Protein Kinase C (PKC)

Cat. No.

A22010

CAS No.

145317-11-9

Bisindolylmaleimide X hydrochloride

Synonyms: BIM-X hydrochloride; Ro31-8425 hydrochloride

Bisindolylmaleimide X hydrochloride (BIM-X hydrochloride) is a potent and selective protein kinase C (PKC) inhibitor.

Cat. No.

A22289

CAS No.

210297-47-5

HA-100 dihydrochloride

HA-100 is an isoquinoline compound with an added piperazinylsulfonyl group that acts as an inhibitor of protein kinases (PKs), including PKA, PKC, and PKG (IC50s = 8, 12, and 4 µM, respectively).

Cat. No.

A22340

CAS No.

130848-06-5

Decursinol angelate

Decursinol angelate, a cytotoxic and protein kinase C (PKC) activating agent from the root of Angelica gigas, possesses anti-tumor and anti-inflammatory activities.

Cat. No.

A22368

CAS No.

140663-38-3

Iso-H7 dihydrochloride

Iso-H7 dihydrochloride is an inhibitor of phosphokinase C.

Cat. No.

A23132

CAS No.

86555-35-3

Malantide

Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide is also an efficient substrate for PKC with a Km of 16 μM.

Cat. No.

A23135

CAS No.

121545-65-1

Protein Kinase C (19-31)

Synonyms: PKC (19-31)

Protein Kinase C (19-31), a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate peptide for testing the protein kinase C activity. Protein kinase C (PKC) is involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins.

Cat. No.

A24122

CAS No.

460331-61-7

ML192

ML192 is a selective antagonist of G protein-coupled receptor 55 (GPR55), effectively inhibiting GPR55-mediated signaling pathways. It blocks β-arrestin trafficking, suppresses ERK1/2 phosphorylation, and prevents PKCβII translocation, thereby interfering with downstream cellular responses. ML192 is a valuable tool for studying the physiological and pathological roles of GPR55 in processes such as inflammation, pain, cancer, and metabolic regulation.

Cat. No.

A24204

CAS No.

5561-99-9

Gondoic acid (cis-11-Eicosenoic acid)

Synonyms: cis-11-Eicosenoic acid

Gondoic acid (cis-11-Eicosenoic acid) is a monounsaturated long-chain fatty acid found in various plant oils and nuts. It exhibits anti-inflammatory activity by reducing reactive oxygen species (ROS) production and inhibiting the PKCθ/ERK/STAT3 signaling pathway. Gondoic acid is also utilized as a raw material in medical applications and as a moisturizing agent in cosmetic formulations.

Cat. No.

A24486

CAS No.

555-55-5

Hispidin

Hispidin is a phenolic compound and protein kinase C (PKC) inhibitor derived from *Phellinus linteus*. It exhibits strong antioxidant, anticancer, antidiabetic, and anti-dementia activities, making it a promising candidate for research in various disease models.

Cat. No.

A24490

CAS No.

1438881-19-6

CRT0066854

CRT0066854 is a potent and selective inhibitor of atypical protein kinase C (PKC) isoenzymes. It inhibits full-length PKCι, PKCζ, and ROCK-II with IC₅₀ values of 132 nM, 639 nM, and 620 nM, respectively.

Cat. No.

A26136

CAS No.

20988-30-1

Variegatic acid

Variegatic acid is a PKCβ1 inhibitor with an IC₅₀ of 36.2 μM, derived from basidiomycete fungi. It effectively inhibits antigen-induced and calcium ionophore-induced β-hexosaminidase release, with IC₅₀ values of 10.4 μM and 22.2 μM, respectively, as well as TNF-α secretion (IC₅₀ values of 16.8 μM and 20.1 μM). By suppressing the enzymatic activity of calcium-activated PKCβ1, variegatic acid also facilitates the generation of hydroxyl radicals through its action on Fe(III), making it valuable for research focused on biological degradation and allergic responses.

Cat. No.

A30249

CAS No.

257879-35-9

PKCβ inhibitor 1

PKCβ Inhibitor 1 is a highly selective, ATP-competitive inhibitor targeting protein kinase C beta (PKCβ) with IC50 values of 21 nM for PKCβ1 and 5 nM for PKCβ2. This compound demonstrates over 60-fold selectivity for PKCβ2 compared to other PKC isozymes such as PKCα, PKCγ, and PKCε. It is a valuable tool for investigating the roles of PKCβ in various signaling pathways and its implications in diseases such as cancer and diabetes.

Cat. No.

A30513

CAS No.

3316-02-7

ζ-Stat

Synonyms: NSC37044

ζ-Stat (NSC37044) is a specific inhibitor of protein kinase C zeta (PKC-ζ), demonstrating an IC50 of 5 μM. This compound has been shown to effectively reduce proliferation in melanoma cell lines while inducing apoptosis. Its antitumor activity in vitro makes ζ-Stat a valuable tool for research into cancer biology and therapeutic development.

Cat. No.

A30535

CAS No.

138516-31-1

Bisindolylmaleimide VIII acetate

Synonyms: Ro 31-7549 acetate; Bis VIII acetate

Bisindolylmaleimide VIII acetate is a potent and selective inhibitor of protein kinase C (PKC), exhibiting an IC50 of 158 nM for rat brain PKC. It demonstrates strong inhibitory activity against various PKC isoforms, with IC50 values of 53 nM for PKC-α, 195 nM for PKC-βI, 163 nM for PKC-βII, 213 nM for PKC-γ, and 175 nM for PKC-ε. This compound is valuable for research applications related to Fas-mediated apoptosis and the modulation of T cell-mediated autoimmune responses.

Cat. No.

A30584

CAS No.

121263-19-2

Calphostin C

Synonyms: UCN-1028C

Calphostin C is a selective inhibitor of protein kinase C (PKC), displaying an IC50 of 0.05 μM. This compound disrupts PKC-mediated phosphorylation, promoting tumor apoptosis and exhibiting potential therapeutic benefits. Additionally, Calphostin C has been shown to restore Na+/K+ ATPase activity in diabetic mouse sciatic nerves, offering insights into its role in mitigating diabetic complications. It serves as a valuable tool for research in cancer biology and neuropathy.

Cat. No.

A31078

CAS No.

31894-34-5

ζ-Stat trisodium

Synonyms: NSC37044 trisodium

ζ-Stat trisodium is a selective inhibitor of protein kinase C zeta (PKC-ζ), exhibiting an IC50 of 5 μM. This compound effectively reduces the proliferation of melanoma cell lines and induces apoptotic cell death. Its antitumor activity in vitro supports its potential application in cancer research and therapeutic development.

Cat. No.

A31209

CAS No.

1351056-65-9

OSU-2S

OSU-2S is a potent activator of Protein Kinase C delta (PKCδ). It effectively inhibits cell proliferation and migration while inducing apoptosis. In combination with Sorafenib, OSU-2S decreases the phosphorylation of ERK1/2 and enhances PKCδ expression (38 kDa). Additionally, OSU-2S is a non-immunosuppressive analogue of FTY720 and demonstrates notable anticancer activity, making it valuable for cancer research applications.

Cat. No.

A31749

CAS No.

154675-18-0

HBDDE

HBDDE is an isoform-selective inhibitor targeting PKCα and PKCγ, with IC50 values of 43 μM and 50 μM, respectively. This compound exhibits selectivity for PKCα and PKCγ over PKCδ, PKCβI, and PKCβII isozymes. HBDDE has been shown to induce neuronal apoptosis, making it a valuable tool for research involving neuronal cell death and signaling pathways regulated by PKC isoforms.

Cat. No.

A32058

CAS No.

359017-79-1

Enzastaurin hydrochloride

Synonyms: LY317615 hydrochloride

Enzastaurin hydrochloride is a potent and selective inhibitor of protein kinase C beta (PKCβ), exhibiting an IC50 of 6 nM. This compound demonstrates a 6- to 20-fold preference for PKCβ over other isoforms, including PKCα, PKCγ, and PKCε. Enzastaurin is utilized in research focused on cancer therapeutics and signal transduction pathways, providing insights into the role of PKCβ in cellular processes and disease mechanisms.

Cat. No.

A32128

CAS No.

365253-37-8

Enzastaurin di(hydrochloride)

Synonyms: LY317615 dihydrochloride

Enzastaurin dihydrochloride is a potent and selective inhibitor of protein kinase C beta (PKCβ), exhibiting an IC50 of 6 nM. This compound demonstrates 6- to 20-fold selectivity over other PKC isoforms, including PKCα, PKCγ, and PKCε. Enzastaurin is utilized in research applications focused on cancer biology and signal transduction pathways, providing insights into therapeutic targets for malignancies and related diseases.

Cat. No.

A33050

CAS No.

125313-65-7

Bisindolylmaleimide VIII

Synonyms: Ro 31-7549; Bis VIII

Bisindolylmaleimide VIII is a highly selective inhibitor of protein kinase C (PKC), exhibiting an IC50 of 158 nM against rat brain PKC. This compound demonstrates significant potency across various PKC isoforms, including IC50 values of 53 nM for PKC-α and 175 nM for PKC-ε. Additionally, Bisindolylmaleimide VIII promotes Fas-mediated apoptosis and serves as a valuable tool in research focused on T cell-mediated autoimmune diseases and efforts to elucidate PKC pathways in cellular signaling.

Cat. No.

A33076

CAS No.

919992-85-1

BHA536

BHA536 is a selective inhibitor targeting PKCα and PKCβ, effectively modulating the NF-kB signaling pathway. It demonstrates significant antitumor activity by inhibiting the proliferation of CD79-mutated ABC DLBCL cells, inducing cell cycle arrest at the G1 phase, and triggering apoptosis in TMD8 cells. Additionally, BHA536 shows promising antitumor efficacy in in vivo mouse models, making it a valuable tool for cancer research and therapeutic studies.

Cat. No.

A34681

CAS No.

1072100-81-2

PF-04577806

PF-04577806 is a selective ATP-competitive inhibitor targeting protein kinase C (PKC) isoforms. It demonstrates strong inhibitory activity against PKCα, PKCβI, PKCβII, PKCγ, and PKCθ, with IC50 values of 2.4 nM, 8.1 nM, 6.9 nM, 45.9 nM, and 29.5 nM, respectively. This compound is utilized in research related to retinal vascular leakage, particularly in models of diabetes.

Cat. No.

A34683

CAS No.

1072100-15-2

PF-03622905

PF-03622905 is a highly selective, ATP-competitive inhibitor of protein kinase C (PKC) isoforms, demonstrating IC50 values of 5.6 nM for PKCα, 14.5 nM for PKCβI, 13 nM for PKCβII, 37.7 nM for PKCγ, and 74.1 nM for PKCθ. This compound exhibits strong specificity for PKC, making it a valuable tool for research applications focused on cell signaling pathways, cancer biology, and therapeutic development targeting PKC-related diseases.

Cat. No.

A36811

CAS No.

2250019-91-9

CRT0066854 hydrochloride

CRT0066854 hydrochloride is a selective inhibitor of atypical protein kinases C (PKCs). It demonstrates potent inhibition against full-length PKCι, PKCζ, and ROCK-II kinases, with IC50 values of 132 nM, 639 nM, and 620 nM, respectively. This compound is valuable for research applications involving cell signaling, cancer biology, and the study of neurodegenerative diseases, providing insights into the role of PKCs in various biological processes.