Search Result

Results for "

PKC inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	PKC (141) 5-HT Receptor (2) Adenosine Kinase (1) Akt (5) AMPK (1) Antibiotic (5) Apoptosis (32) Arrestin (1) ATM/ATR (1) Aurora Kinase (1) Autophagy (14) Bacterial (5) Bcl-2 Family (2) Beta-lactamase (2) Btk (1) c-Kit (2) Calcium Channel (5) CaMK (4) Casein Kinase (1) Caspase (2) CDK (4) Checkpoint Kinase (Chk) (1) CMV (1) COX (1) Cytochrome P450 (2) DNA-PK (8) DNA/RNA Synthesis (1) Dopamine β-hydroxylase (2) Drug Metabolite (4) EGFR (3) Endogenous Metabolite (8) ERK (1) Estrogen Receptor/ERR (2) FLT3 (4) Fungal (2) GPR55 (2) GSK-3 (5) HIV (5) HSP (1) HSV (1) IKK (1) Influenza Virus (3) Isotope-Labeled Compounds (7) JAK (1) Keap1-Nrf2 (1) Lipoxygenase (1) MNK (2) Monoamine Oxidase (2) mTOR (1) Myosin (5) NO Synthase (2) Nucleoside Antimetabolite/Analog (1) Orthopoxvirus (4) p38 MAPK (2) Parasite (2) PARP (1) PDGFR (1) PDK-1 (1) Phosphatase (2) Phospholipase (1) PI3K (1) PKA (19) Pyruvate Kinase (1) RABV (1) Ras (1) Reactive Oxygen Species (1) Reverse Transcriptase (3) ROCK (12) SARS-CoV (2) SHP2 (2) SphK (2) Src (2) Syk (1) Telomerase (2) Topoisomerase (5) Tyrosinase (3) VEGFR (1)
By Research Areas:	Cancer (107) Cardiovascular Disease (10) Infection (17) Inflammation/Immunology (33) Metabolic Disease (17) Neurological Disease (16)

By Targets:

PKC (141)

5-HT Receptor (2)

Adenosine Kinase (1)

Akt (5)

AMPK (1)

Antibiotic (5)

Apoptosis (32)

Arrestin (1)

ATM/ATR (1)

Aurora Kinase (1)

Autophagy (14)

Bacterial (5)

Bcl-2 Family (2)

Beta-lactamase (2)

Btk (1)

c-Kit (2)

Calcium Channel (5)

CaMK (4)

Casein Kinase (1)

Caspase (2)

CDK (4)

Checkpoint Kinase (Chk) (1)

CMV (1)

COX (1)

Cytochrome P450 (2)

DNA-PK (8)

DNA/RNA Synthesis (1)

Dopamine β-hydroxylase (2)

Drug Metabolite (4)

EGFR (3)

Endogenous Metabolite (8)

ERK (1)

Estrogen Receptor/ERR (2)

FLT3 (4)

Fungal (2)

GPR55 (2)

GSK-3 (5)

HIV (5)

HSP (1)

HSV (1)

IKK (1)

Influenza Virus (3)

Isotope-Labeled Compounds (7)

JAK (1)

Keap1-Nrf2 (1)

Lipoxygenase (1)

MNK (2)

Monoamine Oxidase (2)

mTOR (1)

Myosin (5)

NO Synthase (2)

Nucleoside Antimetabolite/Analog (1)

Orthopoxvirus (4)

p38 MAPK (2)

Parasite (2)

PARP (1)

PDGFR (1)

PDK-1 (1)

Phosphatase (2)

Phospholipase (1)

PI3K (1)

PKA (19)

Pyruvate Kinase (1)

RABV (1)

Ras (1)

Reactive Oxygen Species (1)

Reverse Transcriptase (3)

ROCK (12)

SARS-CoV (2)

SHP2 (2)

SphK (2)

Src (2)

Syk (1)

Telomerase (2)

Topoisomerase (5)

Tyrosinase (3)

VEGFR (1)

By Research Areas:

Cancer (107)

Cardiovascular Disease (10)

Infection (17)

Inflammation/Immunology (33)

Metabolic Disease (17)

Neurological Disease (16)

185

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Peptides

Natural
Products

Recombinant Proteins

Isotope-Labeled Compounds

Targets Recommended: PKC

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-112681

PKC-theta inhibitor

PKC Others

PKC-theta inhibitor is a selective PKC-θinhibitor, with an IC₅₀ of 12 nM.

**PKC-theta inhibitor**	PKC	Others
PKC-theta inhibitor is a selective PKC-θinhibitor, with an IC₅₀ of 12 nM.

HY-126328

PKC-theta inhibitor 1	PKC	Inflammation/Immunology
PKC-theta inhibitor 1 is the PKCθ inhibitor with an K_i value of 6 nM, inhibits IL-2 production in vivo with an IC₅₀ of 0.19 μM. PKC-theta inhibitor 1 demonstrates a reduction of symptoms in a mouse model of multiple sclerosis .

HY-126146

PKC-iota inhibitor 1

2 Publications Verification

PKC Cancer

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

PKC-iota inhibitor 1 2 Publications Verification	PKC	Cancer
PKC-iota inhibitor 1 (compound 19) is a *protein kinase C-iota (PKC-ι ℩)* inhibitor with an IC₅₀ value of 0.34 μM .

HY-P10085

PKC-ε translocation inhibitor peptide	PKC	Inflammation/Immunology
PKC-ε translocation inhibitor peptide is a PKC-ε translocation inhibitor. PKC-ε translocation inhibitor peptide can regulate the rate of FcγR-mediated internalization of opsonized beads, has no effect of FcαR trafficking .

HY-P5988

N-myristoyl-RKRTLRRL	PKC	Cancer
N-myristoyl-RKRTLRRL inhibits binding of *PKC* substrates. N-myristoyl-RKRTLRRL inhibits Ca ²⁺- and phosphatidylserine (PS)-dependent histone phosphorylation with IC₅₀ of 5 μM.? histone phosphorylation with IC₅₀ of 80 μM .

HY-P5886

PKC 20-28,myristoylated Myristoylated protein kinase C inhibitor 20-28	PKC	Cancer
PKC 20-28,myristoylated (Myristoylated protein kinase C inhibitor 20-28) is a cell-permeable *PKC* inhibitor that can be used in cancer research .

HY-112412

*PDGFR Tyrosine Kinase Inhibitor* III** PDGF Receptor Tyrosine Kinase inhibitor III	PDGFR	Neurological Disease
PDGFR Tyrosine Kinase Inhibitor III (PDGF Receptor Tyrosine Kinase Inhibitor III), a multikinase inhibitor, inhibits PDGFR, EGFR, FGFR, PKA, and PKC, respectively. PDGFR Tyrosine Kinase Inhibitor III can be used for the research of amyotrophic lateral sclerosis .

HY-162234

PKCTheta-IN-1

PKC Others

PKCTheta-IN-1 (Compound 19) is a selective macrocyclic PKCTheta inhibitor with IC₅₀ value of 0.1 nM .

PKCTheta-IN-1	PKC	Others
PKCTheta-IN-1 (Compound 19) is a selective macrocyclic PKCTheta inhibitor with IC₅₀ value of 0.1 nM .

HY-13335

*PKCβ inhibitor* 1**	PKC Apoptosis	Cancer
PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC₅₀s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε) .

HY-13689

Go 6983 45+ Cited Publications Gö 6983; Goe 6983	PKC	Cancer
Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC₅₀ of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM, respectively.

HY-16903

PKC-IN-1	PKC	Inflammation/Immunology
PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional *PKC* enzymes with K_is of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC₅₀s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.

HY-10343

Sotrastaurin 15+ Cited Publications AEB071	PKC	Inflammation/Immunology Cancer
Sotrastaurin (AEB071) is a potent and orally-active pan-PKC inhibitor, with K_is of 0.22 nM, 0.64 nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively .

HY-13867

Bisindolylmaleimide I 30+ Cited Publications GF109203X; Go 6850	PKC GSK-3	Metabolic Disease Cancer
Bisindolylmaleimide I (GF109203X) is a cell-permeable and reversible *PKC* inhibitor (IC₅₀ of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I is also a GSK-3 inhibitor .

HY-13867A

Bisindolylmaleimide I hydrochloride 30+ Cited Publications GF109203X hydrochloride; Go 6850 hydrochloride	PKC GSK-3	Metabolic Disease Cancer
Bisindolylmaleimide I (GF109203X) hydrochloride is a cell-permeable and reversible *PKC* inhibitor (IC₅₀ of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I hydrochloride is also a GSK-3 inhibitor .

HY-117610A

Bisindolylmaleimide XI hydrochloride 2 Publications Verification Ro 32-0432; Ro 31-8830 hydrochloride	PKC	Inflammation/Immunology
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 .

HY-P3199

*PKCβII Peptide Inhibitor* I**	PKC	Inflammation/Immunology
PKCβII Peptide Inhibitor I is a PKCβII inhibitor. PKCβII Peptide Inhibitor I shows cardioprotective effects in rat cardiac Ischemia/reperfusion injury model. PKCβII Peptide Inhibitor I also prevents vascular endothelial dysfunction .

HY-131305

HBDDE	PKC Apoptosis	Neurological Disease
HBDDE, a derivative of Ellagic acid, is an isoform-selective PKCα and PKCγ inhibitor with IC₅₀s of 43 μM and 50 μM, respectively. HBDDE shows selective for PKCα/PKCγ over PKCδ, PKCβI and PKCβII isozymes. HBDDE induces neuronal apoptosis .

HY-129624A

Bisindolylmaleimide VIII acetate Ro 31-7549 acetate; Bis VIII acetate	PKC Apoptosis	Inflammation/Immunology Cancer
Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC₅₀ of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate has IC₅₀s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-β_I, PKC-β_II, PKC-γ, PKC-ε, respectively . Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases .

HY-139466

PF-03622905	SHP2 PKC	Metabolic Disease
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 .

HY-10342

Enzastaurin 5+ Cited Publications LY317615	PKC Autophagy Apoptosis	Cancer
Enzastaurin (LY317615) is a potent and selective PKCβ inhibitor with an IC₅₀ of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε .

HY-P1286

PKC β pseudosubstrate

PKC Neurological Disease

PKC β pseudosubstrate is a selective cell-permeable inhibitor of PKC .
HY-P1286A

PKC β pseudosubstrate TFA

PKC Neurological Disease

PKC β pseudosubstrate TFA is a selective cell-permeable inhibitor of PKC .
HY-112782

VTX-27

PKC Inflammation/Immunology

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

PKC β pseudosubstrate	PKC	Neurological Disease
PKC β pseudosubstrate is a selective cell-permeable inhibitor of *PKC* .

PKC β pseudosubstrate TFA	PKC	Neurological Disease
PKC β pseudosubstrate TFA is a selective cell-permeable inhibitor of *PKC* .

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

HY-P5888

*PKCε inhibitor* peptide,myristoylated** Myr‐PKCɛ-	PKC	Inflammation/Immunology
PKCε inhibitor peptide,myristoylated (Myr‐PKC?-) is a cell permeable myristic acid conjugated *PKC?* peptide inhibitor that attenuates NO release in cultured human umbilical vein endothelial cells (HUVECs) .

HY-13866

Ro 31-8220 mesylate 10+ Cited Publications Ro 31-8220 methanesulfonate; Bisindolylmaleimide IX mesylate	PKC	Cardiovascular Disease Neurological Disease Cancer
Ro 31-8220 mesylate is a potent *PKC* inhibitor, with IC₅₀s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC₅₀s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.

HY-13866A

Ro 31-8220 Bisindolylmaleimide IX	PKC	Cardiovascular Disease Neurological Disease
Ro 31-8220 is a potent *PKC* inhibitor, with IC₅₀s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC₅₀s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.

HY-122858

PKCiota-IN-2	PKC	Cancer
PKCiota-IN-2 (Compound 49) 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 .

HY-122858A

PKCiota-IN-2 formic	PKC	Cancer
PKCiota-IN-2 formic is a potent PKCiota (PKC-ι) inhibitor with an IC₅₀ of 2.8 nM. PKCiota-IN-2 formic also inhibits *PKC-α* and *PKC-ε* with IC₅₀s of 71 nM and 350 nM, respectively .

HY-122857

PKCiota-IN-1	PKC	Cancer
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 .

HY-P1372

PKC ζ pseudosubstrate

PKC Others

PKC ζ pseudosubstrate, a PKC ζ inhibitor peptide, can be attached to cell permeabilization vector peptide .

PKC ζ pseudosubstrate	PKC	Others
PKC ζ pseudosubstrate, a PKC ζ inhibitor peptide, can be attached to cell permeabilization vector peptide .

HY-139467

PF-04577806	SHP2 PKC	Metabolic Disease
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 .

HY-16982

Cercosporamide (-)-Cercosporamide	Fungal MNK PKC	Infection Cancer
Cercosporamide is a highly potent, ATP-competitive *PKC* kinase inhibitor targeting to *PKC1, with an IC₅₀* of <50 nM and a K_i of <7 nM. Cercosporamide is a unique Mnk inhibitor.

HY-P5885

PKCη pseudosubstrate inhibitor,myristoylated

PKC Others

PKCη pseudosubstrate inhibitor,myristoylated is cell permeable and can be used to study the mechanism of action of PKCη .

*PKCη pseudosubstrate inhibitor,myristoylated*	PKC	Others
PKCη pseudosubstrate inhibitor,myristoylated is cell permeable and can be used to study the mechanism of action of PKCη .

HY-18713A

CRT0066854 hydrochloride	PKC ROCK	Neurological Disease
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 .

HY-P5884

*PKCθ pseudosubstrate peptide inhibitor,myristoylated*	PKC	Others
PKCθ pseudosubstrate peptide inhibitor, myristoylated is a synthetic peptide that can be used to study the mechanism of action of PKCθ .

HY-108601A

(S)-Ro 32-0432	PKC	Neurological Disease Inflammation/Immunology
(S)-Ro 32-0432 is a potent, selective, ATP-competitive and orally active *PKC* inhibitor. The IC₅₀ values of (S)-Ro 32-0432 for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. (S)-Ro 32-0432 is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. (S)-Ro 32-0432 prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research .

HY-18713

CRT0066854
CRT0066854 is a potent and selective atypical PKC isoenzymes 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 .

HY-10195B

Ruboxistaurin hydrochloride 5+ Cited Publications LY333531 hydrochloride	PKC	Metabolic Disease
Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (K_i=2 nM). Ruboxistaurin hydrochloride exhibits ATP dependent competitive inhibition of PKC beta I with an IC₅₀ of 4.7 nM. Ruboxistaurin hydrochloride inhibits PKC beta II with an IC₅₀ of 5.9 nM .

HY-10195

Ruboxistaurin 5+ Cited Publications LY333531	PKC	Metabolic Disease
Ruboxistaurin (LY333531) is an orally active, selective PKC beta inhibitor (K_i=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 .

HY-131900

*Protein kinase inhibitor* H-7**	PKC	Cancer
Protein kinase inhibitor H-7 is a potent inhibitor of protein kinase C (PKC) and cyclic nucleotide dependent protein kinase, with a K_i of 6 μM for PKC .

HY-P0154

Epsilon-V1-2 3 Publications Verification ε-V1-2; EAVSLKPT
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 .

HY-117366

PS432	PKC	Cancer
PS432 is a *PKC* inhibitor with IC₅₀s of 16.9 μM (PKCι) and 18.5 μM (PKCζ), respectively. PS432 effectively inhibits the proliferation of non-small cell lung cancer cells (NSCLCs) and tumor growth in mouse xenograft models .

HY-P3201

PKCζ/ι pseudosubstrate inhibitor	Pyruvate Kinase	Neurological Disease
PKCζ/ι pseudosubstrate inhibitor has broad-spectrum effects on the *PKC* enzyme family and can induce memory impairment .

HY-108601

(S)-Ro 32-0432 free base	PKC	Inflammation/Immunology
(S)-Ro 32-0432 free base is a potent, selective, ATP-competitive and orally active *PKC* inhibitor. The IC₅₀ values of (S)-Ro 32-0432 free base for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. (S)-Ro 32-0432 free base is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. (S)-Ro 32-0432 free base prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research .

HY-147712

PKC-IN-4	PKC	Inflammation/Immunology
PKC-IN-4 (compound 7l) is a potent and orally active aPKC inhibitor with an IC₅₀ of 0.52 µM. PKC-IN-4 inhibits TNF-α induced NF-κB activity in vitro. PKC-IN-4 blocks VEGF- and TNFα-induced permeability across the retinal vasculature .

HY-132304

CC-90005	PKC	Inflammation/Immunology
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 inhibiting IL-2 expression .

HY-D1493

FIM-1	PKC	Others
FIM-1 is a fluorescent *PKC* (protein kinase C) probe that can be used for mitochondrial staining. FIM-1 inhibits PKC and acts as ATP-competitive catalytic site inhibitor .

HY-10195A

Ruboxistaurin mesylate 5+ Cited Publications LY333531 mesylate	PKC	Cardiovascular Disease Metabolic Disease
Ruboxistaurin (LY333531) mesylate is an orally active, selective and ATP competitive PKCβ inhibitor with IC₅₀ values of 4.7 and 5.9 nM for PKCβI and PKCβII, respectively. Ruboxistaurin mesylate can be used for the research of eye disorders, heart failure and diabetes .

HY-144307

Aurora A/PKC-IN-1	Aurora Kinase PKC	Cancer
Aurora A/PKC-IN-1 (Compound 2e) is a potent dual inhibitor of Aurora A (AurA) and PKC (α, β1, β2, and θ) kinases with IC₅₀s of 6.9 nM and 16.9 nM for AurA and PKCα, respectively. Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells and antimetastatic activity .

HY-10195BS

Ruboxistaurin-d6 hydrochloride	Isotope-Labeled Compounds PKC	Metabolic Disease
Ruboxistaurin-d₆ (hydrochloride) is the deuterium labeled Ruboxistaurin hydrochloride. Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin hydrochloride exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin hydrochloride inhibits PKC beta II with an IC50 of 5.9 nM[1][2].

Cat. No.	Product Name

HY-L164

Serine/Threonine Kinase Inhibitor Library

1286 compounds

Protein serine/threonine kinases (PSKs) are protein kinases that use ATP as a high-energy donor molecule to transfer phosphate groups to serine/threonine residues of target protein. As an important signal transduction regulator, serine/threonine kinases can affect the function of target proteins by disrupting enzyme activity or binding of target proteins to other proteins. Serine/threonine kinases are involved in the regulation of immune response, cell proliferation, differentiation, apoptosis and other physiological processes. Serine/threonine kinase inhibitors are an important class of compounds that have been widely studied in cancer, chronic inflammation, autoimmune diseases, aging and other diseases.

MCE designs a unique collection of 1286 serine/threonine kinase inhibitors, mainly targeting the receptor PKA, Akt, PKC, MAPK/ERK, etc, which is an effective tool for development and research of anti-cancer, anti-chronic inflammatory diseases, anti-autoimmune diseases and anti-aging compounds.

HY-L018

TGF-beta/Smad Compound Library

226 compounds

The transforming growth factor beta (TGF-β) signaling pathway is involved in many cellular processes in both the adult organism and the developing embryo including cell growth, cell differentiation, apoptosis, cellular homeostasis and other cellular functions. The TGF-β superfamily comprises TGF-βs, bone morphogenetic proteins (BMPs), activins and related proteins. Signaling begins with the binding of a TGF beta superfamily ligand to a TGF beta type II receptor. The type II receptor is a serine/threonine receptor kinase, which catalyzes the phosphorylation of the Type I receptor. The type I receptor then phosphorylates receptor-regulated SMADs (R-SMADs) which can now bind the coSMAD (e.g. SMAD4). R-SMAD/coSMAD complexes accumulate in the nucleus where they act as transcription factors and participate in the regulation of target gene expression. Deregulation of TGF-β signaling contributes to developmental defects and human diseases, including cancers, some bone diseases, chronic kidney disease, etc.

MCE designs a unique collection of 226 TGF-beta/Smad signaling pathway compounds. TGF-beta/Smad Compound Library acts as a useful tool for TGF-beta/Smad-related drug screening and disease research.

Cat. No.	Product Name	Target	Research Area

HY-P1286

PKC β pseudosubstrate

PKC Neurological Disease

PKC β pseudosubstrate is a selective cell-permeable inhibitor of PKC .

HY-P10085

PKC-ε translocation inhibitor peptide	PKC	Inflammation/Immunology
PKC-ε translocation inhibitor peptide is a PKC-ε translocation inhibitor. PKC-ε translocation inhibitor peptide can regulate the rate of FcγR-mediated internalization of opsonized beads, has no effect of FcαR trafficking .

HY-P5988

N-myristoyl-RKRTLRRL	PKC	Cancer
N-myristoyl-RKRTLRRL inhibits binding of *PKC* substrates. N-myristoyl-RKRTLRRL inhibits Ca ²⁺- and phosphatidylserine (PS)-dependent histone phosphorylation with IC₅₀ of 5 μM.? histone phosphorylation with IC₅₀ of 80 μM .

HY-P5886

PKC 20-28,myristoylated Myristoylated protein kinase C inhibitor 20-28	PKC	Cancer
PKC 20-28,myristoylated (Myristoylated protein kinase C inhibitor 20-28) is a cell-permeable *PKC* inhibitor that can be used in cancer research .

HY-P3199

*PKCβII Peptide Inhibitor* I**	PKC	Inflammation/Immunology
PKCβII Peptide Inhibitor I is a PKCβII inhibitor. PKCβII Peptide Inhibitor I shows cardioprotective effects in rat cardiac Ischemia/reperfusion injury model. PKCβII Peptide Inhibitor I also prevents vascular endothelial dysfunction .

HY-P1286A

PKC β pseudosubstrate TFA

PKC Neurological Disease

PKC β pseudosubstrate TFA is a selective cell-permeable inhibitor of PKC .

HY-P5888

*PKCε inhibitor* peptide,myristoylated** Myr‐PKCɛ-	PKC	Inflammation/Immunology
PKCε inhibitor peptide,myristoylated (Myr‐PKC?-) is a cell permeable myristic acid conjugated *PKC?* peptide inhibitor that attenuates NO release in cultured human umbilical vein endothelial cells (HUVECs) .

HY-P3816

PKCε Inhibitor Scramble Peptide

Peptides Others

PKCε Inhibitor Scramble Peptide is a scrambled peptide with identical amino acid composition to PKCε inhibitor peptide.
HY-P1372

PKC ζ pseudosubstrate

PKC Others

PKC ζ pseudosubstrate, a PKC ζ inhibitor peptide, can be attached to cell permeabilization vector peptide .

HY-P1402

[Glu27]-PKC (19-36)	Peptides	Others
[Glu27]-PKC (19-36) is an inactive control for protein kinase C (PKC) (19-36). PKC (19-36) is a pseudosubstrate peptide inhibitor of protein kinase C, it may be responsible for maintaining the enzyme in the inactive form in the absence of allosteric activators such as phospholipids .

HY-P5885

PKCη pseudosubstrate inhibitor,myristoylated

PKC Others

PKCη pseudosubstrate inhibitor,myristoylated is cell permeable and can be used to study the mechanism of action of PKCη .

HY-P5884

*PKCθ pseudosubstrate peptide inhibitor,myristoylated*	PKC	Others
PKCθ pseudosubstrate peptide inhibitor, myristoylated is a synthetic peptide that can be used to study the mechanism of action of PKCθ .

HY-P3201

PKCζ/ι pseudosubstrate inhibitor	Pyruvate Kinase	Neurological Disease
PKCζ/ι pseudosubstrate inhibitor has broad-spectrum effects on the *PKC* enzyme family and can induce memory impairment .

HY-P1288

Protein Kinase C (530-558) PKC fragment (530-558)	PKC	Others
Protein Kinase C (530-558), a peptide fragment of protein kinase C (PKC), is a potent *PKC* activator. Protein Kinase C (530-558) significantly inhibits osteoclastic bone resorption .

HY-P5881

*PKCα (C2-4) inhibitor* peptide**	PKC	Cardiovascular Disease
PKCα (C2-4) inhibitor peptide is a PKCα‐specific inhibitor peptide that blocks the inhibition of I_Kr by the α_1A‐adrenoreceptor agonist A-61603 (HY-101366) .

HY-P3892

Protein Kinase C (19-35) Peptide	PKC	Inflammation/Immunology
Protein Kinase C (19-35) Peptide is the *PKC* pseudosubstrate inhibitor/region. Protein Kinase C (19-35) Peptide possibly blocks the substrate-binding site in its kinase domain, makes the cytoplasmic form of *PKC* inactive .

HY-P3770

Phosphate acceptor peptide

PKC Others

Phosphate acceptor peptide is a substrate for cAMP-dependent protein kinase (PKA). phosphate acceptor peptide is also a weak PKC inhibitor .
HY-P1289A

[Ala107]MBP(104-118)

PKC Others

[Ala107]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC₅₀s ranging from 46-145 μM .
HY-P1289

[Ala113]MBP(104-118)

PKC Others

[Ala113]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC₅₀s ranging from 28-62 μM .
HY-P1289C

[Ala113]MBP(104-118) TFA

PKC Others

[Ala113]MBP(104-118) TFA is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC₅₀s ranging from 28-62 μM .
HY-P1289B

[Ala107]MBP(104-118) TFA

PKC Others

[Ala107]MBP(104-118) TFA is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC₅₀s ranging from 46-145 μM .

HY-P3083

N-Myristoyl-Lys-Arg-Thr-Leu-Arg	PKC	Inflammation/Immunology
N-Myristoyl-Lys-Arg-Thr-Leu-Arg is a protein kinase C (PKC) inhibitor with an IC₅₀ value of 75 μM. N-Myristoyl-Lys-Arg-Thr-Leu-Arg inhibits IL-2 receptor induction and IL-2 production in the human leukemic cell line Jurkat .

HY-P1746

Protein Kinase C (19-31) PKC (19-31)	PKC	Inflammation/Immunology
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), is used as protein kinase C substrate peptide for testing the protein kinase C activity .

HY-P1401

Protein Kinase C (19-36)	PKC	Metabolic Disease
Protein Kinase C (19-36) is a pseudosubstrate peptide inhibitor of protein kinase C (PKC), with an IC₅₀ of 0.18 μM. Protein Kinase C (19-36) markedly attenuated vascular hyperproliferation and hypertrophy as well as glucose-induced suppression of natriuretic peptide receptor response .

HY-P1746A

Protein Kinase C (19-31) (TFA) PKC (19-31) (TFA)	PKC	Inflammation/Immunology
Protein Kinase C (19-31) TFA, a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31), is used as protein kinase C substrate peptide for testing the protein kinase C activity .

HY-P5452

PKCd (8-17)	Peptides	Others
PKCd (8-17) is a biological active peptide. (This peptide is derived from the V1 domain of protein kinase C (PKC)d. It inhibits phorbol 12-myristate 13-acetate (PMA)-induced PKCd translocation and activation. Inhibition of PKCd reduces ischemia damage in cardiac and cerebral cells, induces proliferation of fibroblasts, and inhibits graft coronary artery disease in mice.)

HY-P1597

Malantide	PKA PKC	Cancer
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 K_m 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 K_m of 16 μM .

HY-P1597A

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

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-18980

Rottlerin 5+ Cited Publications Mallotoxin; NSC 56346; NSC 94525	Structural Classification Chalcones Flavonoids Classification of Application Fields Source classification Phenols Polyphenols Euphorbiaceae Plants Disease Research Fields Mallotus philippensis Cancer	PKC Autophagy Apoptosis HIV RABV
Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific *PKC* inhibitor, with IC₅₀ values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation . Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection .

HY-16982

Cercosporamide (-)-Cercosporamide	Infection Structural Classification Natural Products Microorganisms Classification of Application Fields Source classification Phenols Polyphenols Manihot esculenta Crantz Euphorbiaceae Plants Disease Research Fields	Fungal MNK PKC
Cercosporamide is a highly potent, ATP-competitive *PKC* kinase inhibitor targeting to *PKC1, with an IC₅₀* of <50 nM and a K_i of <7 nM. Cercosporamide is a unique Mnk inhibitor.

HY-N11003

Vanicoside A	Structural Classification Polygonaceae Source classification Phenols Polyphenols Plants Persicaria orientalis (L.) Spach	PKC
Vanicoside A is a protein kinase C(PKC) inhibitor from Polygonum pensylvanicum .

HY-N0278

Anemonin Pulsatilla camphor; Anemonine; trans-Anemonin	Structural Classification Natural Products Source classification Ranunculaceae Clematis crassifolia Benth. Plants	PKC NO Synthase
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 .

HY-108262

UCN-02 7-epi-Hydroxystaurosporine	Structural Classification Microorganisms Classification of Application Fields Antibiotics Source classification Antibacterial Disease Research Disease Research Fields Other Antibiotics Cancer	PKC PKA
UCN-02 (7-epi-Hydroxystaurosporine) is a selective protein kinase C (PKC) inhibitor produced by Streptomyces strain N-12, with IC₅₀s of 62 nM and 250 nM for PKC and protein kinase A (PKA), respectively. UCN-02 (7-epi-Hydroxystaurosporine) displays cytotoxic effect on the growth of HeLa S3 cells .

HY-N0021

Verbascoside 5+ Cited Publications Acteoside; Kusaginin; TJC160	Structural Classification Neurological Disease Classification of Application Fields Acanthaceae Anti-aging Phenols Polyphenols Plants Acanthus mollis L. Inflammation/Immunology Disease Research Fields Cancer	PKC Apoptosis Bacterial HSV
Verbascoside is isolated from Acanthus mollis, acts as an ATP-competitive inhibitor of *PKC, with an IC₅₀* of 25 µM, and has antitumor, anti-inflammatory and antineuropathic pain activity.

HY-N10393

Vibsanin A	Structural Classification Natural Products Classification of Application Fields Viburnaceae Source classification Viburnum awabuki K. Koch Plants Disease Research Fields Cancer	PKC HSP
Vibsanin A, a protein kinase C (PKC) activator, exhibits anti-proliferative activity against human cancer cell lines. Vibsanin A is also a HSP90 inhibitor .

HY-100618

Hispidin 1 Publications Verification	Cardiovascular Disease Structural Classification Microorganisms Classification of Application Fields Source classification Phenols Polyphenols Endogenous metabolite Disease Research Fields	PKC Endogenous Metabolite
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 .

HY-118384

Sangivamycin 2 Publications Verification NSC 65346; BA-90912	Structural Classification Natural Products Microorganisms Classification of Application Fields Source classification Disease Research Fields Cancer	PKC Nucleoside Antimetabolite/Analog
Sangivamycin (NSC 65346), a nucleoside analog, is a potent inhibitor of protein kinase C (PKC) with an K_i of 10 μM. Sangivamycin has potent antiproliferative activity against a variety of human cancers .

HY-N2575

Hypocrellin A 1 Publications Verification	Infection Natural Products other families Microorganisms Classification of Application Fields Source classification Phenols Polyphenols Plants Disease Research Fields	PKC Bacterial Parasite
Hypocrellin A, a naturally occurring *PKC* inhibitor, has many biological and pharmacological properties, such as antitumour, antiviral, antibacterial, and antileishmanial activities. Hypocrellin A is a promising photosensitizer for anticancer photodynamic therapy (PDT) .

HY-13626

Spisulosine ES-285	Alkaloids Classification of Application Fields Animals Source classification Marine natural products Other marine organisms Disease Research Fields Cancer	PKC
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 PKCζ activation .

HY-N2110

Phellopterin	Classification of Application Fields Source classification Coumarins Phenylpropanoids Plants Umbelliferae Helogyne apaloidea Nutt. Inflammation/Immunology Disease Research Fields	Akt
Phellopterin is a natural product isolated from Angelica dahurica. Phellopterin reduces TNF-alpha-induced VCAM-1 expression through regulation of the Akt and PKC pathway, which contributes to inhibit the adhesion of monocytes to endothelium .

HY-N8306

Isojacareubin	Structural Classification Flavonoids Flavones Source classification Guttiferae Plants Hypericum japonicum Thunb. ex Murray	Bacterial PKC Apoptosis SARS-CoV
Isojacareubin can be isolated from Hypericum japonicum. Isojacareubin covalently inhibits SARS-CoV-2 3CLpro. Isojacareubin also has anti-helicobacter activity. Isojacareubin inhibits *PKC, and suppresses hepatocellular carcinoma metastasis and induces apoptosis* .

HY-N8475

6-Deoxyisojacareubin	Structural Classification Flavonoids Source classification Guttiferae Plants Other Flavonoids Garcinia nervosa (Miq.) Miq.	PKC
6-Deoxyisojacareubin is a *PKC* inhibitor that inhibits the proliferation of QGY-7703 cells in a concentration-dependent manner. 6-Deoxyisojacareubin is also a natural product that can be obtained from Garcinia nervosa. 6-Deoxyisojacareubin can be used in cancer research .

HY-121197

Balanol Ophiocordin; Azepinostatin	Structural Classification Natural Products Microorganisms Source classification	PKA PKC
Balanol (Ophiocordin; Azepinostatin) is a potent and ATP competitive *PKC/PKA* inhibitor against human *PKC* isozymes α, β-I, β-II, γ, δ, ε, η (IC₅₀s=4-9 nM) and ζ (IC₅₀=150 nM). Balanol also blocks the phosphorylation of cyclic AMP response element-binding protein (CREB) and myristoylated alanine-rich C kinase substrate (MARCKS). Balanol can be isolated from the fungus Verticillium balanoides .

HY-N6734

K-252b	Infection Alkaloids Microorganisms Classification of Application Fields Source classification Disease Research Fields Indole Alkaloids	PKC
K-252b, an indolocarbazole isolated from the actinomycete Nocardiopsis, is a *PKC* inhibitor. K-252b can be used to inhibit extracellular kinases of cells in culture because it can’t pass through cell membrane freely .

HY-15141

Staurosporine Maximum Cited Publications 92 Publications Verification Antibiotic AM-2282; STS; AM-2282	Infection Alkaloids Structural Classification Microorganisms Classification of Application Fields Source classification Marine natural products Disease Research Fields Marine microorganism Indole Alkaloids	PKC PKA Apoptosis Bacterial Fungal Antibiotic
Staurosporine is a potent, ATP-competitive and non-selective inhibitor of protein kinases with IC₅₀s of 6 nM, 15 nM, 2 nM, and 3 nM for *PKC, PKA, c-Fgr, and Phosphorylase kinase* respectively. Staurosporine also inhibits TAOK2 with an IC₅₀ of 3 μM. Staurosporine is an apoptosis inducer .

HY-118442

Sphingosine (d14:1) Tetradecasphing-4-enine	Natural Products Classification of Application Fields Animals Source classification Disease Research Fields Cancer	PKC
Sphingosine (d14:1) (Tetradecasphing-4-enine), a sphingolipid, is a potent Protein kinase C (PKC) inhibitor. Sphingosine (d14:1) prevents its interaction with sn-1,2-diacylglycerol (DAG)/Phorbol esters .

HY-133680

β-Tocopherol	Monophenols Classification of Application Fields Source classification Phenols Metabolic Disease Plants Palmae Disease Research Fields Trachycarpus fortunei (Hook.) H. Wendl.	Tyrosinase
β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol .

HY-N0453

Hypericin 2 Publications Verification	Natural Products Classification of Application Fields Source classification Guttiferae Phenols Polyphenols Hyperlcurn perforatum L. Plants Disease Research Fields Cancer	Apoptosis Influenza Virus Antibiotic Monoamine Oxidase PKC Cytochrome P450 Dopamine β-hydroxylase Reverse Transcriptase Telomerase
Hypericin is a naturally occurring substance found in Hyperlcurn perforatum L. Hypericin is an inhibitor of *PKC* (protein kinase C), MAO (monoaminoxidase), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450). Hypericin shows antitumor, antiviral, antidepressive activities, and can induce apoptosis .

HY-126419

Kobophenol A	Infection Classification of Application Fields Source classification Cyperaceae Phenols Polyphenols Plants Disease Research Fields Carex kobomugi Ohwi	SARS-CoV PKC
Kobophenol A, an oligomeric stilbene, blocks the interaction between the ACE2 receptor and S1-RBD with an IC₅₀ of 1.81 μM and inhibits SARS-CoV-2 viral infection in cells with an EC₅₀ of 71.6 μM. Kobophenol A inhibits the activity of partially purified rat brain protein kinase C (PKC) with an IC₅₀ of 52 µM .

HY-129099

N-Desmethyltamoxifen	Structural Classification Alkaloids Classification of Application Fields Other Alkaloids Source classification Endogenous metabolite Disease Research Fields Cancer	PKC Estrogen Receptor/ERR Drug Metabolite Endogenous Metabolite
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 .

HY-129099A

N-Desmethyltamoxifen hydrochloride	Structural Classification Alkaloids Classification of Application Fields Other Alkaloids Source classification Endogenous metabolite Disease Research Fields Cancer	PKC Estrogen Receptor/ERR Drug Metabolite Endogenous Metabolite
N-Desmethyltamoxifen hydrochloride 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 hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation .

HY-N6736

K-252c	Infection Alkaloids Structural Classification Microorganisms Classification of Application Fields Source classification Disease Research Fields Indole Alkaloids	Beta-lactamase PKC Bacterial Apoptosis
K-252c, a staurosporine analog isolated from Nocardiopsis sp., is a cell-permeable *PKC* inhibitor, with an IC₅₀ of 2.45 µM. K-252c induces apoptosis in human chronic myelogenous leukemia cancer cells. K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase .

HY-N0551

Wedelolactone 10+ Cited Publications	Structural Classification Classification of Application Fields Alysicarpus ovalifolius (Schumacher) J. Leonard Phenols Polyphenols Plants Compositae Inflammation/Immunology Disease Research Fields	Caspase Lipoxygenase Apoptosis
Wedelolactone suppresses LPS-induced caspase-11 expression by directly inhibits the IKK Complex. Wedelolactone also inhibits 5-lipoxygenase (5-Lox) with an IC₅₀ of 2.5 μM. Wedelolactone induces caspase-dependent apoptosis in prostate cancer cells via downregulation of PKCε without inhibiting Akt. Wedelolactone can extract from Eclipta alba, and it can be used for the research of cancer .

HY-113068

(rel)-β-Tocopherol	Structural Classification Monophenols Microorganisms Classification of Application Fields Source classification Agrostidoideae Phenols Metabolic Disease Plants Disease Research Fields Triticum aestivum L.	Tyrosinase
(rel)-β-Tocopherol is a relative configuration of β-Tocopherol.(±)-β-Tocopherol is a lipid-soluble form of vitamin E with antioxidant activity. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol .

HY-N0453R

Hypericin (Standard)	Structural Classification Natural Products Classification of Application Fields Source classification Guttiferae Phenols Hyperlcurn perforatum L. Plants Disease Research Fields Cancer	Apoptosis Influenza Virus Antibiotic Monoamine Oxidase PKC Cytochrome P450 Dopamine β-hydroxylase Reverse Transcriptase Telomerase
Hypericin (Standard) is the analytical standard of Hypericin. This product is intended for research and analytical applications. Hypericin is a naturally occurring substance found in Hyperlcurn perforatum L. Hypericin is an inhibitor of *PKC* (protein kinase C), MAO (monoaminoxidase), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450). Hypericin shows antitumor, antiviral, antidepressive activities, and can induce apoptosis .

HY-13502

Mitoxantrone 15+ Cited Publications Mitozantrone; NSC 301739	Infection Quinones Structural Classification Classification of Application Fields Anthraquinones Source classification Endogenous metabolite Disease Research Fields Cancer	Topoisomerase PKC Orthopoxvirus Apoptosis Endogenous Metabolite
Mitoxantrone is a potent topoisomerase II inhibitor. Mitoxantrone also inhibits protein kinase C (PKC) activity with an IC₅₀ of 8.5 μM. Mitoxantrone induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone shows antitumor activity . Mitoxantrone also has anti-orthopoxvirus activity with EC₅₀s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .

HY-13502A

Mitoxantrone dihydrochloride 15+ Cited Publications Mitozantrone dihydrochloride; NSC 301739 dihydrochloride	Infection Quinones Structural Classification Classification of Application Fields Anthraquinones Source classification Endogenous metabolite Disease Research Fields Cancer	Topoisomerase PKC Orthopoxvirus Apoptosis Endogenous Metabolite
Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC₅₀ of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity . Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC₅₀s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .

HY-13502B

Mitoxantrone diacetate Mitozantrone diacetate; NSC 301739 diacetate	Infection Quinones Structural Classification Classification of Application Fields Anthraquinones Source classification Endogenous metabolite Disease Research Fields Cancer	Topoisomerase PKC Orthopoxvirus Apoptosis Endogenous Metabolite
Mitoxantrone diacetate is a potent topoisomerase II inhibitor. Mitoxantrone diacetate also inhibits protein kinase C (PKC) activity with an IC₅₀ of 8.5 μM. Mitoxantrone diacetate induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone diacetate shows antitumor activity . Mitoxantrone diacetate also has anti-orthopoxvirus activity with EC₅₀s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .

HY-N2359

Chelerythrine	Alkaloids Structural Classification Classification of Application Fields Source classification Metabolic Disease Macleaya cordata (Willd.) R. Br. Plants Isoquinoline Alkaloids Inflammation/Immunology Disease Research Fields Papaveraceae	Beta-lactamase PKC Bcl-2 Family Apoptosis Autophagy
Chelerythrine is a natural alkaloid, acts as a potent and selective Ca ²⁺/phospholopid-dependent *PKC* antagonist, with an IC₅₀ of 0.7 μM . Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity . Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC₅₀ of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy .

HY-N2535

Coniferaldehyde 4-Hydroxy-3-methoxycinnamaldehyde	Structural Classification Monophenols other families Classification of Application Fields Simple Phenylpropanols Source classification Phenols Phenylpropanoids Plants Inflammation/Immunology Disease Research Fields	Keap1-Nrf2 Apoptosis
Coniferaldehyde (4-Hydroxy-3-methoxycinnamaldehyde) is an effective inducer of heme oxygenase-1 (HO-1). Coniferaldehyde inhibits LPS-induced apoptosis through the PKCα/β II/Nrf-2/HO-1 dependent pathway in RAW264.7 macrophage cells. Coniferaldehyde has antioxidant and anti-inflammatory activities .

HY-N12466

3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine	Structural Classification Alkaloids Microorganisms Source classification Indole Alkaloids	PKC p38 MAPK ROCK
3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine (Compound 7) is an inhibitor of protein kinases, with IC₅₀s of 0.092, 0.26, 0.77 μM for PKC-α, ROCK, ASK1. 3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine shows potent cytotoxicity against PC-3 cancer cells with an IC₅₀ value of 0.16 μM .

HY-N0281

Daphnetin 3 Publications Verification 7,8-Dihydroxycoumarin	Classification of Application Fields Daphne Thymelaeaceae Source classification Coumarins Phenols Polyphenols Phenylpropanoids Plants Disease Research Fields Cancer	EGFR PKA PKC Autophagy Apoptosis AMPK Akt mTOR Reactive Oxygen Species Caspase Bcl-2 Family PARP Parasite
Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC₅₀s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1ß, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .

HY-N5072

Desmethylglycitein 4',6,7-Trihydroxyisoflavone	Flavonoids Classification of Application Fields Leguminosae Glycine max (L.) merr Source classification Phenols Polyphenols Plants Disease Research Fields Isoflavones Cancer	CDK PI3K PKC
Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities. Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity . Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1) . Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes .

Cat. No.	Product Name	Chemical Structure

HY-10230S

Midostaurin-d5
Midostaurin-d₅ is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM[1].

HY-10195BS

Ruboxistaurin-d6 hydrochloride
Ruboxistaurin-d₆ (hydrochloride) is the deuterium labeled Ruboxistaurin hydrochloride. Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin hydrochloride exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin hydrochloride inhibits PKC beta II with an IC50 of 5.9 nM[1][2].

HY-13502S

Mitoxantrone-d8
Mitoxantrone-d₈ (mitozantrone-d8) is the deuterium labeled Mitoxantrone. Mitoxantrone is a topoisomerase II inhibitor and also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM[1][2].

HY-13626S

Spisulosine-d3
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

HY-101047S

D-erythro-Sphingosine-d7
D-erythro-Sphingosine-d₇ is the deuterium labeled D-erythro-Sphingosine. D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator[1][2][3][4].

HY-108263S

3-Hydroxy Midostaurin-d5
3-Hydroxy Midostaurin-d₅ is a deuterium labeled 3-Hydroxy Midostaurin. 3-Hydroxy Midostaurin is a metabolite of PKC412, which effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively[1].

HY-113068S

β-Tocopherol-d3
β-Tocopherol-d₃ is the deuterium labeled β-Tocopherol. β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol can also prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol[1][2][3].

HY-13502AS

Mitoxantrone-d8 dihydrochloride

Mitoxantrone-d₈ dihydrochloride is deuterated labeled Mitoxantrone dihydrochloride (HY-13502A). Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC₅₀ of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity . Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC₅₀s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks