TGF-beta/Smad

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TGF-beta/Smad Inhibitors | Activators (20)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1067 SB431542 SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM in a cell-free assay, 100-fold more selective for ALK5 than p38 MAPK and other kinases.
  • J Clin Invest, 2015, 125(2):796-808
  • Genes Dev, 2014, 28(8):858-74
  • Cell Mole Bioeng, 2014, 10.1007/s12195-014-0333-z
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 in C2C12 cells, respectively, exhibits 200-fold selectivity for BMP versus TGF-β.
  • Cancer Cell, 2014, 26(4):521-33
  • J Clin Invest, 2015, 125(2):796-808
  • Stem Cells, 2015, 33(5):1447-55
S2230 Galunisertib (LY2157299) Galunisertib (LY2157299) is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM in a cell-free assay. Phase 2/3.
  • Cancer Res, 2014, 74(21):5963-77
  • Lab Chip, 2013, 13(10):1969-78
  • Mol Cell Endocrinol, 2015, 10.1016/j.mce.2015.03.012
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 in cell-free assay, 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 in a cell-free assay, 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, 26(12):3027-35
S7627 LDN-214117 LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM.
S7624 SD-208 SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.
S7530 EW-7197 EW-7197 is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. Phase 1.
S7658 Kartogenin Kartogenin is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.
S2186 SB505124 SB505124 is a selective inhibitor of TGFβR for ALK4, ALK5 with IC50 of 129 nM and 47 nM in cell-free assays, 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
  • Biochem Biophys Res Commun, 2015, 10.1016/j.bbrc.2015.04.107
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
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 in cell-free assays, respectively.
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.
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 in a cell-free assay, 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 in a cell-free assay, shows 7-fold selectivity over TGFβR-II.
  • Chem Biol Interact, 2014, 217:1-8

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1067 SB431542 <1 mg/mL 77 mg/mL 3 mg/mL
S2618 LDN-193189 0.01 mg/mL 0.01 mg/mL <1 mg/mL
S2230 Galunisertib (LY2157299) <1 mg/mL 74 mg/mL <1 mg/mL
S2704 LY2109761 <1 mg/mL 2 mg/mL <1 mg/mL
S1476 SB525334 <1 mg/mL 68 mg/mL 68 mg/mL
S7627 LDN-214117 <1 mg/mL 83 mg/mL 83 mg/mL
S7624 SD-208 <1 mg/mL 9 mg/mL <1 mg/mL
S7530 EW-7197 <1 mg/mL 79 mg/mL 43 mg/mL
S7658 Kartogenin <1 mg/mL 63 mg/mL 18 mg/mL
S2186 SB505124 <1 mg/mL 67 mg/mL 67 mg/mL
S2907 Pirfenidone <1 mg/mL 37 mg/mL 37 mg/mL
S7146 DMH1 <1 mg/mL 25 mg/mL <1 mg/mL
S7147 LDN-212854 <1 mg/mL 81 mg/mL <1 mg/mL
S7148 ML347 <1 mg/mL 10 mg/mL <1 mg/mL
S7507 LDN-193189 HCl 52 mg/mL <1 mg/mL <1 mg/mL
S7223 RepSox <1 mg/mL 57 mg/mL <1 mg/mL
S7359 K02288 <1 mg/mL 70 mg/mL <1 mg/mL
S2308 Hesperetin <1 mg/mL 60 mg/mL <1 mg/mL
S2750 GW788388 <1 mg/mL 15 mg/mL <1 mg/mL
S2805 LY364947 <1 mg/mL 1 mg/mL <1 mg/mL
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