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PKC-IN-1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	PKC (27) Akt (1) Antibiotic (1) Apoptosis (6) Aurora Kinase (2) Autophagy (4) Bacterial (1) Caspase (1) CDK (2) DNA-PK (1) Endogenous Metabolite (2) FLT3 (2) Fungal (1) GLUT (1) HIV (1) Isotope-Labeled Compounds (1) NF-κB (2) PKA (1) Proteasome (1) Reference Standards (2) Reverse Transcriptase (1) SphK (2) Tau Protein (1) TNF Receptor (1)
By Research Areas:	Cancer (18) Infection (2) Inflammation/Immunology (5) Metabolic Disease (4) Neurological Disease (2)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: PKC Dan family AIM2 NEKs CD44

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-108604

Bisindolylmaleimide II Bis II	PKC	Metabolic Disease Cancer
Bisindolylmaleimide II is a general inhibitor of all PKC subtypes .

HY-120497

PKCζ-IN-1	PKC CDK	Cancer
PKCζ-IN-1 is a compound that inhibits PKCζ and CDK2, showing an IC50 value of 5.18 nM for PKCζ and 1.04 μM for CDK2, with significant selectivity of 200-fold. PKCζ-IN-1 can reduce the activity of CDK2 while inhibiting PKCζ.

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-P5884A

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

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 ^[1].

HY-167114

(Rac)-Aurora A/PKC-IN-1	Aurora Kinase PKC	Cancer
(Rac)-Aurora A/PKC-IN-1 (Compund 2e) is an orally active Aurora A and PKC (α, β1, β2 and θ) kinase inhibitor. (Rac)-Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells in vitro and antimetastatic activity in vivo ^[1].

HY-P10967

EGFR Peptide	PKC	Metabolic Disease
EGFR Peptide is a selective substrate peptide for PKC. EGFR Peptide can used to measure PKC activity .

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-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-129330

Sapintoxin D	PKC	Others
Sapintoxin D is a fluorescent phorbol ester that can be used to study the activation of protein kinase C (PKC). Sapintoxin D is a calcium-dependent PKC activator .

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-10539

Enzastaurin di(hydrochloride) LY317615 dihydrochloride	PKC Autophagy Apoptosis	Cancer
Enzastaurin (LY317615) dihydrochloride 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-P1595A

CREBtide TFA	PKA PKC	Metabolic Disease
CREBtide TFA is a CREB (cAMP response element binding protein)-like peptide. CREBtide TFA a synthetic 13 amino acid peptide, has been reported as a PKA and *PKC* substrate .

HY-10539B

Enzastaurin hydrochloride LY317615 hydrochloride	PKC Autophagy Apoptosis	Cancer
Enzastaurin (LY317615) hydrochloride 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-116060

RK-286D	Antibiotic PKC Bacterial Fungal	Infection
RK-286D is an antibiotic and a PKC inhibitor with antimicrobial activity. RK-286D shows inhibitory activities against bleb formation induced by PDBu (HY-18985) and in vitro *PKC* activity .

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-10342R

Enzastaurin (Standard) LY317615 (Standard)	Reference Standards PKC Autophagy Apoptosis	Cancer
Enzastaurin (Standard) is the analytical standard of Enzastaurin. This product is intended for research and analytical applications. 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-18739

Phorbol 12-myristate 13-acetate Maximum Cited Publications 480 Publications Verification PMA; 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 (Validated by MedChemExpress (MCE)) .

HY-108263

3-Hydroxy Midostaurin CGP52421	FLT3	Cancer
3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, 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. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412 .

HY-163362

HIV-1 inhibitor-65	Reverse Transcriptase PKC HIV	Infection
HIV-1 inhibitor-65 (compound 3c) is an inhibitor of HIV-1 (EC₅₀: 2.9 nM) and an activator of protein kinase C (PKC). HIV-1 inhibitor-65 inhibits syncytium formation (EC₅₀: 7.0 nM) and inhibits HIV-1 entry and HIV-1 reverse transcriptase ^[1].

HY-126477

NNK 1 Publications Verification	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-134963

SBI-0087702	PKC	Cancer
SBI-0087702 promots the cytoplasmic localization of ATF2 in melanoma cells. SBI-0087702-induced translocation of ATF2 to the mitochondria results in increased apoptosis due to loss of mitochondrial membrane integrity. SBI-0087702 also inhibits growth and motility of melanoma cells. SBI-0087702 was shown to inhibit ATF2 phosphorylation on Thr52 by PKCε .

HY-142943

DNA-PK-IN-1	DNA-PK	Cancer
DNA-PK-IN-1 is a potent inhibitor of DNA-PK. DNA-dependent protein kinase (DNA-PK) is a DNA-PK enzyme complex composed of Ku70/Ku80 heterodimer and DNA-dependent protein kinase catalytic subunit (DNA-PKcs). DNA-PK-IN-1 has the potential for the research of cancer diseases (extracted from patent WO2021136463A1, compound 1) ^[1].

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-126477R

NNK (Standard)	Reference Standards Endogenous Metabolite	Cancer
NNK (Standard) is the analytical standard of NNK. This product is intended for research and analytical applications. NNK is a nicotine-nitrosated derivative. NNK simultaneously stimulates Bcl2 phosphorylation exclusively at Ser70 and c-Myc at Thr58 and Ser62 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-18739R

Phorbol 12-myristate 13-acetate (Standard)	PKC SphK NF-κB	Inflammation/Immunology
Phorbol 12-myristate 13-acetate (Standard) is the analytical standard of Phorbol 12-myristate 13-acetate. This product is intended for research and analytical applications. 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 (Validated by MedChemExpress (MCE)) .

HY-W751180

3-Hydroxy Midostaurin-13C6 CGP52421-¹³C₆	Isotope-Labeled Compounds FLT3	Cancer
3-Hydroxy Midostaurin- ¹³C₆ (CGP52421- ¹³C₆) is the ¹³C-labeled 3-Hydroxy Midostaurin (HY-108263). 3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, 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. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412 .

HY-109076

Tigilanol tiglate EBC-46	PKC Caspase	Cancer
Tigilanol tiglate (EBC-46) is a protein kinase C (PKC)/C1 domain activator. Tigilanol tiglate is associated with mitochondrial/endoplasmic reticulum (ER) dysfunction, leading to activation of the unfolded protein response (UPRmt/ER) and subsequent induction of ATP depletion, organelles expansion, Caspase activation, gasdermin E cleavage, and terminal necrosis. Tigilanol tiglate, as a small anti-tumor molecule with immunomodulatory effects, can be used in the study of head and neck squamous cell carcinoma and soft tissue sarcoma ^[1] .

HY-168060

(8R)-8-Hydroxyepoxyboetirane A	PKC	Neurological Disease
(8R)-8-Hydroxyepoxyboetirane A is a neurogenic compound that interacts with *PKC δ-C1B. (8R)-8-Hydroxyepoxyboetirane A binds to the PKC* enzyme pocket via hydrogen bonds with Gly-253, Leu-251 and Thr242. (8R)-8-Hydroxyepoxyboetirane A induces NRG1 release and differentiation of NSC into neurons. (8R)-8-Hydroxyepoxyboetirane A is promising for research of neurological disorders ^[1].

HY-126257

AKT-IN-3	Akt Apoptosis	Cancer
AKT-IN-3 (compound E22) is a potent, orally active low hERG blocking Akt inhibitor, with 1.4 nM, 1.2 nM and 1.7 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1, P70S6K, and SGK. AKT-IN-3 (compound E22) induces apoptosis and inhibits metastasis of cancer cells ^[1].

HY-11009

CGP60474 5+ Cited Publications	CDK PKC	Cancer
CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC₅₀ values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive *PKC* inhibitor .

HY-139066

Punicic acid Trichosanic acid	TNF Receptor GLUT Proteasome Tau Protein PKC	Neurological Disease Metabolic Disease Inflammation/Immunology
Punicic acid is a bioactive compound of pomegranate seed oil. Punicic acid is an isomer of conjugated α-linolenic acid and ω-5 polyunsaturated fatty acids. Punicic acid has anti-inflammatory and antioxidant activities and can inhibit the expression of inflammatory mediators such as tumor necrosis factor α (TNF-α). Punicic acid can also reduce the formation of β-amyloid deposits and hyperphosphorylation of tau by increasing the expression of GLUT4 protein and inhibiting the overactivation of calpain, and is used to prevent and treat neurodegenerative diseases. In addition, punicic acid also has breast cancer inhibitor properties that depend on lipid peroxidation and *PKC* pathways .

Cat. No.	Product Name

HY-L188

Anti-Brain Cancer Compound Library	1,762 compounds
Although brain cancer only accounts for 2% of all tumors, it has a poor prognosis, high mortality and high recurrence rate. Brain cancer can be divided into primary brain cancer and secondary brain cancer. According to the location of the cancer, brain cancer can also be divided into: brain glioma, pituitary adenoma, schwannoma, craniopharyngioma, meningioma and so on. Glioma is the most common primary brain tumor, accounting for about 1/3 of all brain tumors. At present, brain cancer lacks precision targeted therapeutic drugs, and there is still a great clinical demand that has not been met. With the continuous development of high-throughput screening technology, it may be able to help develop effective anti-brain cancer drugs by screening compounds targeting PKC, PD-1, c-Met, PARP, etc targets. MCE designs a unique collection of 1,762 small molecules with definite or potential anti-brain cancer activity, which is an important tool for studying the pathological mechanism of brain cancer and developing drugs for brain cancer.

Anti-Brain Cancer Compound Library

1,762 compounds

Although brain cancer only accounts for 2% of all tumors, it has a poor prognosis, high mortality and high recurrence rate. Brain cancer can be divided into primary brain cancer and secondary brain cancer. According to the location of the cancer, brain cancer can also be divided into: brain glioma, pituitary adenoma, schwannoma, craniopharyngioma, meningioma and so on. Glioma is the most common primary brain tumor, accounting for about 1/3 of all brain tumors. At present, brain cancer lacks precision targeted therapeutic drugs, and there is still a great clinical demand that has not been met. With the continuous development of high-throughput screening technology, it may be able to help develop effective anti-brain cancer drugs by screening compounds targeting PKC, PD-1, c-Met, PARP, etc targets.

MCE designs a unique collection of 1,762 small molecules with definite or potential anti-brain cancer activity, which is an important tool for studying the pathological mechanism of brain cancer and developing drugs for brain cancer.

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* .

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

CREBtide TFA	PKA PKC	Metabolic Disease
CREBtide TFA is a CREB (cAMP response element binding protein)-like peptide. CREBtide TFA a synthetic 13 amino acid peptide, has been reported as a PKA and *PKC* substrate .

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 .

EGFR Peptide	PKC	Metabolic Disease
EGFR Peptide is a selective substrate peptide for PKC. EGFR Peptide can used to measure PKC activity .

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 .

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* .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-129330

Sapintoxin D	Structural Classification Natural Products Source classification Euphorbiaceae Shirakiopsis indica (Willd.) Esser Plants	PKC
Sapintoxin D is a fluorescent phorbol ester that can be used to study the activation of protein kinase C (PKC). Sapintoxin D is a calcium-dependent PKC activator .

HY-18739

Phorbol 12-myristate 13-acetate 475+ Cited Publications PMA; Phorbol myristate acetate	Ketones, Aldehydes, Acids Croton tiglium Linn. Source classification Euphorbiaceae Plants Inflammation/Immunology Disease Research Fields	PKC SphK NF-κB
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 (Validated by MedChemExpress (MCE)) .

HY-126477

NNK 1 Publications Verification	Structural Classification Alkaloids Classification of Application Fields Source classification Pyridine Alkaloids Endogenous metabolite Disease Research Fields Cancer	Endogenous Metabolite
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-139066

Punicic acid Trichosanic acid	Structural Classification Punica granatum L. Classification of Application Fields Ketones, Aldehydes, Acids Source classification Metabolic Disease Punicaceae Plants Disease Research Fields	TNF Receptor GLUT Proteasome Tau Protein PKC
Punicic acid is a bioactive compound of pomegranate seed oil. Punicic acid is an isomer of conjugated α-linolenic acid and ω-5 polyunsaturated fatty acids. Punicic acid has anti-inflammatory and antioxidant activities and can inhibit the expression of inflammatory mediators such as tumor necrosis factor α (TNF-α). Punicic acid can also reduce the formation of β-amyloid deposits and hyperphosphorylation of tau by increasing the expression of GLUT4 protein and inhibiting the overactivation of calpain, and is used to prevent and treat neurodegenerative diseases. In addition, punicic acid also has breast cancer inhibitor properties that depend on lipid peroxidation and *PKC* pathways .

HY-126477R

NNK (Standard)	Structural Classification Alkaloids Source classification Pyridine Alkaloids Endogenous metabolite	Reference Standards Endogenous Metabolite
NNK (Standard) is the analytical standard of NNK. This product is intended for research and analytical applications. NNK is a nicotine-nitrosated derivative. NNK simultaneously stimulates Bcl2 phosphorylation exclusively at Ser70 and c-Myc at Thr58 and Ser62 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-18739R

Phorbol 12-myristate 13-acetate (Standard)	Ketones, Aldehydes, Acids Croton tiglium Linn. Source classification Euphorbiaceae Plants	PKC SphK NF-κB
Phorbol 12-myristate 13-acetate (Standard) is the analytical standard of Phorbol 12-myristate 13-acetate. This product is intended for research and analytical applications. 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 (Validated by MedChemExpress (MCE)) .

Cat. No.	Product Name	Chemical Structure

HY-W751180

3-Hydroxy Midostaurin-13C6

3-Hydroxy Midostaurin- ¹³C₆ (CGP52421- ¹³C₆) is the ¹³C-labeled 3-Hydroxy Midostaurin (HY-108263). 3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, 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. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412 .

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PKC-IN-1

Inhibitors & Agonists

Screening Libraries

Peptides

NaturalProducts

Isotope-Labeled Compounds

Natural
Products