TGFβRI-IN-3 inhibits TGFβR1 at an IC50 of 0.79 nM with 2000-fold selectivity against MAP4K4. TGFβRI-IN-3 represents a highly selective TGFβR1 inhibitor that has potential applications in immuno-oncology.

SBI-0087702 promots the cytoplasmic localization of ATF2 in melanoma cells. SBI-0087702-induced translocation of ATF2 to the mitochondria results in increased apoptosis due to loss of mitochondrial membrane integrity. SBI-0087702 also inhibits growth and motility of melanoma cells. SBI-0087702 was shown to inhibit ATF2 phosphorylation on Thr52 by PKCε.

(R)-AR-13503 ((R)-AR-13324 M1 metabolite) is the the (R)-enantiomer of AR-13503. BAY-7081 is a potent, selective, orally active and soluble cyanopyridone-based PDE9A inhibitor with an IC50 of 15 nM.

SRI-011381 hydrochloride is an agonist of the transforming growth factor-beta (TGF-β) signalling pathway and exhibits neuroprotective effects with the potential to treat Alzheimer's disease. It also increases fibronectin expression in the NIH‐3T3 cells stimulated by metformin.

A novel, potent, brain permeant PKC inhibitor with IC50 of 80 nM, without detectable binding to the estrogen receptor (Ki>10 uM).

K02288 is a potent, and selective type I BMP receptor inhibitor with IC50 of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA.

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.

PKC-iota inhibitor 1 (compound 19) is a protein kinase C-iota (PKC-ι ?) inhibitor with an IC50 value of 0.34 μM.

CGP60474 is a potent inhibitor of cyclin-dependent kinase (CDK).

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

Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor. Epsilon-V1-2 inhibits the translocationof PKCε, but not α-, β-, and δPKC.

ALK2-IN-4 is a potent ALK2 inhibitor extracted from patent WO2020086963A1, compound Formula I free base.

SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM, 100-fold more selective for ALK5 than p38 MAPK and other kinases.

ICA-1(ICA-1T)is a potent, specific inhibitor of Protein Kinase C-iota (PKC-ι) with IC50 of 0.1 uM, does not inhibit PKC-ζ, the closely related atypical PKC family member.

ζ-Stat trisodium (NSC37044 trisodium) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat trisodium can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro.

SRI-31277 is a tripeptide inhibitor of thrombospondin 1 activation of TGF-β, specifically inhibits TGF-β activation mediated through TSP-1 with pIC50 of 8.28 nM.

Ki26894 (Ki 26894) is a small molecule TGF-beta type I receptor (TbetaR-I) kinase inhibitor, inhibits TGF-β-induced transcriptional activation in MDA-231-D-TβFluc/Rluc cells with IC50 of 0.49 uM.

CDD-1653 (CDD1653) is a potent, selective inhibitor of BMP type 2 receptor BMPR2 with IC50 of 2.8 nM, >360-fold over ALK1, and is inactive versus all other type 1 and type 2 TGFβ family kinases.

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.

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.

Bisindolylmaleimide X is a cell-permeable, reversible, ATP-competitive protein kinase C (PKC) inhibitor (IC50 = 15 nM, rat brain PKC).

GW6604 is a potent and selective ALK-5 inhibitor with potent anticancer activity.

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.

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

VTX-27 is a selective protein kinase C θ (PKC θ) inhibitor, with Kis of 0.08 nM and 16 nM for PKC θ and PKC δ.

N-Desmethyltamoxifen 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 is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.

Phorbol 12-myristate 13-acetate (PMA) is a PKC-activating phorbol ester, increases the intracellular Ca2+ concentration ([Ca2+]i) in a dose-dependent manner, with an EC50 of 11.7 nM.

CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression.

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.

Staurosporine is a prototypical potent ATP-competitive kinase inhibitor with IC50 of 0.7, 7, 8.5, 6, 20 nM for PKC, PKA,PKG, p60v-src tyrosine protein kinase, CaM kinase II, respectively.