TGF-β/Smad

LY317615 (Enzastaurin) is a potent and selective inhibitor of PKCβ with antiproliferative activity (IC50= ~6 nM).

H 89 dihydrochloride is a cell-permeable, selective, reversible, ATP-competitive and potent inhibitor of protein kinase.

A-674563 is a B/Akt inhibitor with an IC50 of 14 nM and also shows inhibitory activity against PKA and CDK2 with IC50 of 16 and 46 nM, respectively.

EW-7197 is a highly potent, selective, and orally bioavailable TGF-β I receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively

Ro 31-8220 mesylate is a PKC-inhibitor, which inhibits stimulated fluid pinocytosis of human PMNs induced by the PKC-activators phorbol myristate acetate (PMA, IC50 = 1.35 x 10(-6) M) or diacylglycerols (OAG, diC8) by 95%.

PKI 14-22 amide, myristoylated is a useful heat stable cAMP-dependent protein kinase inhibitor. This is often used to study PKA in cellular systems in-vitro.

Azaindole 1 (BAY-549) is a highly potent inhibitor of human ROCK-1 and ROCK-2 isoenzymes with IC50 values of 0.6 and 1.1 nM, respectively.

Fasudil HCl is a cyclic nucleotide-dependent protein kinase inhibitor and Rho-associated kinase inhibitor (IC50 = 10.7 μM).

RepSox (SJN 2511) is a selective inhibitor of the TGF-β type I receptor ALK5 (IC50 values are 0.004 and 0.023 μM for ALK5 autophosphorylation and ALK5 binding respectively).

GO6983 is a potent protein kinase C (PKC) inhibitor. It reduces polymorphonuclear leukocyte adherence and infiltration following myocardial ischemia/reperfusion injury.

LDN193189 is a highly potent small molecule BMP inhibitor that inhibits BMP type I receptors ALK2 (IC50: 5 nM), ALK3 (IC50: 30 nM) and ALK6 (TGFβ1/BMP signaling) and subsequent SMAD phosphorylation.

GW788388 is a potent, orally active and selective inhibitor of transforming growth factor beta receptor I (TGF-βR1) (activin receptor-like kinase 5, ALK5).

Staurosporine is a natural product originally isolated in 1977 from the bacterium Streptomyces staurosporeus. The main biological activity of staurosporine is the inhibition of protein kinases through the prevention of ATP binding to the kinase. This is achieved through the stronger affinity of staurosporine to the ATP-binding site on the kinase.

ITD-1 is a novel and highly selective TGFβ pathway inhibitor. ITD-1 molecule turns stem cells into heart cells.

SB 431542 is a potent and specific inhibitor of transforming growth factor-β superfamily type I ALK receptors ALK4, ALK5, and ALK7 .

SIS3 is a novel specific inhibitor of Smad3. It has effect on transforming growth factor-beta1-induced extracellular matrix expression.

GSK 269962 is a potent Rho kinase (ROCK) inhibitor (IC50 values are 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively).

Y-27632 is an ATP-competitive inhibitor of ROCK-I and ROCK-II, with Ki of 220 nM and 300 nM for ROCK-I and ROCK-II, respectively.

Verbascoside is isolated from Lantana camara, acts as an ATP-competitive inhibitor of PKC, with an IC50 of 25 μM, and has antitumor, anti-inflammatory and antineuropathic pain activity.

Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.

DMH-1 is a selective inhibitor of the bone morphogenic protein (BMP) ALK2 receptor (IC50 = 108 nM).

Ripasudil (K-115) is potent ROCK inhibitor with IC50 of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension.

LY2109761, a novel transforming growth factor β receptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis

Y-27632 is a Rho-Associated Coil Kinase (ROCK) inhibitor that increases the cloning efficiency of human embryonic stem cells (hESCs).

A83-01 is a selective inhibitor of the transforming growth factor-beta type I receptor ALK5, the Nodal receptor ALK4, and the nodal receptor ALK7

Chelerythrine affects translocation of PKC from cytosol to plasma membrane. Shown to prevent neurite growth. Induces apoptosis in a concentration- and schedule-dependent manner.

LY2157299 is an orally active transforming growth factor beta receptor (TGF-βR) kinase inhibitor.

Bryostatin 1 is a macrolactone isolated from the marine bryozoan, Bugula neritina, that modulates protein kinase C (PKC) activity. Bryostain 1 induces an initial rapid activation and autophosphorylation of PKC that results in the translocation of the PKC enzyme to the membrane.

Daphnetin is a coumarin analog that acts as an inhibitor of several protein kinases. It inhibits EGFR kinase (IC50 = 7.67 μM), PKA (IC50 = 9.33 μM), and PKC (IC50 = 25 μM), in vitro. The inhibition of EGFR kinase by daphnetin was competitive to ATP and non-competitive to the peptide substrate. Also acts as a potent antioxidant and anti-malarial agent.

GSK429286A is a cell-permeable, selective small molecule inhibitor of Rho-associated, coiled-coil containing protein kinase (ROCK).

Hesperetin, a selective phosphodiesterase (PDE)4 inhibitor, is present in the traditional Chinese medicine, ?€?Chen Pi.?€? Hesperetin is a citrus flavonoid that has been reported to lower plasma cholesterol. Hesperetin reduces the transcription of ACAT-2 mRNA in Hep-G2 cells and reduces ApoB protein synthesis in a dose-dependent manner. It also is a potential therapy for carcinoid cancer.

SB525334 is a selective inhibitor of transforming growth factor-β receptor I (ALK5, TGF-βRI) (IC50 = 14.3 nM). Inhibits TGF-β1-induced smad2/3 nuclear localization and TGF-βRI-induced mRNA expression in kidney cells

RKI-1313 is a negative control for RKI-1447 which is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer.

Thiazovivin is a selective inhibitor of Rho-associated kinase (ROCK).

PT-262 is a selective ROCK inhibitor with an IC50 of approximately 5 μM. This compound induces loss of mitochondrial membrane potential and enhances caspase-3 activation, leading to apoptosis. PT-262 also inhibits phosphorylation of ERK and CDC2 through a p53-independent mechanism, disrupts cytoskeletal dynamics, and impairs cell migration. Its efficacy in promoting anti-cancer activity makes PT-262 a valuable reagent for cancer research.

Y-27632 hydrochloride hydrate is a selective inhibitor of Rho-associated protein kinases (ROCK-I and ROCK-II), exhibiting ATP-competitive activity with IC50 values of 220 nM and 300 nM, respectively. This compound has been shown to reduce Doxorubicin-induced apoptosis in human cardiac stem cells and suppress apoptosis in dissociation-induced murine prostate stem/progenitor cells. Additionally, Y-27632 hydrochloride hydrate enhances the differentiation of human induced pluripotent stem cells (hIPSCs) towards a mesendodermal lineage by modulating epithelial-mesenchymal transition.

PKCβ Inhibitor 1 is a highly selective, ATP-competitive inhibitor targeting protein kinase C beta (PKCβ) with IC50 values of 21 nM for PKCβ1 and 5 nM for PKCβ2. This compound demonstrates over 60-fold selectivity for PKCβ2 compared to other PKC isozymes such as PKCα, PKCγ, and PKCε. It is a valuable tool for investigating the roles of PKCβ in various signaling pathways and its implications in diseases such as cancer and diabetes.

DJ4 is an ATP-competitive inhibitor of ROCK1/2 and MRCKα/β, with IC₅₀ values of 5 nM and 50 nM for ROCK1 and ROCK2, and 10 nM and 100 nM for MRCKα and MRCKβ, respectively. It blocks stress fiber formation and induces apoptosis, making it a valuable compound for cancer research.

Cotosudil is a ROCK kinase inhibitor that can be used in research related to glaucoma and ocular hypertension. It functions by reducing intraocular pressure through modulation of aqueous humor outflow.

THK01 is a potent and selective ROCK2 inhibitor, with IC₅₀ values of 5.7 nM for ROCK2 and 923 nM for ROCK1. It inhibits breast cancer metastasis by targeting the ROCK2–STAT3 signaling pathway and is suitable for research in breast cancer.

HSD1590 is a potent inhibitor of Rho-associated protein kinases, with IC₅₀ values of 1.22 nM for ROCK1 and 0.51 nM for ROCK2. It exhibits strong binding affinity to ROCK isoforms (K\_d < 2 nM) and demonstrates low cytotoxicity, making it suitable for further research applications.

CRT0066854 is a potent and selective inhibitor of atypical protein kinase C (PKC) isoenzymes. It inhibits full-length PKCι, PKCζ, and ROCK-II with IC₅₀ values of 132 nM, 639 nM, and 620 nM, respectively.

AS1892802 is a potent, orally active, and highly selective inhibitor of Rho-associated kinase (ROCK). It exhibits a rapid onset of antinociceptive effect, comparable to that of Tramadol and Diclofenac. Unlike traditional analgesics, AS1892802 does not induce gastric irritation or abnormal behavior, making it a promising candidate for research in the treatment of severe osteoarthritis pain.

PF-4950834 is a potent, selective, and orally bioavailable ATP-competitive inhibitor of Rho-associated kinases, with IC₅₀ values of 8.35 nM for ROCK2 and 33.12 nM for ROCK1. It effectively inhibits neutrophil migration and is suitable for research on inflammation and immune cell regulation.

OXA-06 hydrochloride is an ATP-competitive inhibitor of Rho-associated protein kinase (ROCK) that suppresses anchorage-dependent growth and invasion of non-small cell lung cancer (NSCLC) cell lines. It inhibits cofilin phosphorylation without inducing apoptosis.

Hispidin is a phenolic compound and protein kinase C (PKC) inhibitor derived from *Phellinus linteus*. It exhibits strong antioxidant, anticancer, antidiabetic, and anti-dementia activities, making it a promising candidate for research in various disease models.

MY-673 is a colchicine binding site inhibitor (CBSI) that disrupts microtubule dynamics by inhibiting tubulin polymerization. In addition to its antimitotic effects, MY-673 suppresses the ERK signaling pathway, which leads to modulation of SMAD4 protein expression within the TGF-β/SMAD signaling axis. These combined actions result in potent inhibition of cancer cell proliferation and migration, and the induction of apoptosis, both in vitro and in vivo. MY-673 holds promise as a therapeutic candidate for targeting cancers driven by aberrant microtubule dynamics and dysregulated TGF-β/ERK signaling.

HA-1004 is a selective and multifunctional inhibitor of cyclic nucleotide-dependent protein kinases, including protein kinase A (PKA) and cyclic GMP-dependent protein kinase (PKG). It regulates key second messenger pathways involving cyclic AMP and cyclic GMP and has broad pharmacological effects. HA-1004 inhibits lipolysis and induces vascular smooth muscle relaxation, acting as a vasodilator. It also functions as a calcium antagonist, contributing to its ability to suppress contraction in rabbit aortic strips. In neurological models, HA-1004 has been shown to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models, suggesting potential relevance in addiction and neurochemical regulation. Its diverse actions make it a valuable tool for studying cardiovascular, metabolic, and neurobiological processes.

Akt1&PKA-IN-2 (Compound R-29) is a AKT1 and PKA inhibitor with selectivity for CDK2, with IC50 values of 0.007 and 0.01 μM, respectively. Akt1&PKA-IN-2 is applicable for cancer research.

Akt1&PKA-IN-1 is a potent dual inhibitor targeting both Akt and Protein Kinase A (PKA), exhibiting IC50 values of 0.03 μM for PKAα and 0.11 μM for Akt, with a higher IC50 of 9.8 μM for cyclin-dependent kinase 2 (CDK2). This compound demonstrates selective inhibition of CDK2, making it a valuable tool for research in cancer biology and cellular signaling pathways. Akt1&PKA-IN-1 is useful for studying the regulatory role of these kinases in cellular processes and potential therapeutic applications.