-yl-1,3-thiazol-2-yl]amino]methyl)benzamide - 146258 2.7.11.30 4-([[5-(6-ethylpyridin-2-yl)-4-quinoxalin-6-yl-1,3-thiazol-2-yl]amino]methyl)benzonitrile - 146259 2.7.11.30 4-([[5-(6-methylpyridin-2-yl)-4-quinoxalin-6-yl-1,3-thiazol-2-yl]amino]methyl)benzamide - 146260 2.7.11.30 4-([[5-(6-methylpyridin-2-yl)-4-quinoxalin-6-yl-1,3-thiazol-2-yl]amino]methyl)benzonitrile - 146261 2.7.11.30 4-phenyl substituted pyrazole inhibitors inhibitory potency of 4-phenyl substituted pyrazole derivatives, IC50 of 30-555 nM, overview 58832 2.7.11.30 4-phenyl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole derivatives IC50 of 0.000005-0.0195 mM 23717 2.7.11.30 4-phenyl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole derivatives IC50 of 0.00011-0.020 mM, overview 23717 2.7.11.30 4-[[(5-pyridin-2-yl-4-quinoxalin-6-yl-1,3-thiazol-2-yl)amino]methyl]benzamide - 146276 2.7.11.30 4-[[(5-pyridin-2-yl-4-quinoxalin-6-yl-1,3-thiazol-2-yl)amino]methyl]benzonitrile - 146277 2.7.11.30 5-(6-ethylpyridin-2-yl)-4-quinoxalin-6-yl-1,3-thiazol-2-amine - 146288 2.7.11.30 5-(6-methylpyridin-2-yl)-4-quinoxalin-6-yl-1,3-thiazol-2-amine - 146289 2.7.11.30 5-pyridin-2-yl-4-quinoxalin-6-yl-1,3-thiazol-2-amine - 146300 2.7.11.30 6-ethyl-2-methylpyridine i.e. 2-ethyl-6-methylpyridine 146945 2.7.11.30 A-83-01 - 146940 2.7.11.30 calphostin C - 21952 2.7.11.30 GW6604 - 146941 2.7.11.30 IN-1130 - 146942 2.7.11.30 IN-1166 - 146943 2.7.11.30 LY-2157299 LY-2157299 inhibits TGF-beta mediated SMAD2 activation and hematopoietic suppression in primary hematopoietic stem cells. In vivo administration of LY-2157299 ameliorates anemia in a TGF-beta overexpressing transgenic mouse model of bone marrow failure. Treatment with LY-2157199 stimulates hematopoiesis from primary myelodysplastic syndrome bone marrow specimens 217787 2.7.11.30 LY2109761 TGF-beta receptor kinase inhibitor LY2109761 reverses the anti-apoptotic effects of TGF-beta1 in myelo-monocytic leukaemic cells, it LY2109761 enhanced apoptosis only in the presence of exogenously added TGF-beta1 146946 2.7.11.30 LY2157299 inhibits Smad3 and Smad3 phosphorylation and antagonizes TGF-beta receptor I kinase activity in vivo in human cancer cells implanted into nude mice, pharmacokinetic model, overview 146937 2.7.11.30 LY364947 competitive to ATP, noncompetitive to the peptide substrate, IC50 is 175 nM, mechanism 11307 2.7.11.30 LY364947 IC50 is 51 nM 11307 2.7.11.30 LY364947 IC50 is 31 nM 11307 2.7.11.30 LY566578 competitive to ATP, noncompetitive to the peptide substrate, IC50 is 70 nM, mechanism 33456 2.7.11.30 LY580276 competitive to ATP, noncompetitive to the peptide substrate, IC50 is 580 nM, mechanism 22321 2.7.11.30 LY580276 - 22321 2.7.11.30 additional information a dominant negative SEK1 mutant abolishes the ALK7-induced apoptosis 2 2.7.11.30 additional information ALK1 mediates inhibition of the ALK5/Smad2/3 pathway 2 2.7.11.30 additional information no inhibition of GDF-9-induced receptor activation by Smad6 2 2.7.11.30 additional information LY294002 completely abolishes the ALK7 mutant T194D/Smad3-induced synergistic effect by inhibiting interaction between the Smad3-Linker and PDX-1 2 2.7.11.30 additional information inhibitory potency of 5-(pyridin-2-yl)thiazole inhibitors, overview 2 2.7.11.30 PD98059 - 3036 2.7.11.30 PEG10 ancient retroviral/retrotransposon element intergrated as a single copy gene in to human chromosome 7q21, encodes two splicing varaiants PEG10-RF1 and PEG10-RF1/2, gag- and gag-pol-like proteins that interact with TGF-beta family proteins, DNA and amino acid sequence deteramination and analysis of PEG10-RF1, PEG10-RF1 inhibits ALK1 and ALK5 signaling by direct interaction, overview 129623 2.7.11.30 Rapamycin - 4862 2.7.11.30 SB-431542 specific TGF-beta receptor kinase inhibitor, a potent antitumor agent for human cancers, induces anchorage-independent cell growth in TGF-beta growth-inhibited cells, and colony formation in growth-induced cells, overview 58833 2.7.11.30 SB-431542 - 58833 2.7.11.30 SB-505124 - 146938 2.7.11.30 SB-525334 - 146939 2.7.11.30 SB203580 - 1808 2.7.11.30 SD-208 - 25848 2.7.11.30 SD-208 inhibition of the TBRI kinase inhibits TGF-beta-mediated smad2 activation in hematopoietic progenitors, alleviates anemia, and stimulates hematopoiesis in vivo in bone marrow 25848 2.7.11.30 SD-208 inhibitor reduces the monocrotaline-induced increase in RV systolic pressure, but the effects on established pulmonary arterial hypertension are modest, and no convincing evidence for in vivo inhibition of TGF-beta-driven target genes is presented 25848 2.7.11.30 SD-208 selektive ALK5 kinase inhibitor 25848 2.7.11.30 Smad7 inhibits induction of receptor activation/signaling by GDF-9 in vivo 58834