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Isoforms Recommended:	PKCα

Results for "

PKC-α

" in MedChemExpress (MCE) Product Catalog:

By Targets:	PKC (34) Angiotensin-converting Enzyme (ACE) (1) Apoptosis (5) Aurora Kinase (1) Autophagy (1) CDK (1) Endogenous Metabolite (1) Glucosidase (1) GSK-3 (4) JAK (1) p38 MAPK (1) PI3K (1) ROCK (2) SHP2 (2) SphK (2)
By Research Areas:	Cancer (24) Cardiovascular Disease (4) Inflammation/Immunology (8) Metabolic Disease (5) Neurological Disease (7)

Inhibitors & Agonists

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Targets Recommended: PKC

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-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-P3766

Protein kinase C (alpha) peptide TFA	PKC	Others
Protein kinase C α peptide (TFA) is a peptide of *PKC-α. PKC*-α acts as a lipid-dependent ser/thr protein kinase, can modulate various cellular processes, including cell survival, proliferation, differentiation, migration, adhesion and so on .

HY-B0719

Ingenol Mebutate 1 Publications Verification Ingenol 3-angelate; PEP005	PKC	Inflammation/Immunology Cancer
Ingenol Mebutate is an active ingredient in Euphorbia peplus, acts as a potent *PKC* modulator, with K_is of 0.3, 0.105, 0.162, 0.376, and 0.171 nM for PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε, respectively, and has antiinflammatory and antitumor activity.

HY-148413

Aprinocarsen sodium ISIS 3521 sodium	PKC	Cancer
Aprinocarsen (ISIS 3521) sodium, a specific antisense oligonucleotide inhibitor of protein kinase C-alpha (PKC-α). Aprinocarsen sodium is a 20-mer oligonucleotide, it regulates cell differentiation and proliferation. Aprinocarsen sodium inhibits the growth of human tumor cell lines in nude mice. Aprinocarsen sodium shows the value as a chemotherapeutic compound of human cancers .

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-N12466

3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine	PKC p38 MAPK ROCK	Cancer
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-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 .

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-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-13689

Go 6983 Maximum Cited Publications 48 Publications Verification 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-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-N8018

Leucosceptoside A	PKC Glucosidase Angiotensin-converting Enzyme (ACE)	Neurological Disease Metabolic Disease
Leucosceptoside A is a phenylethanoid glycoside with anti-hyperglycemic and anti-hypertensive activities. Leucosceptoside A shows inhibitory activity against α-glucosidase and *PKCα* (IC₅₀ of 19.0 μM) .

HY-117393

Bisindolylmaleimide III	PKC	Cancer
Bisindolylmaleimide III is a potent and selective inhibitor of protein kinase C (PKC). Bisindolylmaleimide III selectively interacts with either PKCα or ribosomal S6 protein kinase 1 after activation of these kinases .

HY-100207

CP21R7 4 Publications Verification CP21	GSK-3	Cancer
CP21R7 is potent GSK-3β inhibitor, with an IC₅₀ of 1.8 nM; CP21R7 also shows inhibitory activitiy against *PKCα, with an IC₅₀* of 1900 nM.

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 PKC*ε, 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-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-101569

Darovasertib 3 Publications Verification 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-149490

AJH-836	PKC	Neurological Disease
AJH-836 is an activator of Munc13-1 and PKC ε/α (K_d: 4.5 nM for PKCα) . AJH-836 triggers the translocation of Munc13-1 from the cytoplasm to the plasma membrane. AJH-836 can be used for research of neurodegenerative diseases .

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-P1088

[Ser25] Protein Kinase C (19-31)	PKC	Others
[Ser25] Protein Kinase C (19-31) is a substrate of protein kinase C (PKC) (K_m: 0.3 μM). [Ser25] Protein Kinase C (19-31) is derived from the pseudo-substrate regulatory domain of PKCα (19-31) with a Serine at position 25 replacing the wild-type Alanine .

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-108264

TCS 21311 NIBR3049	JAK PKC GSK-3	Cancer
TCS 21311 (NIBR3049) is a potent, highly selective JAK3 inhibitor with an IC₅₀ of 8 nM, it displays >100-fold selectivity over JAK1, JAK2 and TYK2. TCS 21311 (NIBR3049) inhibits *PKCα, PKCθ, and GSK3β* with IC₅₀s of 13, 68, and 3 nM, respectively .

HY-126477

NNK	Endogenous Metabolite	Cancer
NNK is a nicotine-nitrosated derivative. NNK simultaneously stimulates Bcl2 phosphorylation exclusively at Ser ⁷⁰ and c-Myc at Thr ⁵⁸ and Ser ⁶² through activation of both ERK1/2 and *PKCα* . NNK induces survival and proliferation of human lung cancer cells. NNK can be used for lung cancer mice model structure .

HY-117800

BJE6-106 1 Publications Verification B106	PKC Apoptosis	Inflammation/Immunology Cancer
BJE6-106 (B106) is a potent, selective 3 ^rd generation PKCδ inhibitor with an IC₅₀ of 0.05 μM and targets selectivity over classical PKC isozyme PKCα (IC₅₀=50 μM). BJE6-106 (B106) induces caspase-dependent apoptosis. BJE6-106 (B106) possesses tumor-specific effect.

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 IC₅₀*s 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-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-103045

CMPD101 3 Publications Verification	PKC ROCK	Cardiovascular Disease
CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC₅₀ of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC₅₀s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure .

HY-119016

SK1-I 1 Publications Verification BML-258	SphK	Cancer
SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a K_i value of 10 µM . SK1-I shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I enhances autophagy and has antitumor activity .

HY-119016A

SK1-I hydrochloride 1 Publications Verification BML-258 hydrochloride	SphK	Cancer
SK1-I hydrochloride (BML-258 hydrochloride), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a K_i value of 10 µM . SK1-I hydrochloride shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I hydrochloride enhances autophagy and has antitumor activity .

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-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-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-149489

JH-131e-153	Others	Neurological Disease
JH-131e-153, a diacylglycerol (DAG)-lactone, is a small molecule activator of Munc13-1, targeting the C1 domain. The activation sequence of JH-131e-153 on Munc13-1 is WT>I590≈R592A≈W588A. The C1 domain of Munc13-1 and protein kinase C (PKC) are homologous in sequence and structure. The activation sequence of JH-131e-153 on Munc13-1 and PKC was PKCα>Munc13-1>PKCε. JH-131e-153 regulates neuronal processes through Munc13-1 and can be further used in the study of neurodegenerative diseases .

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) .

Protein kinase C (alpha) peptide TFA	PKC	Others
Protein kinase C α peptide (TFA) is a peptide of *PKC-α. PKC*-α acts as a lipid-dependent ser/thr protein kinase, can modulate various cellular processes, including cell survival, proliferation, differentiation, migration, adhesion and so on .

[Ser25] Protein Kinase C (19-31)	PKC	Others
[Ser25] Protein Kinase C (19-31) is a substrate of protein kinase C (PKC) (K_m: 0.3 μM). [Ser25] Protein Kinase C (19-31) is derived from the pseudo-substrate regulatory domain of PKCα (19-31) with a Serine at position 25 replacing the wild-type Alanine .

Ingenol Mebutate 1 Publications Verification Ingenol 3-angelate; PEP005	Structural Classification Classification of Application Fields Terpenoids Euphorbia peplus Linn. Diterpenoids Euphorbiaceae Plants Inflammation/Immunology Disease Research Fields	PKC
Ingenol Mebutate is an active ingredient in Euphorbia peplus, acts as a potent *PKC* modulator, with K_is of 0.3, 0.105, 0.162, 0.376, and 0.171 nM for PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε, respectively, and has antiinflammatory and antitumor activity.

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 .

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PKC-α

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