Mongersen is a 21-mer phosphorothioate antisense oligonucleotide targeting the mRNA of the Smad7 protein, thus leading to suppression of TGF-β1 pathways and remission of Crohn's disease.

SC-9 is a PKC activator in the presence of Ca2+.

Safingol is a lyso-sphingolipid PKC (protein kinase C ) inhibitor.

1,2-Dimyristoyl-sn-glycerol is a saturated diacylglycerol and a weak second messenger for the activation of PKC.

H-7 is a specific protein kinase C inhibitor, which inhibits superoxide release from human neutrophils (PMN) stimulated with phorbol myristate acetate or synthetic diacylglycerol.

Chromenone 1 is a potent osteogenic bone morphogenetic protein (BMP) potentiator. Chromenone 1 exhibits a unique mode of action as it induces a pronounced, kinase-independent, negative TGFβ feedback that enhances nuclear BMP-Smad signaling outputs.

ALK5-IN-9 (Compound 8h) is a potent and orally active inhibitor of TGFβRI (ALK5). ALK5-IN-9 inhibits ALK5 autophosphorylation and NIH3T3 cell activity with IC50 values of 25 nM and 74.6 nM, respectively. ALK5-IN-9 also shows favorable pharmacokinetic profile and ameliorated hERG inhibition. ALK5-IN-9 has the potential for the research of cancer disease.

ALK5-IN-8 is a potent inhibitor of TGFβRI (ALK5). ALK5-IN-8 Inhibits the phosphorylation of ALK5 on its downstream signaling proteins (Smad2 or Smad3) by blocking the binding of TGFβRI to ligands, thereby affecting or blocking TGF-β signaling. ALK5-IN-8 has the potential for the research of various ALK5-mediated related diseases (extracted from patent WO2021190425A1, compound 1).

Myostatin-IN-1 is a potent myostatin inhibitor (IC50 of 0.19, 0.63, 0.89 and 1.6 μM for myostatin, GDF-11, activin A and TGF-β1, respectively). Myostatin-IN-1 increases the tibialis anterior muscle mass in mice. Myostatin-IN-1 can be used for researching the prolonged inactivation of myostatin in skeletal muscle.

NP627 (NP-627) is a specific small-molecule inhibitor of protein kinase C deltaI (PKCδI) with Kd of 1 nM.NP627 inhibits the cleavage of PKCδI in adipocyte (at 10 nM) and decreases PKCδI kinase activity.NP627 does not inhibit other PKC isozyme activities.NP627 prevents caspase-3 mediated cleavage of PKCδI, significantly inhibits PKCδI catalytic fragment release, decreases inflammation and apoptosis, and significantly improves mitochondrial metabolism in human adipocytes from obese individuals.

PF-06952229 is a potent, selective and orally active TGFbR1 inhibitor, specifically binds to TGFbR1 and prevents TGFbR1-mediated signal transduction, shows with potential antineoplastic activity.

PKCθ inhibitor 22 is a potent, selective, orally bioavailable inhibitor of Protein Kinase Cθ (PKCθ) with IC50 of 6 nM.PKCθ inhibitor 22 inhibits IL-2 release from PBMCs following stimulation with anti-CD3/CD28 (IC50=0.19 uM).PKCθ inhibitor 22 also inhibits the release of IL-17 from CD3/CD28 stimulated Th-17 cells with an IC50 of 1 uM.PKCθ inhibitor 22 demonstrated a reduction of symptoms in a mouse model of multiple sclerosis.

Bisindolylmaleimide II is a general inhibitor of all PKC subtypes.

TP0427736 hydrochloride 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). TP0427736 hydrochloride also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. TP0427736 hydrochloride can be used for the research of androgenic alopecia (AGA).

Pm26TGF-β1 peptide TFA is a peptide is a portion of the human TGF-β1 molecule, which shows high affinity for the TGF-β1 receptor.

SJ000063181 is a potent BMP signaling activator with an EC50 ≤1 µM. SJ000063181 can be used as chemical probes to interrogate BMP signaling due to it can penetrate zebrafish embryos.

SY-LB-35 is a potent bone morphogenetic protein (BMP) receptor agonist. SY-LB-35 can stimulate significant increases in cell number and cell viability in the C2C12 myoblast cell line, and causes shifts towards the S and G2/M phases of the cell cycle. SY-LB-35 stimulates canonical Smad and non-canonical PI3K/Akt, ERK, p38 and JNK intracellular signaling pathways.

SY-LB-57 is a highly potent bone morphogenetic protein (BMP) receptor signaling agonist. SY-LB-57 can be used in studies of diseases such as fractures and pulmonary arterial hypertension.

7-Oxostaurosporine is a potent protein kinase C (PKC) inhibitor that effectively inhibits tumor growth by inducing apoptosis and inhibiting the nuclear factor (NF)-κB/p-p65 pathway.

Z640 is a novel non-selective atypical PKC (aPKC) agonist, increases PKCζ and PKCι kinase activity with EC50 of 1.09 and 3.47 µM in vitro kinase activity assays, respectively.

CDD-1115 (CDD1115) is a potent, selective inhibitor of BMP type 2 receptor BMPR2 with IC50 of 1.8 nM and Kiapp of 6.2 nM.

CDD-1281 (CDD1281) is a potent, selective inhibitor of BMP type 2 receptor BMPR2 with IC50 of 1.2 nM and Kiapp value of 8 nM.