TGF-β / Smad Signaling
Transforming growth factor-beta (TGF-beta) is a multifunctional cytokine that regulates proliferation, migration, differentiation, and survival of many different cell types. Deletion or mutation of different members of the TGF-β family have been shown to cause vascular remodeling defect and absence of mural cell formation, leading to embryonic lethality or severe vascular disorders. TGF-β induces smooth muscle differentiation via Notch or SMAD2 and SMAD3 signaling in ES cells or in a neural crest stem cell line. TGF-β binds to TGF-βRI and to induce phosphorylation of SMAD2/3, thereby inhibiting proliferation, tube formation, and migration of endothelial cells (ECs).
TGF-β is a pluripotent cytokine with dual tumour-suppressive and tumour-promoting effects. TGF-β induces the epithelial-to-mesenchymal transition (EMT) leading to increased cell plasticity at the onset of cancer cell invasion and metastasis.
Targets for TGF-β / Smad Signaling
Products for TGF-β / Smad Signaling
- Cat.No. Product Name Information
- GC44729 Prostratin An HIV reactivator
- GC37014 Protein Kinase C 19-31 Protein Kinase C 19-31, a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate peptide for testing the protein kinase C activity.
- GC37015 Protein Kinase C 19-36 Protein Kinase C 19-36 is a pseudosubstrate peptide inhibitor of protein kinase C (PKC), with an IC50 of 0.18 μM.
- GC66006 Protein kinase inhibitor H-7 Protein kinase inhibitor H-7 is a potent inhibitor of protein kinase C (PKC) and cyclic nucleotide dependent protein kinase, with a Ki of 6 μM for PKC.
- GC11803 Pseudo RACK1 Activator of protein kinase C
-
GC69776
PT-262
PT-262 is an effective ROCK inhibitor with an IC50 value of approximately 5 μM. PT-262 induces loss of mitochondrial membrane potential and increases activation of caspase-3 and cell apoptosis. PT-262 inhibits phosphorylation of ERK and CDC2 through a p53-independent pathway. PT-262 blocks cellular cytoskeleton function and cell migration. PT-262 has anti-cancer activity.
- GC14583 R 59-022 Diacylglycerol (DAG) kinase inhibitor
-
GC69792
R 59-022 hydrochloride
R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 μM). R 59-022 hydrochloride inhibits OAG phosphorylation to OAPA. It is also a 5-HT receptor antagonist that can activate protein kinase C (PKC). R 59-022 enhances the production of thromboxane in platelets induced by thrombin and inhibits phosphatidic acid production in neutrophils.
- GC32840 R-268712 R-268712 is an orally active and selective ALK-5 inhibitor, with an IC50 of 2.5 nM.
-
GC18246
R-59-949
R-59-949 is an inhibitor of diacylglycerol kinase α (DGK-α) with an IC50 value of 300 nM in isolated platelet plasma membranes using exogenous diacylglycerol as a substrate.
- GC11140 Radotinib(IY-5511) Bcr-Abl tyrosine kinase inhibitor
- GC16793 RepSox A selective inhibitor of ALK5
- GC33310 Rho-Kinase-IN-1 Rho-Kinase-IN-1 is a Rho kinase (ROCK) inhibitor (Ki values of 30.5 and 3.9 nM for ROCK1 and ROCK2, respectively) extracted from US20090325960A1, compound 1.008.
- GC66050 Rho-Kinase-IN-2 Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and central nervous system (CNS)-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC50=3 nM). Rho-Kinase-IN-2 can be used in Huntington's research.
- GC37534 Ripasudil free base Ripasudil free base (K-115 free base) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.
- GC17322 Ro 31-8220 pan-PKC inhibitor
- GC17014 Ro 31-8220 Mesylate Pan-PKC inhibitor
- GC10029 Ro 31-8220 methanesulfonate Ro 31-8220 methanesulfonate 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.
- GC13677 Ro 32-0432 hydrochloride protein kinase C inhibitor
- GC37551 ROCK inhibitor-2 ROCK inhibitor-2 is a selective dual ROCK1 and ROCK2 inhibitor with IC50s of 17 nM and 2 nM, respectively.
- GC31952 ROCK-IN-1 ROCK-IN-1 is a potent inhibitor of ROCK, with an IC50 of 1.2 nM for ROCK2.
- GC66338 ROCK1-IN-1 ROCK1-IN-1 is a ROCK1 inhibitor with a Ki value of 540 nM. ROCK1-IN-1 can be used for the research of hypertension, glaucoma and erectile dysfunction.
- GC31883 ROCK2-IN-2 ROCK2-IN-2 is a selective ROCK2 inhibitor extracted from patent US20180093978A1, Compound A-30, has an IC50 of <1 μM.
- GC10820 Rottlerin PKC inhibitor
- GC63177 Ruboxistaurin Ruboxistaurin (LY333531) is an orally active, selective PKC beta inhibitor (Ki=2 nM).
- GC16405 Safingol PKC and sphingosine kinases inhibitor
- GC63439 Sangivamycin Sangivamycin (NSC 65346), a nucleoside analog, is a potent inhibitor of protein kinase C (PKC) with an Ki of 10 μM. Sangivamycin has potent antiproliferative activity against a variety of human cancers.
- GC13759 SAR407899 ATP-competitive ROCK inhibitor
- GC16289 SAR407899 hydrochloride ATP-competitive ROCK inhibitor
- GC15197 Saracatinib (AZD0530) Saracatinib (AZD0530) (AZD0530) is a potent Src family inhibitor with IC50s of 2.7 to 11 nM for c-Src, Lck, c-YES, Lyn, Fyn, Fgr, and Blk. Saracatinib (AZD0530) shows high selectivity over other tyrosine kinases.
- GC11022 SB 218078 checkpoint kinase 1 (Chk1) inhibitor
- GC11545 SB 431542 SB-431542, a small molecule inhibitor
- GC15170 SB 772077B dihydrochloride Rho-kinase (ROCK) inhibitor
- GC10421 SB-505124 hydrochloride Inhibitor of receptors ALK4, ALK5, and ALK7
- GC13769 SB505124 ALK4/ALK5/ALK7 inhibitor
- GC14349 SB525334 (TGF-beta1) receptor inhibitor
- GC13320 SC-10 Protein kinase C activator
- GC18055 SC-9 protein kinase C activator
- GC13904 SD-208 A potent, selective inhibitor of TGF-βRI
- GC17191 SIS3 HCl SIS3HCl is a potent and selective inhibitor of Smad3 with an IC50 of 3 μM for Smad3 phosphorylation.
-
GC69903
SJ000063181
SJ000063181 is an effective BMP signal activator with an EC50 ≤1 µM. It can be used as a chemical probe to explore BMP signaling because it can penetrate zebrafish embryos.
- GC32788 SJ000291942 A BMP signaling activator
-
GC19447
SM 16
SM 16 is a ALK5/ALK4 kinase inhibitor
- GC44903 SMAD3 Inhibitor, SIS3 SMAD3 Inhibitor, SIS3 is a potent and selective inhibitor of Smad3 phosphorylation.
- GC65592 SNIPER(ABL)-020 SNIPER(ABL)-020, conjugating Dasatinib (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein.
- GC15520 Sotrastaurin (AEB071) Sotrastaurin (AEB071) (AEB071) is a potent and orally-active pan-PKC inhibitor, with Kis of 0.22 nM, 0.64 nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively.
- GC10722 SR-3677 Rho Kinase (ROCK-II) inhibitor
- GC19338 SRI-011381 hydrochloride An oral bioavailabile TGF-beta signaling agonist
-
GC15299
Staurosporine(CGP 41251)
A potent inhibitor of protein kinase C
-
GC69981
SY-LB-35
SY-LB-35 is an effective bone morphogenetic protein (BMP) receptor agonist. It can stimulate C2C12 cells to significantly increase cell number and cell vitality, causing the cell cycle to transition into S phase and G2/M phase. SY-LB-35 stimulates typical Smad and atypical PI3K/Akt, ERK, p38, and JNK intracellular signaling pathways.
- GC16821 TAE226(NVP-TAE226) TAE226(NVP-TAE226) (TAE226) is a potent and ATP-competitive dual FAK and IGF-1R inhibitor with IC50s of 5.5 nM and 140 nM, respectively.
- GC17901 Tamoxifen Tamoxifen(TAM) serves as a selective estrogen receptor regulator (SERM), inhibiting estrogen's effects in breast cells while potentially stimulating estrogen activity in cells found in different tissues.
-
GC10682
TAS 301
inhibitor of smooth muscle cell migration and proliferation, inhibits PKC signaling
- GC11181 Thiazovivin ROCK inhibitor
- GC26000 TP0427736 HCl TP0427736 is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50 = 836 nM for ALK3). It also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM.
-
GC70050
Trabedersen
Trabedersen (AP 12009) is an antisense oligodeoxynucleotide that specifically inhibits TGF-β2 (TGF-beta/Smad). Trabedersen can be used to study malignant brain tumors and other solid tumors that overexpress TGF-β2, such as skin, pancreatic, and colon tumors.
- GC40928 Trimethylamine N-oxide Trimethylamine N-oxide (TMAO) is a product of the oxidation of TMA by flavin-containing mono-oxygenase 3 in the liver.
- GC16678 UCN-02 protein kinase C inhibitor
- GC37880 Vactosertib Hydrochloride Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib Hydrochloride has potently antimetastatic activity and anticancer effect.
- GC16934 Valrubicin chemotherapy drug used to treat bladder cancer
-
GC70110
Vamotinib
Vamotinib (PF-114) is an effective, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the self-phosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis. Vamotinib exhibits anti-proliferative and anti-tumor activity. Vamotinib has potential in the study of resistant Philadelphia chromosome-positive (Ph+) leukemia.
- GC13232 Verbascoside PKC/NF-κB inhibitor
- GC31912 VTX-27 VTX-27 is a selective protein kinase C θ (PKC θ) inhibitor, with Kis of 0.08 nM and 16 nM for PKC θ and PKC δ.
- GC26055 WAY-301398 WAY-301398 (6-methoxynaphthalene) can bind to protein kinase C (PKC).
- GC26065 WAY-354831 WAY-354831 exhibits antibacterial activity.
- GC10970 WP1130 WP1130 (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. WP1130 has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2.
- GC62146 XST-14 XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC50 of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects.
-
GC15712
Y-27632
A ROCK inhibitor,potent and selective
- GC37947 Y-33075 Y-33075 is a selective ROCK inhibitor derived from Y-27632, and is more potent than Y-27632, with an IC50 of 3.6 nM.
- GC13423 Y-39983 dihydrochloride ROCK family inhibitor
-
GC70166
Z-Arg-SBzl
Z-Arg-SBzl is a substrate for activating protein C in both cows and humans.
- GC33120 ZINC00881524 A ROCK inhibitor
- GC13273 ZIP ZIP is a selective peptide inhibitor of PKMζ.
- GC13461 ZIP (SCRAMBLED) PKMζ inhibitor
- GC16510 ZIP, Biotinylated ZIP with a biotin moiety covalently attached
- GC14701 Zoledronic Acid Potent nitrogen-containing bisphosphonates
- GC17727 [Ala107]-MBP (104-118) Non-competitive inhibitor of PKC
- GC15345 [Ala113]-MBP (104-118) Non-competitive inhibitor of PKC
- GC10343 α-Amyloid Precursor Protein Modulator α-Amyloid Precursor Protein Modulator is a cell-permeable benzolactam-derived protein kinase C (PKC) activator with a Ki of 11.9 nM.
- GC62478 ζ-Stat ζ-Stat (NSC37044) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro.