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
-
GC12560
Dorsomorphin (Compound C) 2HCl
BML-275 2HCl,Compound C 2HCl
IC50: Dorsomorphin inhibited BMP4-induced phosphorylation of BMP-responsive SMADs in a dose-dependent manner (half maximal inhibitory concentration (IC50) =0.47 mM). -
GC35897
DPH
A potent cell permeable c-Abl activator
-
GC73653
DT-6
DT-6 is an effective TGF-β1 inhibitor.
-
GC90543
EGFR Peptide (human, mouse) (myristoylated) (trifluoroacetate salt)
A PKC inhibitor
-
GC69052
Elezanumab
Elezanumab (ABT-555; AE12-1Y-QL) is a human monoclonal antibody that selectively targets repulsive guidance molecule A (RGMa). Elezanumab effectively inhibits RGMa-mediated BMP signaling through the SMAD1/5/8 pathway, with an IC50 of approximately 97 pM. Elezanumab promotes neuronal regeneration and neuroprotection in models of nerve injury and demyelination by binding to the N-terminal of RGMa, blocking BMP signaling, and lacking cross-reactivity with RGMc. Elezanumab has activity in promoting neuronal regeneration and neuroprotection without affecting iron metabolism.
-
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)
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
Vactosertib, TEW-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
Fasudil (HA-1077; AT877) is a non-specific RhoA/ROCK inhibitor with a Ki of 0.33μM and an IC50 of 0.158μM for ROCK1, and IC50 of 4.58μM, 12.30μM, and 1.650μM for ROCK2, PKA, PKC, and PKG, respectively.
-
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)
HH-GV-678
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
FR 236924 (FR236924), a linoleic acid derivative, selectively and directly activates PKCε. -
GC65539
Fresolimumab
Fresolimumab is a high-affinity humanized monoclonal antibody that binds to and inhibits all isoforms of the protein transforming growth factor β (TGFβ). The Kd values of Fresolimumab for TGFβ1, TGFβ2, and TGFβ3 are 1.7±0.6nM, 3.0±1.2nM, and 2.0±1.2nM, respectively.
-
GC15431
GF 109203X (Bisindolylmaleimide I)
Gö 6850;Bisindolylmaleimide I
GF 109203X is a selective inhibitor of protein kinase C, selective for the α and β1 isoforms with IC50 values of 0.0084, 0.0180, 0.210, 0.132, and 5.8μM for α, β1, δ, ε and ζ isoforms of protein kinase C respectively. -
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
Bcr-Abl inhibitor -
GC15079
GNF 5
Bcr-Abl inhibitor
-
GC10607
GNF-7
Type II Bcr-Abl inhibitor
-
GC15564
Go 6976
Go6976;Go-6976
PKCα/PKCβ1 inhibitor -
GC16907
Go 6983
Goe 6983;Go6983;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
GSK269962A, GSK269962B
ROCK inhibitor -
GC25482
GSK269962A HCl
GSK269962B, GSK269962, GSK 269962
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
GZD824 dimesylate; HQP1351 dimesylate
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
1-O-hexadecyl-2-O-methyl-sn-Glycerol
protein kinase C activity inhibitor -
GC71477
HG-7-86-01
HG-7-86-01 (Compound 26) is type II tyrosine kinase inhibitor.
-
GC15018
Hispidin
protein kinase Cβ inhibitor
-
GC64326
Hydrochlorothiazid-d2
-
GC17523
Hydrochlorothiazide
HCTZ, NSC 53477, SU 5879
diuretic drug of the thiazide class -
GC74190
Hydrochlorothiazide-13C6
HCTZ-13C6
Hydrochlorothiazide-13C6 is the 13C labeled drochlorothiazide.
-
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)
CGP57148B, 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, 3Ingenyl Angelate, PEP005, Picato
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
Ionomycin calcium salt is a narrow spectrum antibiotic being active against Gram-positive bacteria, which produced by the bacterium Streptomyces conglobatus.
-
GC15446
Ionomycin free acid
Ionomycin free acid is a selective and potent calcium ion carrier that acts as an active Ca2+ carrier.
-
GC60210
Isosaponarin
Isosaponarin is a flavone glycoside isolated from wasabi leaves.
-
GC72815
Itacnosertib (hydrocholide)
TP-0184 (hydrocholide
Itacnosertib drocholide is an inhibitor of JAK2, ACVR1 (ALK2) and ALK5. -
GC12108
ITD 1
First selective TGFβ inhibitor
-
GC11362
K 252a
SF 2370
A protein kinase 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.
-
GC15281
K-252c
Staurosporinone
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
-
GC71494
Kartogenin sodium
Kartogenin (KGN) sodium is an inducer of chondrogenic tissue formation (EC50: 100 nM).
-
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.
-
GC72215
KRFK TFA
KRFK TFA, a peptide derived from TSP-1, can activate TGF-β.
-
GC17346
KT 5823
A protein kinase G inhibitor
-
GC40770
L-erythro Sphingosine (d18:1)
L-erythro Sphingosine, L-erythro-C18-Sphingosine
L-erythro Sphingosine is a synthetic stereoisomer of sphingosine (d18:1). -
GC17815
L-threo-Sphingosine C-18
L-threo-Sphingosine C18
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
LDN 193189;LDN193189
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
LDN 193189 hydrochloride; LDN-193189 hydrochloride
LDN193189 Hydrochloride is a selective inhibitor of the transcriptionally active morphogenetic protein (BMP) type I receptor, a family of BMP receptors that includes activin receptor-like kinases (ALK1, ALK2, ALK3, and ALK6). LDN193189 Hydrochloride inhibits ALK2 and ALK3 with IC50 values of 5nM and 30nM, respectively. -
GC36433
LDN193189 Tetrahydrochloride
A selective BMP type I receptor inhibitor
-
GC70857
LIMK-IN-1
LIMK-IN-1 (Compound 14) is an inhibitor of LIM-Kinase (LIMK), with IC50s of 0.5 nM and 0.9 nM for LIMK1 and LIMK2, respectively.
-
GC74573
Livmoniplimab
ABBV-151; ARGX-115
Livmoniplimab (ABBV-151) is a monoclonal antibody against GARP/TGF-β1 that can inhibit the release of active TGF-β1. -
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.
-
GC69412
Luspatercept
ACE-536; luspatercept-aamt
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.
-
GC44094
LX7101 (hydrochloride)
LX7101 is a potent inhibitor of LIM kinase (LIMK) 1 and 2 and Rho-associated kinase 1 (ROCK-1) and ROCK-2 with IC50 values of 32, 4.3, 69, and 32 nM, respectively.
-
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; IDE196
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
Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM). -
GC12363
LY2109761
TβRI/II kinase inhibitor
-
GC18015
LY2157299
LY-2157299;LY 2157299
LY2157299 is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 value of 56nM. -
GC19234
LY3200882
LY3200882 is a novel and highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).
-
GC11604
LY364947
HTS 466284, TGFβ RI Kinase Inhibitor
Inhibitor of TGF-β type I receptor kinase domain
-
GC69418
Lyn-IN-1
Bafetinib analog
Lyn-IN-1 (Bafetinib analog) is a highly active dual inhibitor of Bcr-Abl and Lyn.
-
GC48345
Lyso-Monosialoganglioside GM2 (ammonium salt)
Lysoganglioside GM2, Lyso-GM2, lyso-Monosialoganglioside GM2
-
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)
CGP 41251
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 is an antitumor anthrandione derivative.
-
GC14363
Mitoxantrone HCl
NCI 301739, NSC 301739
Mitoxantrone HCl is a potent topoisomerase II inhibitor. -
GC17582
ML347
LDN193719
BMP receptor inhibitor,potent and selective -
GC65585
Mongersen
GED-0301
Mongersen (GED-0301) is a specific and orally active SMAD7 antisense oligonucleotide. -
GC73107
Mongersen sodium
GED-0301 sodium
Mongersen sodium is a specific and orally active SMAD7 antisense oligonucleotide. -
GC74326
MPSD TFA
MARCKS-ED TFA
MPSD TFA (MARCKS-ED TFA) is the TFA salt form of MPSD. -
GC73234
MY-673
MY-673 is a colchicine binding site inhibitor (CBSI), that inhibits tubulin polymerization.
-
GC63778
Myelin Basic Protein TFA
MHP4-14 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
Myristoylated-ZIP, Myristoylated Zeta-Pseudosubstrate Inhibitory Peptide, Myr-Ser-Ile-Tyr-Arg-Arg-Gly-Ala-Arg-Arg-Trp-Arg-Lys-Leu, Myr-SIYRRGARRWRKL-OH, Ζeta Inhibitory Peptide
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.
-
GC74419
N-myristoyl-RKRTLRRL
N-myristoyl-RKRTLRRL inhibits binding of PKC substrates.