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TGF-βR1 (transforming growth factor beta receptors) are a serine/threonine protein kinase that involved in the regulation of cell cycle arrest, cell proliferation and differentiation, production of extracellular matrix, wound healing, tumorgenesis and immunosuppression etc.

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  1. Cat.No. Product Name Information
  2. B3687 LDN-212854 LDN-212854 is a selective inhibitor of bone morphogenetic protein (BMP) signaling with IC50 value of 1.2nM .
  3. 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) .
  4. A8301 GW788388 GW788388 is a potent selective inhibitor of TGF-beta type I receptor [activin receptor-like kinase 5 (ALK5)].
  5. A3808 SD-208 SD-208 inhibits the growth inhibition of TGF-β–sensitive CCL64 cells at an EC50 of 0.1 μmol/L
  6. A3133 A 83-01 A 83-01 is a small-molecule inhibitor of activin receptorlike kinase (ALK)-5 with IC50 value of 12 nM.
  7. A3132 A 77-01 Transforming growth factor (TGF)-β signaling facilitates tumor growth and metastasis in advanced cancer.
  8. C3656 ALK5 Inhibitor II (hydrochloride)
  9. A8348 LY2157299 LY2157299 is a potent small-molecule antagonist that specifically inhibits Transforming Growth Factor-β receptor I (TβRI).
  10. A5602 SB525334 SB525334 is a potent inhibitor of transforming growth factor-beta1 (TGF-beta1) receptor, activin receptor-like kinase (ALK5). It specifically inhibits ALK5 with IC50 value of 14.3nM, which shows 4-fold higher potency against ALK4 .
  11. A8249 SB 431542

    SB431542 is a selective ATP-competitive inhibitor of ALK5 (activin receptor-like kinase 5) with an IC50 value of 94 nM .

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