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TGF-β / Smad Signaling

  1. Cat.No. Product Name Information
  2. A8464 LY2109761 LY2109761 is a small-molecule inhibitor selectively targeting both TGF-β receptor type I and II ((TβRI/II)) with Ki of 38 nM and 300 nM, respectively . It gave IC50 value of 69 nM in TβRI enzymatic assay . Crystal structure showed the binding of LY2109761 to the ATP binding site of the TGF-β R1 kinase domain . Weak inhibitory activities were reported for other kinases, including Lck, Sapk2α, MKK6, Fyn, and JNK3 (18–89% inhibition at 20 µM) .
  3. A8345 PF-562271 HCl PF-562271 is a potent, ATP-competitive and reversible inhibitor of both focal adhesion kinase (FAK), a non-receptor tyrosine kinase involved in a variety of cellular events, and proline-rich tyrosine kinase 2 (Pyk2), an FAK homolog containing 48% amino acid identity, with half maximal inhibitory concentration (IC50) of 1.5 nmol/L and 14 nmol/L respectively. As a potential therapeutic agent either alone or in combination with other agents for the treatment of cancer, PF-562271 has been reported to effectively inhibit the proliferation of tumors in both xenograft and transgenic mouse models, in which it dose-dependently inhibits FAK phosphorylation in tumor-bearing mice with half maximal effective concentration (EC50) of 93 ng/mL.
  4. A8324 LDN-193189 LDN193189 is a selective transcriptional activity morphogenetic protein (BMP) type I receptors inhibitor. It inhibits activin receptor-like kinase-2 (ALK2) and ALK3 with IC50 values of 5 nM and 30 nM, respectively .
  5. A8310 PF-562271

    PF-562271 is a potent, ATP-competitive and reversible inhibitor of both focal adhesion kinase (FAK), a non-receptor tyrosine kinase involved in a variety of cellular events, and proline-rich tyrosine kinase 2 (Pyk2), an FAK homolog containing 48% amino acid identity, with half maximal inhibitory concentration (IC50) of 1.5 nmol/L and 14 nmol/L respectively. As a potential therapeutic agent either alone or in combination with other agents for the treatment of cancer, PF-562271 has been reported to effectively inhibit the proliferation of tumors in both xenograft and transgenic mouse models, in which it dose-dependently inhibits FAK phosphorylation in tumor-bearing mice with half maximal effective concentration (EC50) of 93 ng/mL.

  6. A8301 GW788388 GW788388 is a potent selective inhibitor of TGF-beta type I receptor [activin receptor-like kinase 5 (ALK5)].
  7. A5734 Fasudil (HA-1077) HCl Cyclic nucleotide-dependent protein kinase inhibitor and Rho-associated kinase inhibitor (IC50 = 10.7 μM).
  8. A5611 GSK429286A Selective Rho-kinase inhibitor (IC50 values are 14, 780 and 1940 nM for ROCK1, RSK and p70S6K respectively).
  9. A5467 Ponatinib (AP24534) Potent multi-kinase and pan-BCR-ABL inhibitor.
  10. A5506 Thiazovivin Greatly enhances the efficiency of fibroblast reprogramming to generate induced pluripotent stem cells (iPSCs) when used in combination with SB 431542 and PD 0325901.
  11. A2133 Saracatinib (AZD0530) Saracatinib (AZD0530) is a novel, potent Src family kinase (SFK)/Abl dual-kinase inhibitor with IC50 value of 2.7 nM .

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