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
- GC13890 (±)-Palmitoylcarnitine chloride intermediate in mitochondrial fatty acid oxidation
- GC10603 (-)-epicatechin gallate major catechin in green tea
- GC17242 (-)-epigallocatechin green tea epicatechin
- GC14049 (-)-Epigallocatechin gallate (EGCG) (-)-Epigallocatechin Gallate sulfate (EGCG) is a major polyphenol in green tea that inhibits cell proliferation and induces apoptosis. In addition, it inhibits the activity of glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) ..
- GC14012 (-)-Indolactam V A protein kinase C activator
- GC18062 1,2-Dilauroyl-sn-glycerol A longchain DAG
- GC14134 1,2-Dimyristoyl-sn-glycerol A longchain DAG
-
GC13877
1,2-Dipalmitoyl-sn-glycerol
weak activator of PKC
- GC12662 1,2-Distearoyl-sn-glycerol A diacylglycerol
- GC12172 1-Naphthyl PP1 Src family kinases inhibitor
- GC41863 10,11-dehydro Curvularin A natural mycotoxin
-
GN10444
12-O-tetradecanoyl phorbol-13-acetate
A PKC activator
- GC13927 A 77-01 A potent ALK5 inhibitor
- GC10166 A 83-01 A TGF-β type I receptor inhibitor
- GC35210 A 83-01 sodium salt A potent inhibitor of TGF-β type I receptor ALK5 kinase
- GC60037 A-3 hydrochloride A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases.
- GC15579 Adaphostin P210bcr/abl tyrosine kinase inhibitor
- GC16475 Afuresertib pan-AKT inhibitor
- GC42747 Afuresertib (hydrochloride) Afuresertib is a selective, orally bioavailable inhibitor of Akt1, 2, and 3 with Ki values of 0.08, 2, and 2.6 nM, respectively.
- GC65294 ALK2-IN-2 ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, and over 700-fold selectivity against ALK3.
- GC11050 ALK5 Inhibitor II (hydrochloride) ALK5 inhibitor
- GC34300 AR-13324 analog mesylate
-
GC19034
AR-13324 mesylate
AR-13324 is a potent inhibitor of ROCK I and ROCK II that has been shown to induce morphologic changes in cultured human and porcine TM cells at low concentration.
- GC31959 AS2521780 AS2521780 is a novel PKCθ selective inhibitor with an IC50 of 0.48 nM.
- GC32703 Asciminib (ABL001) Asciminib (ABL001) (ABL001) is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.
- GC64462 Asciminib hydrochloride Asciminib (ABL001) hydrochloride is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.
- GN10534 Asiaticoside
- GC17712 AT13148 Multi-AGC kinase inhibitor,ATP-competitive
- GC64815 Aurothiomalate sodium Aurothiomalate sodium is a potent and selective oncogenic PKCι signaling inhibitor.
- GC50589 AZ 12799734 Potent TGF-βRI inhibitor
- GC35442 Azaindole 1 Azaindole 1 (Azaindole 1; TC-S 7001) is an orally active and ATP-competitive ROCK inhibitor with IC50s of 0.6 and 1.1nM for human ROCK-1 and ROCK-2, respectively.
-
GC35462
Bafetinib
Bcr-Abl/Lyn tyrosine kinase inhibitor
- GC33343 BCR-ABL-IN-1 BCR-ABL-IN-1 is an inhibitor of BCR-ABL tyrosine kinase, with a pIC50 of 6.46, and may be used in the research of chronic myelogenous leukemia.
- GC33368 BCR-ABL-IN-2 BCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC50s of 57 nM, 773 nm for ABL1native and ABL1T315I, respectively.
-
GC32868
BDP5290
BDP5290 is a potent inhibitor of ROCK and MRCK with IC50 values of 17nM, 230nM, 123nM and 100nM for MRCKβ, ROCK1, ROCK2, respectively .
- GC34493 BIBF0775 BIBF0775 is a potent and selective transforming growth factor β (TGFβ) type I receptor (Alk5) inhibitor with an IC50 of 34 nM.
- GC62868 BIO-013077-01 BIO-013077-01 is a pyrazole TGF-β inhibitor.
- GC12135 Bisindolylmaleimide II protein kinase C (PKC) inhibitor
- GC14716 Bisindolylmaleimide IV protein kinase C (PKC) inhibitor
- GC17239 Bisindolylmaleimide V negative control for protein kinase C (PKC)-inhibitory activity
- GC13226 Bisindolylmaleimide VIII (acetate) A protein kinase C (PKC) inhibitor
- GC18354 Bisindolylmaleimide X (hydrochloride) Bisindolylmaleimide X is a cell-permeable, reversible, ATP-competitive protein kinase C (PKC) inhibitor (IC50 = 15 nM, rat brain PKC).
- GC35530 BJE6-106 BJE6-106 (B106) is a potent, selective 3rd generation PKCδ inhibitor with an IC50 of 0.05 μM and targets selectivity over classical PKC isozyme PKCα (IC50=50 μM).
-
GC50593
BMP signaling agonist sb4
Potent BMP4 agonist
- GC13343 Bosutinib (SKI-606) Bosutinib (SKI-606) is an oral Src/Abl tyrosine kinase inhibito with IC50 of 1.2 nM and 1 nM, respectively.
- GC40080 Bosutinib-d8 Bosutinib-d8 is intended for use as an internal standard for the quantification of bosutinib by GC- or LC-MS.
- GC17670 Bryostatin 1 PKC activator
- GC12842 Bryostatin 2 Protein kinase C (PKC) activator
- GC12695 Bryostatin 3 protein kinase C activator
- GC16539 Butaprost A selective agonist for the EP2 receptors
- GC11605 C-1 C-1 is a potent protein kinase inhibitor, with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. C-1 also used as a ROCK inhibitor.
- GC43105 C8 Ceramide (d18:1.8:0) C8 Ceramide (d18:1.8:0) (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides.
-
GC11159
Calphostin C
protein kinase C inhibitor
- GC62612 CC-90005 CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM.
- GC38898 CCG-222740 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. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis.
- GC35651 Cenisertib Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.
- GC18521 Cercosporin Cercosporin is a pigmented phytotoxin isolated from the fungus C.
- GC10687 CGP 53353 PKCβII inhibitor
- GC14650 CGP60474 A CDK inhibitor
- GC32250 Chebulinic acid An ellagitannin with diverse biological activities
- GN10463 Chelerythrine
- GC13065 Chelerythrine Chloride Potent inhibitor of PKC and Bcl-xL
- GC35682 CHMFL-ABL/KIT-155 CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM) and PDGFRβ (IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis.
- GC43286 CMPD101 A GRK2 and GRK3 inhibitor
- GC50704 CRT 0066854 hydrochloride CRT 0066854 hydrochloride is a potent and selective atypical PKCs inhibitor.
- GC45414 CRT0066854
- GC35753 CT-721 CT-721 is a potent and time-dependent Bcr-Abl kinase inhibitor with an IC50 of 21.3 nM for wild-type Bcr-Abl kinase, and possesses anti-chronic myeloid leukemia (CML) activities.
- GC33351 CZC-8004 (CZC-00008004) CZC-8004 (CZC-00008004) (CZC-00008004), an aminopyrimidine, is a pan-kinase inhibitor. CZC-8004 (CZC-00008004) can bind a range of tyrosine kinases, including EGFR and VEGFR2 with IC50 values of 650 and 437 nM, respectively.
- GC17591 D-erythro-Sphingosine (synthetic) D-erythro-Sphingosine (synthetic) (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (synthetic) (Erythrosphingosine) is also a PP2A activator.
- GN10336 Daphnetin
- GC38186 Daphnoretin A coumarin with diverse biological activities
- GC35812 Dasatinib hydrochloride A potent and dual AblWT/Src inhibitor
- GC15884 Dasatinib Monohydrate Inhibitor of ABL, SRC, KIT, PDGFR, and other tyrosine kinases.
- GC14007 DCC-2036 (Rebastinib) DCC-2036 (Rebastinib) (DCC-2036) is an orally active, non-ATP-competitiveBcr-Abl inhibitor for Abl1WT and Abl1T315I with IC50s of 0.8 nM and 4 nM, respectively. DCC-2036 (Rebastinib) also inhibits SRC, KDR, FLT3, and Tie-2, and has low activity to seen towards c-Kit.
- GC38388 DCPLA-ME DCPLA-ME, the methyl ester form of DCPLA, is a potent PKCε activator for use in the treatment of neurodegenerative diseases.
- GC31892 Decursin ((+)-Decursin) Decursin ((+)-Decursin) ((+)-Decursin ((+)-Decursin)) is a potent anti-tumor agent.
- GC38085 Decursinol angelate Decursinol angelate, a cytotoxic and protein kinase C (PKC) activating agent from the root of Angelica gigas, possesses anti-tumor and anti-inflammatory activities.
- GC16354 Dequalinium Chloride anti-tumor agent and PKC inhibitor
- GC38482 Desmethylglycitein Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities.Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1). Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes.
- GC17767 Dihydrosphingosine Dihydrosphingosine is a potent inhibitor of PKC and phospholipase A2 (PLA2).
- GC34060 Disitertide (P144) Disitertide (P144) (P144) is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) (P144) is also a PI3K inhibitor and an apoptosis inducer.
- GC68333 Disitertide diammonium
- GC60782 Disitertide TFA Disitertide (P144) TFA is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) TFA is also a PI3K inhibitor and an apoptosis inducer.
- GC14298 DMH-1 Selective BMP ALK2 receptor
- GC17243 Dorsomorphin (Compound C) Dorsomorphin (Compound C) (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (Compound C) (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin (Compound C) induces autophagy.
- GC12560 Dorsomorphin (Compound C) 2HCl Dorsomorphin (Compound C) 2HCl (BML-275 dihydrochloride; Compound C dihydrochloride) is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin (Compound C) 2HCl inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin (Compound C) 2HCl induces autophagy.
- GC35897 DPH A potent cell permeable c-Abl activator
- GC32914 EMT inhibitor-1 EMT inhibitor-1 is an inhibitor of of Hippo, TGF-β, and Wnt signaling pathways with antitumor activities.
- GC11499 Enzastaurin (LY317615) Enzastaurin (LY317615) (LY317615) is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε.
- GC65329 EW-7195 EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung.
- GC13354 EW-7197 EW-7197 (EW-7197) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. EW-7197 also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. EW-7197 has potently antimetastatic activity and anticancer effect.
- GC13869 Fasudil Calcium antagonist
- GC14289 Fasudil (HA-1077) HCl Fasudil (HA-1077; AT877) Hydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil (HA-1077) HCl is also a potent Ca2+ channel antagonist and vasodilator.
- GC32867 Flumatinib (HHGV678) Flumatinib (HHGV678) (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib (HHGV678) inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively.
- GC13914 Flumatinib mesylate PDGRFβ inhibitor
- GC12027 FR 236924 FR 236924 (FR236924), a linoleic acid derivative, selectively and directly activates PKCε.
- GC65539 Fresolimumab Fresolimumab (GC1008) is a high-affinity fully human monoclonal antibody that neutralizes the active form of human TGFβ1, TGFβ2, and TGFβ3.
- GC15431 GF 109203X (Bisindolylmaleimide I) GF 109203X (GF109203X) is a highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor with a Ki of 14 nM.
- GC36167 GMB-475 GMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.
- GC10858 GNF 2 Bcr-Abl inhibitor