TGF-beta/Smad

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TGF-beta/Smad Inhibitors (16)

water-soluble

Cat.No. Product Name Information Product Citations Customer Reviews
S1067 SB431542 SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM, 100-fold more selective for ALK5 than p38 MAPK and other kinases.
  • Genes Dev, 2014, 28(8):858-74
  • Cell Mole Bioeng, 2014, 10.1007/s12195-014-0333-z
  • Proc Natl Acad Sci U S A, 2013, 110(52):E5039-48
S2618 LDN-193189 LDN193189 is a selective BMP signaling inhibitor, inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively, exhibits 200-fold selectivity for BMP versus TGF-β.
  • Cancer Cell, 2014, 26(4):521-33
  • J Cell Sci, 2012, 126(Pt 1):234-43
  • Int J Cancer, 2014, 10.1002/ijc.29220
S2230 LY2157299 LY2157299 is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM. Phase 2/3.
  • Cancer Res, 2014, 74(21):5963-77
  • Lab Chip, 2013, 13(10):1969-78
S2704 LY2109761 LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM, respectively; shown to negatively affect the phosphorylation of Smad2.
  • Toxicology, 2014, 326C:9-17
  • Invest Ophthalmol Vis Sci, 2014, 55(3):1770-9
  • PLoS One, 2013, 8(12):e83521
S1476 SB525334 SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM, is 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6.
  • Hypertension, 2013, 62(5):951-6
  • Cancer Lett, 2014, 355(1):130-40
  • Cell Signal, 2014, 10.1016/j.cellsig.2014.09.010
S7146 DMH1 DMH1 is a selective BMP receptor inhibitor with IC50 of 107.9 nM for ALK2, exhibiting no inhibition on AMPK, ALK5, KDR (VEGFR-2) or PDGFR.
S7147 LDN-212854 LDN-212854 is a potent and selective BMP receptor inhibitor with IC50 of 1.3 nM for ALK2, about 2-, 66-, 1641-, and 7135-fold selectivity over ALK1, ALK3, ALK4, and ALK5, respectively.
S7148 ML347 ML347 is a selective BMP receptor inhibitor with IC50 of 32 nM for ALK2, >300-fold selectivity over ALK3. Also inhibits ALK1 activity with IC50 of 46 nM.
S7507 LDN-193189 HCl LDN193189 HCl is the hydrochloride salt of LDN193189, which is a selective BMP signaling inhibitor, and inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively, 200-fold selectivity for BMP versus TGF-β.
  • Proc Natl Acad Sci U S A, 2013, 110(52):E5039-48
S7359 K02288 K02288 is a potent, and selective type I BMP receptor inhibitor with IC50 of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA.
S2186 SB505124 SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5 with IC50 of 129 nM and 47 nM, respectively, also inhibits ALK7, but does not inhibit ALK1, 2, 3, or 6.
S2907 Pirfenidone Pirfenidone is an inhibitor for TGF-β production and TGF-β stimulated collagen production, reduces production of TNF-α and IL-1β, and also has anti-fibrotic and anti-inflammatory properties. Phase 3.
  • Histochem Cell Biol, 2014, 10.1007/s00418-014-1223-0
S7223 RepSox RepSox is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation, respectively.
S2308 Hesperetin Hesperetin is a bioflavonoid and, to be more specific, a flavanone.
S2750 GW788388 GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, also inhibits TGF-β type II receptor and activin type II receptor activities, but does not inhibit BMP type II receptor.
S2805 LY364947 LY364947 is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, shows 7-fold selectivity over TGFβR-II.
  • Chem Biol Interact, 2014, 217:1-8
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