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
- GC15079 GNF 5 Bcr-Abl inhibitor
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GC10607
GNF-7
Type II Bcr-Abl inhibitor
- GC15564 Go 6976 PKCα/PKCβ1 inhibitor
- GC16907 Go 6983 Go 6983 (GÖ 6983) is one of the bisindolylmaleimide group of PKC inhibitor compounds, Go 6983 (GÖ 6983) was able to differentiate between PKC mu and other PKC isoenzymes.
- GC38791 GSK-25 GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM).
- GC19177 GSK180736A GSK180736A is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 uM.
- GC17936 GSK269962A ROCK inhibitor
- GC25482 GSK269962A HCl GSK269962A HCl (GSK269962B, GSK269962) is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.
- GC18119 GSK429286A Selective ROCK1/ROCK2 inhibitor
- GC11878 GW788388 ALK5 inhibitor,potent and selective
- GC10915 GZD824 Olverembatinib (GZD824) dimesylate is a potent and orally active pan-Bcr-Abl inhibitor. GZD824 potently inhibits a broad spectrum of Bcr-Abl mutants. GZD824 strongly inhibits native Bcr-Abl and Bcr-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. GZD824 has antitumor activity.
- GC33201 GZD856 GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-AblT315I inhibitor, with IC50s of 19.9 and 15.4?nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity.
- GC36207 H-1152 H-1152 is a membrane-permeable and selective ROCK inhibitor, with a Ki value of 1.6 nM, and an IC50 value of 12 nM for ROCK2.
- GC36208 H-1152 dihydrochloride H-1152 dihydrochloride is a membrane-permeable and selective ROCK inhibitor, with a Ki value of 1.6 nM, and an IC50 value of 12 nM for ROCK2.
- GC31650 Halofuginone (RU-19110) Halofuginone (RU-19110) (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM.
- GC31950 Halofuginone hydrobromide (RU-19110 (hydrobromide)) Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM.
- GC10299 Hexadecyl Methyl Glycerol protein kinase C activity inhibitor
- GC15018 Hispidin protein kinase Cβ inhibitor
- GC64326 Hydrochlorothiazid-d2
- GC17523 Hydrochlorothiazide diuretic drug of the thiazide class
- GC36282 Hypocrellin A Hypocrellin A, a naturally occurring PKC inhibitor, has many biological and pharmacological properties, such as antitumour, antiviral, antibacterial, and antileishmanial activities.
- GC15420 ICP 103 Protein kinase inhibitor
- GC10314 Imatinib (STI571) Imatinib (STI571) (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib (STI571) also is an inhibitor of SARS-CoV and MERS-CoV.
- GC11759 Imatinib Mesylate (STI571) Imatinib Mesylate (STI571) (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.
- GC50317 IN 1130 Potent and selective inhibitor of TGF-βRI
- GC32870 Ingenol ((-)-Ingenol) Ingenol ((-)-Ingenol) is a PKC activator, with a Ki of 30 μM, with antitumor activity.
- GC61776 Ingenol 3,20-dibenzoate Ingenol 3,20-dibenzoate is a potent protein kinase C (PKC) isoform-selective agonist.
- GC31656 Ingenol Mebutate (Ingenol 3-angelate) Ingenol Mebutate (Ingenol 3-angelate) is an active ingredient in Euphorbia peplus, acts as a potent PKC modulator, with Kis of 0.3, 0.105, 0.162, 0.376, and 0.171 nM for PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε, respectively, and has antiinflammatory and antitumor activity.
-
GC15148
Ionomycin calcium salt
Lonomycin is a selective calcium ionophore derived from S. conglobatus that mobilizes intracellular calcium stores.
- GC15446 Ionomycin free acid Ionomycin free acid (SQ23377) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus.
- GC60210 Isosaponarin Isosaponarin is a flavone glycoside isolated from wasabi leaves.
- GC12108 ITD 1 First selective TGFβ inhibitor
- GC11362 K 252a A protein kinase inhibitor
- GC15281 K-252c Protein kinase inhibitor
- GC15567 K02288 ALK inhibitor
- GC43993 K252b K252b is an indolocarbazole isolated from the actinomycete Nocardiopsis, first described as an inhibitor of protein kinase C.
- GC15057 Kartogenin Promote differentiation of multipotent MSCs into chondrocytes
- GC64263 Kobophenol A Kobophenol A, an oligomeric stilbene, blocks the interaction between the ACE2 receptor and S1-RBD with an IC50 of 1.81 μM and inhibits SARS-CoV-2 viral infection in cells with an EC50 of 71.6 μM.
- GC17346 KT 5823 A protein kinase G inhibitor
- GC12817 K–115 hydrochloride dihydrate K-115 hydrochloride dihydrate (K-115) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.
- GC40770 L-erythro Sphingosine (d18:1) L-erythro Sphingosine is a synthetic stereoisomer of sphingosine (d18:1).
- GC17815 L-threo-Sphingosine C-18 L-threo-Sphingosine C-18 is a potent MAPK inhibitor. L-threo-Sphingosine C-18 induces apoptosis and clear DNA fragmentation. L-threo-Sphingosine C-18 shows anticancer effect.
- GC16580 LDN-193189 ALK inhibitor,potent and selective
- GC17035 LDN-212854 BMP receptor inhibitor,potent and selective
- GC13225 LDN-214117 potent and selective ALK2 inhibitor
- GC14931 LDN193189 Hydrochloride An inhibitor of BMP receptors ALK1, ALK2, ALK3, and ALK6
- GC36433 LDN193189 Tetrahydrochloride A selective BMP type I receptor inhibitor
- GC39398 LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA) LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier.
- GC32728 LSKL, Inhibitor of Thrombospondin TSP-1 LSKL, Inhibitor of Thrombospondin TSP-1 is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin TSP-1 inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin TSP-1 suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin TSP-1 can readily crosse the blood-brain barrier.
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GC69412
Luspatercept
Luspatercept (ACE-536) is a recombinant modified ActRIIB fusion protein that can bind to the ligands of the transforming growth factor β superfamily. Luspatercept increases red blood cell count and promotes maturation of red blood cell precursors. Luspatercept binds with GDF11, inhibiting the Smad2/3 signaling pathway. Luspatercept can be used for research on anemia.
- GC12402 LX7101 HCL LX7101 HCL is a potent inhibitor of LIMK and ROCK2 with IC50 values of 24, 1.6 and 10 nM for LIMK1, LIMK2 and ROCK2, respectively; also inhibits PKA with an IC50 less than 1 nM.
- GC32811 LXS196 LXS196 (LXS196) is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. LXS196 has the potential for uveal melanoma research.
- GC17563 LY 333531 hydrochloride Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM).
- GC12363 LY2109761 TβRI/II kinase inhibitor
- GC18015 LY2157299 LY2157299 (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
- GC19234 LY3200882 LY3200882 is a novel and highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).
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GC11604
LY364947
Inhibitor of TGF-β type I receptor kinase domain
- GC30545 Malantide Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide is also an efficient substrate for PKC with a Km of 16 μM.
- GC10496 Midostaurin (PKC412) Midostaurin (PKC412) (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin (PKC412) inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM. Midostaurin (PKC412) also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin (PKC412) shows powerful anticancer effects.
- GC32714 Mitoxantrone (mitozantrone) Mitoxantrone (mitozantrone) is a potent topoisomerase II inhibitor.
- GC14363 Mitoxantrone HCl Mitoxantrone HCl is a potent topoisomerase II inhibitor.
- GC17582 ML347 BMP receptor inhibitor,potent and selective
- GC65585 Mongersen Mongersen (GED-0301) is a specific and orally active SMAD7 antisense oligonucleotide.
- GC63778 Myelin Basic Protein TFA Myelin Basic Protein (MHP4-14) TFA, a synthetic peptide comprising residues 4-14 of myelin basic protein, is a very selective PKC substrate (Km=7 μM).
- GC49269 Myr-ZIP A PKMζ inhibitor
- GC44303 N-Acetylpuromycin N-Acetylpuromycin is a non-ribotoxic form of the antibiotic puromycin that is formed in puromycin-resistant S.
- GC25662 N-Desmethyltamoxifen N-Desmethyltamoxifen, the major metabolite of Tamoxifen in humans and a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen, also is a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.
- GC38931 N-Desmethyltamoxifen hydrochloride N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.
- GC10716 Netarsudil (AR-13324) ROCK inhibitor
- GC13514 NG25 An inhibitor of MAP4K2 and TAK1
- GC25669 Nilotinib hydrochloride Nilotinib hydrochloride (AMN-107) is the hydrochloride salt form of nilotinib, an orally bioavailable Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
- GC14075 Nocodazole A tubulin production inhibitor,anti-neoplastic agent
- GC60274 O-Desmethyl Midostaurin O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin via cytochrome P450 liver enzyme metabolism. O-Desmethyl Midostaurin can be used as an indicator for Midostaurin metabolism in vivo. Midostaurin is a multi-targeted protein kinase inhibitor?with?IC50?ranging from 22-500 nM.
- GC36807 ON 146040 ON 146040 is a potent PI3Kα and PI3Kδ (IC50≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC50<150 nM).
- GN10378 Oxymatrine
- GC36833 p32 Inhibitor M36 p32 inhibitor M36 (M36) is a p32 mitochondrial protein inhibitor, which binds directly to p32 and inhibits p32 association with LyP-1.
- GC12637 PD 180970 P210bcr/abl tyrosine kinase inhibitor
- GC13592 PD173955 Dual Src/Abl kinase inhibitor, ATP-competitive,
- GC33901 Pentanoic acid
- GC61585 Pep2m, myristoylated TFA Pep2m, myristoylated TFA (Myr-Pep2m TFA) is a cell-permeable peptide.
- GC14767 PF-00562271 PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively.
- GC14407 PF-431396 Pyk2 and FAK inhibitor
- GC15380 PF-562271 ATP-competitive FAK inhibitor, reversible
- GC10810 PF-562271 HCl PF-562271 (VS-6062) hydrochloride is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively.
- GC17352 Phorbol 12,13-dibutyrate Protein kinase C activator
- GC12790 Pirfenidone TGF-β production inhibitor
- GC40197 Pirfenidone-d5 Pirfenidone-d5 is intended for use as an internal standard for the quantification of pirfenidone by GC- or LC-MS.
- GC15471 PKC β pseudosubstrate Selective cell-permeable peptide inhibitor of protein kinase C
- GC10404 PKC ζ pseudosubstrate PKC ζ pseudosubstrate is a selective cell-permeable inhibitor of PKC.
- GC11671 PKC fragment (530-558) Potent activator of protein kinase C
- GC44655 PKCε Inhibitor Peptide PKCε Inhibitor Peptide (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor.
- GC31711 PKC-IN-1 PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.
- GC65126 PKC-iota inhibitor 1 PKC-iota inhibitor 1 (compound 19) is a protein kinase C-iota (PKC-ι ?) inhibitor with an IC50 value of 0.34 μM.
- GC30200 PKC-theta inhibitor PKC-theta inhibitor is a selective PKC-θinhibitor, with an IC50 of 12 nM.
- GC67686 PKCiota-IN-2 formic
- GC14396 Ponatinib (AP24534) Ponatinib (AP24534) (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
- GC45828 Ponatinib-d8 An internal standard for the quantification of ponatinib
- GC68339 Ponsegromab
- GC12779 PPY A Abl kinases inhibitor
- GC36974 Procyanidin A1 Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca2+ influx from an internal store in RBL-213 cells.