pkcδ

RO-3306 is a selectivity ATP-competitive CDK1 inhibitor (Ki: 20 nM). The selectivity of RO-3306 for CDK1 is >15-fold higher than a diverse panel of human kinases.

Go 6983, a pan-PKC inhibitor, targets PKCα, PKCβ, PKCγ, PKCδ, and PKCζ, with IC50 values of 7 nM, 7 nM, 6 nM, 10 nM, and 60 nM, respectively.

Delcasertib (KAI-9803) is a potent and selective inhibitor of δ-protein kinase C (δPKC).

A-443654, a pan-Akt inhibitor, exhibits equal potency against Akt1, Akt2, and Akt3 within cells (Ki=160 pM).

Rottlerin (NSC-56346) is a natural product purified from Mallotus Philippinensis and is a specific PKC inhibitor (IC50: PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM). Rottlerin causes apoptosis via caspase 3 activation.

Ruboxistaurin hydrochloride (LY 333531 hydrochloride) is an Isozyme-selective inhibitor of protein kinase C (PKC); competitively and reversibly inhibits PKCβI and PKCβII (IC50 values are 4.7 and 5.9 nM respectively). Selective for PKCβ over other PKC isozymes (IC50values are 0.052, 0.25, 0.30, 0.36, 0.60 and >100 μM for PKCη, -δ, -γ, -α, -ε and -ζ respectively). Exhibits selectivity for PKC over other ATP-dependent kinases, including protein kinase A, casein kinase and src).

PKCδ Peptide Substrate is a highly specific substrate for the δ-type of Protein kinase C, composed of a sequence that mirrors murine eEF-1α (422-443) and includes Thr-431 [1].

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6 15 2 3 3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

DCPLA-ME (2-[(2-Pentylcyclopropyl)methyl]cyclopropaneoctanoic acid methyl ester) is the methyl ester form of DCPLA and can be used to treat neurodegenerative diseases. It is an effective PKCε activator.

20-HETE promotes cell proliferation and migration in cancer and can be used to study prostate tumors and cardiac hypertrophy by activating the protein kinase C pathway to increase FBXO10 expression.20-HETE promotes cell proliferation and migration in cancer and can be used to study prostate tumors and cardiac hypertrophy by activating the protein kinase C pathway.

Phorbol 12,13-dibutyrate (Phorbol dibutyrate) is a PKC activator that inhibits α1-adrenoceptor-mediated positive inotropic effects in a concentration-dependent manner, induced by contraction of isolated rabbit vascular smooth muscle.

Bisindolylmaleimide I (GF109203X) is a potent and highly selective protein kinase C (PKC) inhibitor, exhibiting a Ki of 14 nM.

Phorbol 12-myristate 13-acetate (PMA), a member of the phorbol ester group of natural products, activates PKC, SphK, and NF-κB, and induces THP1 cell differentiation.

Ionomycin calcium (SQ23377 calcium) is an effective and selective calcium ionophore, demonstrating high specificity for divalent cations (Ca>Mg>Sr=Ba).

Gue1654 is a selective OXE-R inhibitor that attenuates coronary artery ligation-induced ischemic myocardial injury and cardiomyocyte oxygen glucose deprivation-induced injury in mice through activation of BCAT1.Gue1654 inhibits OXE-R-inhibited protein kinase C-ε (PKC-ε) nuclear factor κB (NF-κB) signaling and apoptosis in cardiomyocytes. Gue1654 can be used to study cardiovascular disease.

Bisindolylmaleimide VIII (Ro-31-7549) is a selective and potent protein kinase C (PKC) inhibitor with good inhibition of PKC-α, PKC-β I, PKC-β II, PKC-γ, and PKC-ε.Bisindolylmaleimide VIII Bisindolylmaleimide VIII inhibits T cell-mediated autoimmune diseases and enhances Fas-mediated apoptosis through a protein kinase C-independent mechanism.

Safingol hydrochloride (L-threo-dihydrosphingosine hydrochloride) is a specific inhibitor of protein kinase C. It induces autophagy in solid tumor cells and cancer cell death by inhibiting the PKC and PI3-kinase pathways.BIIB 722 Mesylate is a selective sodium-hydrogen exchange inhibitor. Safingol hydrochloride inhibits PKC and PI3k.

Ellagic acid (Gallogen), a thickened tetracyclic natural product, is a potent CK2 inhibitor (IC50=40 nM; Ki=20 nM) with ATP-competitive properties. Ellagic acid is an antioxidant and also possesses antiproliferative activity.

Piceatannol (Astringenin) is an anti-inflammatory, immunomodulatory and antiproliferative agent. It inhibits p56lck and syk protein tyrosine kinases and inhibits NF-κB activation and gene expression of TNF-induced. It is synthetic from the conversion of resveratrol by cytochrome P450 1B1.

Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.

α-Vitamin E (Dexrabeprazole Sodium) is a naturally-occurring form of vitamin E, a fat-soluble vitamin with potent antioxidant properties.

Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.

Mitoxantrone (mitozantrone) is an anthracenedione antibiotic with antineoplastic activity. Mitoxantrone intercalates into and crosslinks DNA, thereby disrupting DNA and RNA replication. This agent also binds to topoisomerase II, resulting in DNA strand breaks and inhibition of DNA repair. Mitoxantrone is less cardiotoxic compared to doxorubicin.