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.

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.

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.

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.

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).

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.

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.

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

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.

LY2157299 is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM. Phase 2.

ζ(ZETA)-Stat (1,3,6-Naphthalenetrisulfonic acid) is a novel PKC-zeta (PKC-ζ) specific inhibitor with IC50 of 5 uM, showed only 13% inhibition on PKC-I at 20 uM.

LY-333,531 Hydrochloride is a potent, selective inhibitor of Protein Kinase C isozymes, PKC beta I (IC50 = 4.7 nM) and PKC beta II (IC50 = 5.9 nM). It is potentially beneficial for cancer research.

Teleocidin A1 (Lyngbyatoxin A), a highly toxic skin irritant, is a potent activator of protein kinase C (PKC). Teleocidin A1 shows antiproliferative activity against HeLa cancer cells (IC50=9.2 nM).

TGFβ-IN-1 is an antitumor growth and metastasis agent through inhibiting the transforming growth factor‑β signaling pathway.

A 77-01 is a potent inhibitor of TGF-β type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM.

TGFβR-IN-1 is a long-acting tumor-activated prodrug of a TGFβR inhibitor.

1-Oleoyl-2-acetyl-sn glycerol is a synthetic, cell permeable diacylglycerol analog. 1-Oleoyl-2-acetyl-sn glycerol activates calcium-dependent protein kinase C (PKC) and induces the superoxide-production.

Bisindolylmaleimide IV (Arcyriarubin A) is a potent protein kinase C (PKC) inhibitor, with IC50s ranging from 0.1 to 0.55 μM. Bisindolylmaleimide IV also inhibits PKA (IC50=3.1-11.8μM). Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with an IC50 of 0.2 μM.

Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.

LY3200882 is a novel, highly selective TGFβRI small molecule inhibitor.

1,2-Didecanoylglycerol, a synthetic diacylglycerol, is metabolized by platelets to 1,2-didecanoylphosphatidic acid (PA10) and activates protein kinase C (PKC).

(±)-1,2-Diolein (1,2-Dioleoyl-rac-glycerol) is a PKC activator.

PF-04577806 is a potent, selective and ATP competitive PKC inhibitor. PF-04577806 shows potent inhibitory activity towards PKCα, PKCβI, PKCβII, PKCγ, and PKCθ with IC50s of 2.4 nM, 8.1 nM, 6.9 nM, 45.9 nM, and 29.5 nM, respectively. PF-04577806 can reverse retinal vascular leakage in diabetic rats.

Bryostatin 3, a macrocyclic lactone, is a protein kinase C activator, with a Ki of 2.75 nM. Bryostatin 3 can block 12-O-tetradecanoylphorbol-13-acetate (TPA) inhibition of cell proliferation, yet did not block TPA-enhanced cell-substratum adhesion.

Sangivamycin (NSC 65346), a nucleoside analog, is a potent inhibitor of protein kinase C (PKC) with an Ki of 10 μM. Sangivamycin has potent antiproliferative activity against a variety of human cancers.

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). Myelin Basic Protein TFA is not phosphorylated by cyclic AMP-dependent protein kinase, casein kinases I and II, Ca2+/calmodulin-dependent protein kinase II, or phosphorylase kinase, and can be routinely used for the assay of protein kinase C with low background in the crude tissue extracts.

PF-03622905 is a potent and ATP-competitive PKC inhibitor with IC50s of 5.6 nM, 14.5 nM, 13 nM, 37.7 nM, and 74.1 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCθ, respectively. PF-03622905 shows high specificity for PKC over other protein kinases.

Bisindolylmaleimide XI hydrochloride (Ro 32-0432) is a potent, selective and orally active PKC inhibitor with IC50s of 9 nM, 28 nM, 31 nM, 37 nM, and 108 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCε, respectively.

Mezerein is a PKC activator that exhibits antileukemic properties. Mezerein inhibits the growth of yeast expressing PKC alpha (IC50=1190 nM), PKC beta1 (IC50=908 nM), and PKC delta (IC50=141 nM) but not of yeast expressing PKC.

TGFβRI-IN-1 is an oral active and selective TGFβ receptor type I (TGFβRI) kinase inhibitor, with IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively .