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Results for "

Protein kinase C

" in MCE Product Catalog:

93

Inhibitors & Agonists

2

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1

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17

Peptides

19

Natural
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42

Recombinant Proteins

5

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • 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-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) 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.
  • 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) 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) TFA 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.
  • HY-108136A
    Bisindolylmaleimide X hydrochloride

    BIM-X hydrochloride; Ro31-8425 hydrochloride

    PKC CDK Cardiovascular Disease
    Bisindolylmaleimide X hydrochloride (BIM-X hydrochloride) is a potent and selective protein kinase C (PKC) inhibitor. Bisindolylmaleimide X hydrochloride is a potent cyclin-dependent kinase 2 (CDK2) antagonist with an IC50 of 200 nM.
  • HY-105416
    Calphostin C

    UCN-1028C

    Antibiotic PKC Apoptosis Cancer Infection
    Calphostin C is a potent and specific inhibitor of protein kinase C. Calphostin C is an antitumor antibiotic. Calphostin C has 1000 times more inhibitory to protein kinase C with an IC50 of 0.05 μM than other protein kinases. Calphostin C induces apoptosis in some tumor cell lines. Calphostin C has potent cytotoxic activity and antitumor activity.
  • 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-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-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-108602
    Bryostatin 3

    PKC Cancer
    Bryostatin 3, a macrocyclic lactone, is a protein kinase C activator, with a Ki of 2.75 nM. Bryostatin 3 can block 12-O-tetradecanoylphorbol-13-acetate (TPA) inhibition of cell proliferation, yet did not block TPA-enhanced cell-substratum adhesion.
  • HY-129624A
    Bisindolylmaleimide VIII acetate

    Ro 31-7549 acetate; Bis VIII acetate

    PKC Apoptosis Cancer Inflammation/Immunology
    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-βI, PKC-βII, PKC-γ, PKC-ε, respectively. Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases.
  • HY-N0453
    Hypericin

    Apoptosis Influenza Virus Antibiotic Monoamine Oxidase PKC Cytochrome P450 Dopamine β-hydroxylase Reverse Transcriptase Telomerase Cancer Infection Neurological Disease
    Hypericin is a naturally occurring substance found in Hypericum. 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-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 Ki of 6 μM for PKC.
  • HY-100983
    Protein kinase inhibitor H-7 dihydrochloride

    PKC Cancer
    Protein kinase inhibitor H-7 dihydrochloride is a potent PKC (protein kinase C) inhibitor. At 100 μM, Protein kinase inhibitor H-7 dihydrochloride completely inhibits both TPA (skin tumour promoter, 12-O-tetradecanoylphorbol-13-acetate) and phospholipase C-induced ODC (ornithine decarboxylase).
  • HY-100984
    HA-100

    PKA PKC Myosin ROCK Cancer
    HA-100 is a potent protein kinase inhibitor, with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 also used as a ROCK inhibitor.
  • HY-100984A
    HA-100 hydrochloride

    PKA PKC Myosin ROCK Cancer
    HA-100 hydrochloride is a potent protein kinase inhibitor, with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 hydrochloride also used as a ROCK inhibitor.
  • HY-10183
    Go6976

    PKC Influenza Virus Cancer
    Go6976 is a Protein Kinase C (PKC) inhibitor, with an IC50 of 20 nM.
  • HY-112384
    Safingol

    L-threo-dihydrosphingosine

    PKC Cancer
    Safingol is a lyso-sphingolipid PKC (protein kinase C ) inhibitor.
  • HY-123979
    ζ-Stat

    NSC37044

    PKC Apoptosis Cancer
    ζ-Stat (NSC37044) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro.
  • HY-123979A
    ζ-Stat trisodium

    NSC37044 trisodium

    PKC Apoptosis Cancer
    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.
  • HY-P1821
    Myelin Basic Protein

    MHP4-14

    PKC Neurological Disease
    Myelin Basic Protein (MHP4-14), a synthetic peptide comprising residues 4-14 of myelin basic protein, is a very selective PKC substrate (Km=7 μM). Myelin Basic Protein is not phosphorylated by cyclic AMP-dependent protein kinase, casein kinases I and II, Ca 2+/calmodulin-dependent protein kinase II, or phosphorylase kinase, and can be routinely used for the assay of protein kinase C with low background in the crude tissue extracts.
  • HY-101962
    HNMPA

    Insulin Receptor Metabolic Disease
    HNMPA is a membrane impermeable insulin receptor tyrosine kinase inhibitor. HNMPA inhibits serine and tyrosine autophosphorylation by the human insulin receptor. HNMPA has no effect on protein kinase C or cyclic AMP-dependent protein kinase activities
  • HY-P1821A
    Myelin Basic Protein TFA

    MHP4-14 TFA

    PKC Neurological Disease
    Myelin Basic Protein (MHP4-14) TFA, a synthetic peptide comprising residues 4-14 of myelin basic protein, is a very selective PKC substrate (Km=7 μM). Myelin Basic Protein TFA is not phosphorylated by cyclic AMP-dependent protein kinase, casein kinases I and II, Ca 2+/calmodulin-dependent protein kinase II, or phosphorylase kinase, and can be routinely used for the assay of protein kinase C with low background in the crude tissue extracts.
  • HY-12359
    TPPB

    PKC Neurological Disease
    TPPB is a cell-permeable benzolactam-derived protein kinase C (PKC) activator with a Ki of 11.9 nM.
  • HY-13867
    Bisindolylmaleimide I

    GF109203X; Go 6850

    PKC Metabolic Disease Cancer
    Bisindolylmaleimide I (GF109203X) is a highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor with a Ki of 14 nM.
  • HY-133083
    BAY-474

    c-Met/HGFR Cancer
    BAY-474 is a tyrosine-protein kinase c-Met inhibitor. BAY-474 acts as an epigenetics probe.
  • HY-101047
    D-erythro-Sphingosine

    Erythrosphingosine; erythro-C18-Sphingosine; trans-4-Sphingenine

    PKC Phosphatase Endogenous Metabolite Cancer
    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.
  • HY-112782
    VTX-27

    PKC Inflammation/Immunology
    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.
  • HY-130516
    Cdc7-IN-4

    CDK Cancer
    Cdc7-IN-4 (compound I-C) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-C. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
  • HY-13977A
    PKR-IN-C16

    Apoptosis Neurological Disease
    PKR-IN-C16 (Compound C16) is a specific double-stranded RNA-dependent protein kinase (PKR) inhibitor. PKR-IN-C16 shows promising neuroprotective properties and can rescue acute brain lesions.
  • HY-13343
    ZM 336372

    Raf Apoptosis Cancer
    ZM 336372 is a potent inhibitor of the protein kinase c-Raf. The IC50 value is 0.07 μM in the standard assay, which contains 0.1 mM ATP.
  • HY-126146
    PKC-iota inhibitor 1

    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-115769
    1,2-Didecanoylglycerol

    PKC Endocrinology
    1,2-Didecanoylglycerol, a synthetic diacylglycerol, is metabolized by platelets to 1,2-didecanoylphosphatidic acid (PA10) and activates protein kinase C (PKC).
  • HY-N4322
    Decursinol angelate

    PKC Cancer Inflammation/Immunology
    Decursinol angelate, a cytotoxic and protein kinase C (PKC) activating agent from the root of Angelica gigas, possesses anti-tumor and anti-inflammatory activities.
  • HY-N10393
    Vibsanin A

    PKC HSP Cancer
    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-11010
    AS601245

    JNK Cancer Inflammation/Immunology Neurological Disease
    AS601245 is an orally active, selective, ATP competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. AS601245 exhibits 10- to 20-fold selectivity over c-src, CDK2, and c-Raf and more than 50- to 100-fold selectivity over a range of Ser/Thr- and Tyr-protein kinases. Neuroprotective properties.
  • HY-108262
    UCN-02

    7-epi-Hydroxystaurosporine

    PKC PKA Cancer
    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-112400
    Bisindolylmaleimide V

    BIM V

    Ribosomal S6 Kinase (RSK) Cancer
    Bisindolylmaleimide V is a cell-permeable negative control for protein kinase C inhibition studies with an IC50 value over 100 µM. Bisindolylmaleimide V blocks the activation of mitogen-stimulated protein kinase p70 s6k/p85 s6k (S6K) in vivo with an IC50 of 8 µM.
  • HY-118384
    Sangivamycin

    NSC 65346; BA-90912

    PKC Nucleoside Antimetabolite/Analog Cancer
    Sangivamycin (NSC 65346), a nucleoside analog, is a potent inhibitor of protein kinase C (PKC) with an Ki of 10 μM. Sangivamycin has potent antiproliferative activity against a variety of human cancers.
  • HY-P1399
    Pep2m, myristoylated

    Myr-Pep2m

    PKC Neurological Disease
    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).
  • 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-118131
    PKR-IN-C51

    Ser/Thr Protease Infection
    PKR-IN-C51(compound 51) is an ATP-competitive double-stranded RNA-activated protein kinase (PKR) inhibitor with an IC50 of 9 μM. PKR-IN-C51 inhibits intracellular PKR activation in a dose-dependent manner in primary mouse macrophages.
  • HY-150026
    Multi-kinase-IN-2

    VEGFR PDGFR FGFR c-Kit Akt Src Apoptosis Cancer
    Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity.
  • HY-101047S
    D-erythro-Sphingosine-d7

    Erythrosphingosine-d7; erythro-C18-Sphingosine-d7; trans-4-Sphingenine-d7

    PKC Phosphatase Endogenous Metabolite Cancer
    D-erythro-Sphingosine-d7 (Erythrosphingosine-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.
  • HY-15141
    Staurosporine

    Antibiotic AM-2282; STS; AM-2282

    PKC PKA Apoptosis Bacterial Fungal Antibiotic Cancer Infection
    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-19825
    Rebeccamycin

    Topoisomerase ADC Cytotoxin Cancer
    Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I and has negligible effect on protein kinase C and topoisomerase II.
  • HY-P1399A
    Pep2m, myristoylated TFA

    Myr-Pep2m TFA

    PKC Neurological Disease
    Pep2m, myristoylated TFA (Myr-Pep2m TFA) is a cell-permeable peptide. Pep2m, myristoylated TFA 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).
  • HY-108391
    C8-Ceramide

    N-Octanoyl-D-erythro-sphingosine

    Apoptosis PKC Autophagy Cancer Inflammation/Immunology
    C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro.
  • HY-13502S
    Mitoxantrone-d8

    Mitozantrone-d8; NSC 301739-d8

    Topoisomerase PKC Cancer
    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.
  • HY-N0699
    Daphnoretin

    Dephnoretin; Thymelol

    PKC Influenza Virus Infection
    Daphnoretin (Dephnoretin), isolated from Wikstroemia indica, possesses antiviral activity. Daphnoretin likes PMA, may direct activation of protein kinase C which in turn activated NADPH oxidase and elicited respiratory burst.
  • HY-107613
    R 59-022

    DKGI-I; Diacylglycerol kinase inhibitor I

    PKC 5-HT Receptor Inflammation/Immunology
    R 59-022 (DKGI-I) is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 is a 5-HTR antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
  • HY-108355
    R59949

    PKC Cancer
    R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol.
  • HY-119312
    C8 Dihydroceramide

    Others Cancer
    C8 Dihydroceramide is a negative control of C8 Ceramide. C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro.
  • HY-130530
    AP-C5

    Others Metabolic Disease
    AP-C5 displays selective inhibition of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 7.2, which can be used for the research of diarrheal disease.
  • HY-106262B
    Delcasertib hydrochloride

    KAI-9803 hydrochloride; BMS-875944 hydrochloride

    PKC Inflammation/Immunology Cardiovascular Disease
    Delcasertib (KAI-9803) hydrochloride is a potent and selective δ-protein kinase C (δPKC) inhibitor. Delcasertib (KAI-9803) hydrochloride could ameliorate injury associated with ischemia and reperfusion in animal models of acute myocardial infarction (MI).
  • HY-12048
    Chelerythrine chloride

    PKC Bcl-2 Family Apoptosis Autophagy Cancer Metabolic Disease Inflammation/Immunology
    Chelerythrine chloride is a potent, cell-permeable inhibitor of protein kinase C, with an IC50 of 660 nM. Chelerythrine chloride inhibits the Bcl-XL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from Bcl-XL. Chelerythrine chloride induces apoptosis and autophagy.
  • HY-106262
    Delcasertib

    KAI-9803; BMS-875944

    PKC Inflammation/Immunology Cardiovascular Disease
    Delcasertib (KAI-9803) is a potent and selective δ-protein kinase C (δPKC) inhibitor. Delcasertib (KAI-9803) could ameliorate injury associated with ischemia and reperfusion in animal models of acute myocardial infarction (MI).
  • HY-10206
    Amuvatinib

    MP470; HPK 56

    c-Kit PDGFR RAD51 FLT3 c-Met/HGFR RET Apoptosis Cancer
    Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
  • HY-10206A
    Amuvatinib hydrochloride

    MP470 hydrochloride; HPK 56 hydrochloride

    c-Kit PDGFR RAD51 FLT3 c-Met/HGFR RET Cancer
    Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib hydrochloride (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
  • HY-118834
    Teleocidin A1

    Lyngbyatoxin A

    PKC Cancer
    Teleocidin A1 (Lyngbyatoxin A), a highly toxic skin irritant, is a potent activator of protein kinase C (PKC). Teleocidin A1 shows antiproliferative activity against HeLa cancer cells (IC50=9.2 nM).
  • HY-N2344
    Procyanidin A1

    Proanthocyanidin A1

    PKC Inflammation/Immunology
    Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca 2+ influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects.
  • HY-131648
    1-Oleoyl-2-acetyl-sn-glycerol

    PKC Metabolic Disease
    1-Oleoyl-2-acetyl-sn glycerol is a synthetic, cell permeable diacylglycerol analog. 1-Oleoyl-2-acetyl-sn glycerol activates calcium-dependent protein kinase C (PKC) and induces the superoxide-production.
  • HY-13856
    (R)-PS210

    PDK-1 Cancer
    (R)-PS210, the R enantiomer of PS210 (compound 4h-eutomer), is a substrate-selective allosteric activator of PDK1 with an AC50 value of 1.8 μM. (R)-PS210 targets to the PIF-binding pocket of PDK1. PIF: The protein kinase C-related kinase 2 (PRK2)-interacting fragment.
  • HY-118442
    Sphingosine (d14:1)

    Tetradecasphing-4-enine

    PKC Cancer
    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-142830
    B-Raf IN 6

    Raf Cancer
    B-Raf IN 6 (compound 2c) is a potent inhibitor of protein kinase B-Raf with an IC50 of 1.7 nM. B-Raf IN 6 is devoid of binding to the secondary target PXR and resists rapid metabolism. B-Raf IN 6 has the potential for the research of cancer disease.
  • HY-15463
    Imatinib

    STI571; CGP-57148B

    Bcr-Abl PDGFR c-Kit SARS-CoV Autophagy Cancer
    Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
  • HY-138779
    ICCB-19 hydrochloride

    Autophagy RIP kinase Apoptosis Inflammation/Immunology
    ICCB-19 hydrochloride is a TRADD (TNFRSF1A associated via death domain) inhibitor. ICCB-19 hydrochloride binds with N-terminal domain of TRADD (TRADD-N), disrupting its binding to both TRADD-C and TRAF2. ICCB-19 hydrochloride is indirect inhibitor of RIPK1 kinase activity. ICCB-19 hydrochloride effectively induces autophagy and the degradation of long-lived proteins.
  • HY-101569
    Darovasertib

    LXS196; IDE196

    PKC Cancer
    Darovasertib (LXS196) is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. Darovasertib has the potential for uveal melanoma research.
  • HY-13434
    Ionomycin

    SQ23377

    Calcium Channel PKC Bacterial Apoptosis Antibiotic Cancer Infection
    Ionomycin (SQ23377) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. Ionomycin (SQ23377) is highly specific for divalent cations (Ca>Mg>Sr=Ba). Ionomycin (SQ23377) promotes apoptosis. Ionomycin also induces the activation of protein kinase C (PKC).
  • HY-W010983
    SC-236

    COX PPAR Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    SC-236 is an orally active COX-2 specific inhibitor (IC50 = 10 nM) and a PPARγ agonist. SC-236 suppresses activator protein-1 (AP-1) through c-Jun NH2-terminal kinase. SC-236 exerts anti-inflammatory effects by suppressing phosphorylation of ERK in a murine model.
  • HY-131275
    Imatinib Impurity E

    Others Others
    Imatinib Impurity E is the impurity of Imatinib. Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
  • HY-129099
    N-Desmethyltamoxifen

    PKC Estrogen Receptor/ERR Drug Metabolite Endogenous Metabolite Cancer
    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

    PKC Estrogen Receptor/ERR Drug Metabolite Endogenous Metabolite Cancer
    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-124761
    Poloppin

    Polo-like Kinase (PLK) Autophagy Cancer
    Poloppin is a potent, cell penetrant inhibitor of the mitotic Polo-like kinase (PLK) (IC50=26.9 μM) and prevents the protein-protein interaction via the Polo-box domain (PBD) (Kd= 29.5 μM). Poloppin selectively kills cells expressing mutant KRAS, enhancing death in mitosis. Poloppin is used for the study of KRAS-mutant cancers as single agents, or in combination with c-MET inhibitors.
  • HY-18981
    Decursin

    (+)-Decursin

    PKC Apoptosis CXCR Cancer Inflammation/Immunology Neurological Disease
    Decursin ((+)-Decursin) is a potent anti-tumor agent. Decursin also is a cytotoxic agent and a potent protein kinase C activator. Decursin induces apoptosis and cell cycle arrest at G1 phase. Decursin decreases the expression of CDK2, CDK4, CDK6, cyclin D1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities.
  • HY-18739
    Phorbol 12-myristate 13-acetate

    PMA; TPA; Phorbol myristate acetate

    PKC SphK NF-κB Inflammation/Immunology
    Phorbol 12-myristate 13-acetate (PMA), a phorbol ester, is a dual SphK and protein kinase C (PKC) activator. Phorbol 12-myristate 13-acetate is a NF-κB activator. Phorbol 12-myristate 13-acetate induces differentiation in THP-1 cells.
  • HY-107613S
    R 59-022-d5

    DKGI-I-d5; Diacylglycerol kinase inhibitor I-d5

    PKC 5-HT Receptor Inflammation/Immunology
    R 59-022-d5 (DKGI-I-d5) is the deuterium labeled R 59-022. R 59-022 (DKGI-I) is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 is a 5-HTR antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
  • 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 IL-2 expression.
  • HY-10230
    Midostaurin

    PKC412; CGP 41251

    PKC VEGFR c-Kit NO Synthase Apoptosis Cancer
    Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin 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. Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects.
  • HY-13434A
    Ionomycin calcium

    SQ23377 calcium

    Calcium Channel PKC Bacterial Apoptosis Antibiotic Cancer Infection
    Ionomycin calcium (SQ23377 calcium) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. Ionomycin calcium (SQ23377 calcium) is highly specific for divalent cations (Ca>Mg>Sr=Ba). Ionomycin (SQ23377) promotes apoptosis. Ionomycin calcium (SQ23377 calcium) also induces the activation of protein kinase C (PKC).
  • HY-126419
    Kobophenol A

    SARS-CoV PKC Infection
    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-108254
    Bisindolylmaleimide IV

    Arcyriarubin A

    PKC CMV Infection
    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). Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with an IC50 of 0.2 μM.
  • HY-50867
    Lestaurtinib

    CEP-701; KT-5555

    JAK FLT3 Trk Receptor Apoptosis STAT Cancer
    Lestaurtinib (CEP-701) is an orally active and selective RPTKs (receptor protein tyrosine kinase) inhibitor, competitively inhibits ATP binding to the TrkA/B/C domain. Lestaurtinib inhibits RPTKs phosphorylation, with IC50s of 2, 25 and 0.9 nM for FLT3, TrkA and JAK2, respectively. Lestaurtinib induces apoptosis and cycle arrest, also can inhibit growth of tumor.
  • HY-13502B
    Mitoxantrone diacetate

    Mitozantrone diacetate; NSC 301739 diacetate

    Topoisomerase PKC Orthopoxvirus Apoptosis Endogenous Metabolite Cancer Infection
    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-13502
    Mitoxantrone

    Mitozantrone; NSC 301739

    Topoisomerase PKC Orthopoxvirus Apoptosis Endogenous Metabolite Cancer Infection
    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-16558
    Butein

    2’,3,4,4’-tetrahydroxy Chalcone

    EGFR Autophagy Apoptosis Phosphodiesterase (PDE) Cancer
    Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60 c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).
  • HY-13502A
    Mitoxantrone dihydrochloride

    Mitozantrone dihydrochloride; NSC 301739 dihydrochloride

    Topoisomerase PKC Orthopoxvirus Apoptosis Endogenous Metabolite Cancer Infection
    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-108543
    NSC 95397

    Phosphatase Apoptosis Cancer
    NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor (Ki=32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C); IC50=22.3 nM (human Cdc25A), 56.9 nM (human Cdc25C), 125 nM (Cdc25B)). NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway.
  • HY-137295
    Ingenol 3,20-dibenzoate

    PKC Apoptosis Inflammation/Immunology
    Ingenol 3,20-dibenzoate is a potent protein kinase C (PKC) isoform-selective agonist. Ingenol 3,20-dibenzoate induces selective translocation of nPKC-delta, -epsilon, and -theta and PKC-mu from the cytosolic fraction to the particulate fraction and induces morphologically typical apoptosis through de novo synthesis of macromolecules. Ingenol 3,20-dibenzoate increases the IFN-γ production and degranulation by NK cells, especially when NK cells are stimulated by NSCLC cells.
  • HY-107024
    Osteogenic Growth Peptide (10-14)

    OGP(10-14); Historphin

    Src Others
    Osteogenic Growth Peptide (10-14) (OGP(10-14)), the C-terminal truncated pentapeptide of osteogenic growth peptide (OGP), retains the full OGP-like activity. Osteogenic Growth Peptide (10-14) is responsible for the binding to the OGP receptor and activates an intracellular Gi-protein-MAP kinase signaling pathway. Osteogenic Growth Peptide (10-14) is a potent mitogen and stimulator of osteogenesis and hematopoiesis. Osteogenic Growth Peptide (10-14) acts as a Src inhibitor.
  • HY-100434
    PD-161570

    FGFR PDGFR EGFR Src TGF-β Receptor Cancer Cardiovascular Disease
    PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor.
  • HY-107544
    8-pCPT-2'-O-Me-cAMP-AM

    PKA Metabolic Disease
    8-pCPT-2'-O-Me-cAMP-AM is a cyclic AMP analogue, selectively activates Epac-Rap signaling pathway. 8-pCPT-2'-O-Me-cAMP-AM protects renal function by activating Epac from ischemia injury. 8-pCPT-2'-O-Me-cAMP-AM also stimulates insulin secretion by interaction with PKA pathway.
  • HY-N5072
    Desmethylglycitein

    4',6,7-Trihydroxyisoflavone

    CDK PI3K PKC Cancer
    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.