PKCiota-IN-1 (compound 51) is a potent PKCiota (PKC-ι) inhibitor with an IC50 of 2.7 nM. PKCiota-IN-1 also inhibits PKC-α and PKC-ε with IC50s of 45 nM and 450 nM, respectively[1].
GSK269962A is a potent ROCK inhibitor with IC50s of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively.
Chelerythrine is a natural alkaloid, acts as a potent and selective Ca2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM[1]. Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity[2].
ROCK2-IN-6 (Comp A) is a selective ROCK2 inhibitor, can be used for ROCK mediated diseases, autoimmune diseases and inflammation research[1].
A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12, 45 and 7.5 nM, respectively.
K-252a, a staurosporine analog isolated from Nocardiopsis sp. soil fungi, inhibits protein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively[1][2].
Y-27632 dihydrochloride is a cell-permeable, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively.
Fasudil (HA-1077; AT877) dihydrochloride 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 dihydrochloride is also a potent Ca2+ channel antagonist and vasodilator[1][2][3].
Ruboxistaurin (LY333531) is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin inhibits PKC beta II with an IC50 of 5.9 nM[1][2].
Netarsudil mesylate is a small-molecule inhibitor of Rho kinase and a norepinephrine transporter; reduces intraocular pressure (IOP) in normotensive monkey eyes.
GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
Spisulosine-d3 is deuterium labeled Spisulosine. Spisulosine (ES-285) is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKC
RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC50 values of 14.5 nM and 6.2 nM, respectively.
Hispidin, a PKC inhibitor and a phenolic compound from Phellinus linteus, has been shown to possess strong anti-oxidant, anti-cancer, anti-diabetic, and anti-dementia properties[1].
Pep2m, myristoylated (Myr-Pep2m) is a cell-permeable peptide. Pep2m, myristoylated can disrupt the protein kinase ζ (PKMζ) downstream targets, N-ethylmaleimide-sensitive factor/glutamate receptor subunit 2 (NSF/GluR2) interactions. PKMζ is an autonomously active isozyme of protein kinase C (PKC)[1][2].
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[1][2].
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)[1]. Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with an IC50 of 0.2 μM[2].
CRT0066854 hydrochloride is a potent and selective atypical PKCs inhibitor. CRT0066854 is against full-length (FL) PKCι, PKCζ, and ROCK-II kinases with IC50 values of 132 nM, 639 nM, and 620 nM, respectively[1].
Luspatercept (ACE-536) is a recombinant modified ActRIIB fusion protein that binds with transforming growth factor β superfamily ligands. Luspatercept increases the erythrocyte numbers and promotes maturation of erythroid precursors. Luspatercept binds with GDF11 and inhibits Smad2/3 signaling. Luspatercept can be used for the research of anemia[1].
PKCiota-IN-2 is a potent PKCiota (PKC-ι) inhibitor with an IC50 of 2.8 nM. PKCiota-IN-2 also inhibits PKC-α and PKC-ε with IC50s of 71 nM and 350 nM, respectively[1].
H-Leu-Ser-Lys-Leu-OH (LSYL) is a latency-associated peptide at the amino terminus of LAP, with inhibitory effect on TGF-β1 activation. H-Leu-Ser-Lys-Leu-OH, binding with KRFK (HY-P3970), can block the signal transduction of TGF-β1, and prevent the progression of hepatic damage and fibrosis[1].
DCP-LA (FR236924), a linoleic acid derivative, selectively and directly activates PKCε[1].
PKCη pseudosubstrate inhibitor,myristoylated is cell permeable and can be used to study the mechanism of action of PKCη[1].
Halofuginone (RU-19110) is a less-toxic form of Febrifugine, which is isolated from the plant Dichroa febrifuga[1]. Halofuginone inhibits prolyl-tRNA synthetase in an ATP-dependent manner with a Ki of 18.3 nM[2]. Halofuginone attenuates osteoarthritis (OA) by inhibition of TGF-β activity[3].
MY-673 is a colchicine binding site inhibitor (CBSI), that inhibits tubulin polymerization. MY-673 inhibits the ERK signaling pathway, which in turn affects SMAD4 protein expression levels in the TGF-β/SMAD pathway. MY-673 inhibited cell proliferation, migration and induced apoptosis in vivo and in vitro[1].
ALK5-IN-28 (compound Ex-05) is a selective ALK-5 inhibitor (IC50≤10 nM), inhibits TGF-β-induced SMAD signaling. ALK5-IN-28 has the potential to inhibit growth of tumour in vivo. ALK5-IN-28 can be used in study of proliferative diseases such as cancer, fibrotic diseases, and systemic sclerosis[1].
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[1].
Phorbol 12,13-dibutyrate (Phorbol dibutyrate) is a PKC activator and a potent skin tumor promoter[1][2].
LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with Kis of 38 nM and 300 nM, respectively.
(Rac)-Anemonin ((Rac)-Pulsatilla camphor) is the diastereoisomer of Anemonin (HY-N0278). Anemonin (Pulsatilla camphor), a selective iNOS inhibitor, is also a PKC-θ inhibitor. Anemonin can significantly inhibit the translation or protein stability of PKC-θ protein. Anemonin also ameliorates dextran sodium sulfate-induced acute ulcerative colitis (UC) in mice. Anemonin can be used in the research of inflammation-related diseases[1][2].