TGF-β/Smad

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  1. ROCK inhibitor

    Y-33075 dihydrochloride is a selective ROCK inhibitor with an IC50 of 3.6 nM.
  2. TGFβR-I Inhibitor

    LY364947 is a diheteroaryl-substituted pyrazole compound used as a selective, ATP-competitive inhibitor of TGF-βRI (TGF-β Receptor I kinase).
  3. PKA, PKG, Casein Kinase I and II inhibitor

    A-3 Hydrochloride is an inhibitor of PKA (cAMP-dependent protein kinase, Ki=4.3μM) and cGMP-dependent protein kinase, Ki=3.8μM, PKC (protein kinase C, Ki=47μM), casein kinase I and II, and MLCK (myosin light chain kinase) ( Ki=7.4μM).
  4. MAPKAP-K2 (MK-2) inhibitor

    MK-2 Inhibitor III (compound 16) is an orally active, selective, and ATP-competitive MAPKAP-K2 (MK-2) inhibitor with an IC50 of 0.85 nM.
  5. ROCK inhibitor

    Glycyl-H 1152 2HCl is a selective and potent ROCK inhibitor (IC50 values are 0.0118, 2.35, 2.57, 3.26, > 10 and >10 uM for ROCKII, Aurora A, CAMKII, PKG, PKA and PKC respectively.)
  6. PKC activator

    Prostratin is a protein kinase C activator found in the bark of the mamala tree of Samoa, Homalanthus nutans.
  7. ROCK Inhibitor

    HA-1077 inhibits vascular smooth muscle contraction by acting as an intracellular Ca2+ antagonist.
  8. TGF-βR Inhibitor

    SD-208 is a potent, orally active ATP-competitive transforming growth factor-β receptor 1 (TGF-βRI) inhibitor (IC50= 49 nM); displays > 100-fold and > 17-fold selectivity over TGF-βRII and other common kinases respectively.
  9. TGF-beta receptor inhibitor

    N/A
  10. BMP receptor inhibitor

    ML347 is a selective BMP receptor inhibitor .
  11. eEF-2 inhibitor

    NH125 is a selective eEF-2 kinase inhibitor.
  12. BMP inhibitor

    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.
  13. Valrubicin is a semisynthetic derivative of the antineoplastic anthracycline antibiotic doxorubicin.
  14. ALK5 inhibitor

    A 77-01 is a potent inhibitor of TGF-β type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM.
  15. PKs inhibitor

    HA-100 is an isoquinoline compound with an added piperazinylsulfonyl group that acts as an inhibitor of protein kinases (PKs), including PKA, PKC, and PKG (IC50 = 8, 12, and 4 μM, respectively).
  16. TGFβRI inhibitor

    BIBF0775 is an inhibitor of the transforming growth factor β receptor I (TGFβRI).
  17. protein kinase A activator

    8-Bromo-cAMP is a cell perbeable cyclic AMP (cAMP) analog and a PKA activator.
  18. ROCK inhibitor

    SAR407899 is a potent and selective Rho kinase inhibitor with promising antihypertensive activity.
  19. PKA inhibitor

    KT 5720 is prepared by a modificiation of K-252a (sc-200517), which is synthesized by the fungus Nocardiopsis sp.
  20. PKA-selective activator

    6-Bnz-cAMP is a PKA-selective activator. It regulates the PKA dependent signaling pathways.
  21. reversible PKA inhibitor

    Rp-cAMPS is a cell-permeable and reversible inhibitor of PKA (protein kinase A) (Ki = 11 uM). Rp-cAMPS is resistant to hydrolysis by phosphodiesterases and is noncompetitive with respect to ATP.
  22. PKG/PKA inhibitor

    cGMP Dependent Kinase Inhibitor Peptid is a specific cGKI (cyclic GMP-dependent protein kinase) inhibitor. Data indicates that it does not block cyclic GMP-dependent protein kinase phosphorylation of intact histones and has been used to study Plasmodium falciparum.
  23. TGF-β inhibitor

    (+)-ITD-1 is a resolved enantiomer of ITD-1 that possesses a greater than 2-fold increase in TGF-β inhibition (~400 nM) and 1.3-fold increase in cardiogenesis compared to the racemic ITD-1.
  24. ALK2 inhibitor

    LDN-214117 is a selective and potent ALK2 inhibitor. LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM.
  25. GRK2/5 inhibitor

    CCG215022 is a potent GRK2 and GRK5 inhibitor. CCG215022 exhibited nanomolar IC50 values against both GRK2 and GRK5 and good selectivity against other closely related kinases such as GRK1 and PKA.
  26. ALK5 inhibitor

    R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
  27. Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNA gyrase, also can inhibit SMAD-3 phosphorylation, inhibit H+ K+-ATPase activity.
  28. TGF-beta agonist

    SRI-011381 hydrochloride is a TGF-beta signaling agonist.
  29. PKC inhibitor

    PKC-IN-1 is a poent PKC beta II inhibitor with Ki of 14.9 nM; compound example H6 from patent WO 2008096260 A1.
  30. PKC inhibitor

    NSC305787 is a small molecule inhibitor of PKC, with IC50 of 8.3 uM, 9.4 uM, 55 uM for PKC phosphorylation of recombinant ezrin, of moesin, and of radixin.
  31. Synaptamide is a potent mediator for neurogenic differentiation of NSCs acting through PKA/CREB activation.
  32. Cetrimonium bromide is an amine based cationic quaternary surfactant, is one of the components of the topical antiseptic Cetrimide.
  33. PKCβ1 and PKCβ2 inhibitor

    LY333531 is a β-specific protein kinase C inhibitor. It competitively and reversibly inhibits PKCβ1 and PKCβ2 with IC50 values of 4.7 and 5.9 nM respectively.
  34. TGFβRI inhibitor

    LY 3200882 is a potent, highly selective inhibitor of TGF-β receptor type 1 (TGFβRI). It potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells and in vivo in subcutaneous tumors in a dose dependent fashion.
  35. ROCK and MRCK inhibitor

    BDP5290 is a potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.
  36. protein kinase A inhibitor

    Warangalone is a prenylated isoflavone from the insecticidal plant Derris scandens that acts as a powerful inhibitor of protein kinase A.
  37. PKCθ selective inhibitor

    AS2521780 is a novel PKCθ selective inhibitor with an IC50 of 0.48 nM.
  38. Ionomycin (SQ23377) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus.
  39. ROCK inhibitor

    Fasudil (HA-1077; AT877), is a nonspecific ROCK inhibitor and also has inhibitory effect on protein kinases.
  40. MAPKAPK2(MK2) inhibitor

    MK2-IN-1 hydrochloride is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode.
  41. PKC inhibitor

    Ro 31-8220 is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively.
  42. BMP type I receptor inhibitor

    LDN193189 Tetrahydrochloride is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50??500 nM).
  43. PKC inhibitor

    Bisindolylmaleimide X hydrochloride (BIM-X hydrochloride) is a potent and selective protein kinase C (PKC) inhibitor.
  44. PKs inhibitor

    HA-100 is an isoquinoline compound with an added piperazinylsulfonyl group that acts as an inhibitor of protein kinases (PKs), including PKA, PKC, and PKG (IC50s = 8, 12, and 4 ?M, respectively).
  45. BMP signaling inhibitor

    LDN193189 HCl (DM-3189) 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 in C2C12 cell lines, respectively, 200-fold selectivity for BMP versus TGF-β.
  46. PKC activating agent

    Decursinol angelate, a cytotoxic and protein kinase C (PKC) activating agent from the root of Angelica gigas, possesses anti-tumor and anti-inflammatory activities.
  47. MRTF pathway inhibitor

    CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression.
  48. BMP4 signaling agonist

    BMP signaling agonist sb4 is a potent benzoxazole bone morphogenetic protein 4 (BMP4) signaling agonist with a EC50 value of 74 nM, activates BMP signaling by stabilizing intracellular p-SMAD-1/5/9.
  49. PKC inhibitor

    Iso-H7 dihydrochloride is an inhibitor of phosphokinase C.
  50. GRK2 inhibitor

    GSK180736A is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.

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