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DGKα&ζ-IN-1 (Compound II) is a DGK target inhibitor. DGKα&ζ-IN-1 can enhance the function of T cells, and has a synergistic effect with PD-1, which has therapeutic effects IN both immune and tumor .
DGKζ-IN-4 is a DGK-zeta inhibitor. DGKζ-IN-4 can be used as an active component of pharmaceutical compositions. DGKζ-IN-4 is used to treat cancers associated with immune cell activation or cancers resistant to anti-PD-1 antibody/anti-PD-11 antibody treatment .
DGKζ-IN-1 (compound 9) is an inhibitor of DGKζ. DGKζ-IN-1 can be used for research in cancer related to immunocyte activation or cancer resistant to anti-PD-1 antibody/anti-PD-L1 antibody .
BMS-502 (Compound 22) is a potent dual inhibitor of diacylglycerol kinase (DGK) α and ζ with IC50 of 4.6 nM and 2.1 nM. BMS-502 enhanced T cell immune responses in mice. BMS-502 can be used in tumor immunity related research .
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 .
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 .
BAY 2965501 is a potent and selective diacylglycerol kinase zeta(DGKζ) inhibitor. BAY 2965501 induces pERK activation. BAY 2965501 can be used for the research of cancer .
(S)-BAY 2965501 is the left-handed isomer of BAY 2965501 (HY-153343). BAY 2965501 is a potent and selective diacylglycerol kinase zeta(DGKζ) inhibitor. BAY 2965501 induces pERK activation. BAY 2965501 can be used for the research of cancer .
Momordicine I, a triterpenoid compound extracted from momordica charantia L. Momordicine I alleviates isoproterenol-induced cardiomyocyte hypertrophy through suppression of PLA2G6 and DGK-ζ .
CU-3 is the racemate of (5Z,2E)-CU-3. (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells .
BMS-684 is a selective DGKα inhibitor with an IC50 of 15 nM. BMS-684 inhibits DGKα kinase activity with >100-fold selectivity over the related DGK type I family members DGKβ and DGKγ. BMS-684 does not inhibit any of the other seven DGK isozymes .
DGKα-IN-6 is a DGKα inhibitor with the IC50 of 1.377 nM, extracted from patent WO2022271650 (compound 143). DGKα-IN-6 has the potential for cancer study.
DGKα-IN-7 is a DGKα inhibitor with the IC50 of 6.225 nM, extracted from patent WO2022271684 (compound 100). DGKα-IN-7 has the potential for cancer study.
DGKα-IN-2 (example 48) is a DGKα inhibitor with the IC50 of 0.9 nM, extracted from patent WO2021105115. DGKα-IN-2 significantly enhances the anti-tumor effect of anti-PD-1 by increasing the proliferation and function of T cells. DGKα-IN-2 has the potential for cancer and immunology study.
DGKα-IN-3 (example 25) is a DGKα inhibitor with the IC50 of 283 nM, extracted from patent WO2021105115. DGKα-IN-2 significantly enhances the anti-tumor effect of anti-PD-1 by increasing the proliferation and function of T cells. DGKα-IN-2 has the potential for cancer and immunology study.
DGKα-IN-4 (example 432) is a DGKα inhibitor with the IC50 of 0.1 nM, extracted from patent WO2021105117. DGKα-IN-2 significantly enhances the anti-tumor effect of anti-PD-1 by increasing the proliferation and function of T cells. DGKα-IN-3 has the potential for cancer and immunology study.
DGKα-IN-8 (Example 51) is a DGKα inhibitor (IC50=22.491 nM; EC50=0.256 nM). DGKα-IN-8 can be used to study cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection .
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 .
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) .
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) .
AMB639752 is a potent DGKα inhibitor. AMB639752 restores restimulation induced cell death (RICD) in SAP deficient lymphocytes by inhibiting DGKα in intact cells. AMB639752 can be used for X-linked lymphoproliferative disease 1(XLP-1) research .
(5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells .
MY10 is a potent and orally active receptor protein tyrosine phosphatase (RPTPβ/ζ) inhibitor. MY10 attenuates binge-like ethanol consumption and ethanol reward .
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 .
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 .
Cladospirone bisepoxide is a metabolite that isolated from cultures of a fungus. Cladospirone bisepoxide displays selective antibiotic activity against several bacteria and fungi and inhibits germinations of Lepidium sativum at low concentrations .
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 .
JNJ-3790339, a Ritanserin (HY-10791) analog, is a potent and selective diacylglycerol kinase (DGKα) inhibitor with an IC50 of 9.6 μM. JNJ-3790339 has induction of toxicity in malignant cells, and improves ability to upregulate T cell activation .
9-β-D-Arabinofuranosylguanine is a Guanosine (HY-N0097) analog and shows high affinity for deoxyguanosine kinase (dGK) with a Km of 8.0 μM. 9-β-D-Arabinofuranosylguanine can be used for the research of T-cell lymphoblastic disease .
ZAP-180013 is a zeta-chain-associated protein kinase 70 (ZAP-70) inhibitor with an IC50 of 1.8 μM. ZAP-180013 inhibits the interaction of ZAP-70 SH2 domain with immunoreceptor tyrosine-based activation motif (ITAMs) .
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 .
R 59-022 (DKGI-I) is a DGK inhibitor (IC50: 2.8 µM). R 59-022 inhibits the phosphorylation of OAG to OAPA. R 59-022 is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils .
R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 µM). R 59-022 hydrochloride inhibits the phosphorylation of OAG to OAPA. R 59-022 hydrochloride is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils .
PS315, a derivative of PS48 (HY-15967), is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCη (IC50=30 μM). PS315 has anti-cancer activity .
MY33-3 is a potent and selective inhibitor of receptor protein tyrosine phosphatase (RPTP)β/ζ, with an IC50 of ~0.1 μM. MY33-3 also inhibits PTP-1B (IC50 ~0.7 μM). MY33-3 can reduce ethanol consumption and alleviate Sevoflurane-induced neuroinflammation and cognitive dysfunction .
MY33-3 hydrochloride is a potent and selective inhibitor of receptor protein tyrosine phosphatase (RPTP)β/ζ, with an IC50 of ~0.1 μM. MY33-3 hydrochloride also inhibits PTP-1B (IC50 ~0.7 μM). MY33-3 hydrochloride can reduce ethanol consumption and alleviate Sevoflurane-induced neuroinflammation and cognitive dysfunction .
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 .
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 .
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) .
Epoetin zeta is a derivative of the endogenous protein erythropoietin, acting as an erythropoiesis-stimulating agent. Epoetin zeta can be used for researching symptomatic anemia of renal origin, symptomatic renal anemia .
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) .
Momordicine I, a triterpenoid compound extracted from momordica charantia L. Momordicine I alleviates isoproterenol-induced cardiomyocyte hypertrophy through suppression of PLA2G6 and DGK-ζ .
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 .
Cladospirone bisepoxide is a metabolite that isolated from cultures of a fungus. Cladospirone bisepoxide displays selective antibiotic activity against several bacteria and fungi and inhibits germinations of Lepidium sativum at low concentrations .
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 .
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 .
The hemoglobin zeta subunit (HBAZ) protein acts as an α-type chain in mammalian embryonic hemoglobin. It contributes to the formation of heterotetramers and is involved in various developmental stages. Hemoglobin subunit zeta/HBAZ Protein, Human (His) is the recombinant human-derived Hemoglobin subunit zeta/HBAZ protein, expressed by E. coli , with N-6*His labeled tag. The total length of Hemoglobin subunit zeta/HBAZ Protein, Human (His) is 142 a.a., with molecular weight of ~15.0 kDa.
The COPZ1 protein is a key coating subunit essential for intracellular protein transport. In coat isoform complexes, it binds to a dilysine motif that facilitates reversible association with Golgi vesicles. COPZ1 Protein, Rat (His) is the recombinant rat-derived COPZ1 protein, expressed by E. coli , with N-His labeled tag. The total length of COPZ1 Protein, Rat (His) is 177 a.a., with molecular weight of ~22.4 KDa.
IFN-zeta/Limitin protein is a member of the alpha/beta interferon family. IFN-zeta/Limitin Protein, Mouse (HEK293, His) is the recombinant mouse-derived IFN-zeta/Limitin protein, expressed by HEK293 , with C-6*His labeled tag. The total length of IFN-zeta/Limitin Protein, Mouse (HEK293, His) is 161 a.a., with molecular weight of ~19 kDa.
PKCz proteins are involved in multiple cellular processes, including mitotic signaling, cell proliferation, cell polarity, inflammatory responses, and maintenance of long-term potentiation (LTP). PRKCZ Protein, Human (Sf9, GST) is the recombinant human-derived PKCz protein, expressed by Sf9 insect cells , with N-GST labeled tag. The total length of PRKCZ Protein, Human (Sf9, GST) is 591 a.a., .
DGKE protein is a membrane-bound diacylglycerol kinase that balances cell signaling by converting diacylglycerol (DAG) to phosphatidic acid (PA). As a central switch in signaling pathways, DGKE has opposite effects on various biological processes and significantly promotes complex lipid biosynthesis. DGKE Protein, Human (Cell-Free, His, SUMO, Myc) is the recombinant human-derived DGKE protein, expressed by E. coli Cell-free , with N-10*His, C-Myc, N-SUMO labeled tag. The total length of DGKE Protein, Human (Cell-Free, His, SUMO, Myc) is 567 a.a., with molecular weight of 83.9 kDa.
CD3 zeta/CD247 is a component of the TCR-CD3 complex and can transmit APC-induced TCR signals to initiate immune responses. CD3D, CD3E, CD3G, and CD3Z contain ITAMs that are phosphorylated by LCK and FYN upon TCR engagement, providing docking sites for ZAP70. CD3 zeta/CD247 Protein, Human (GST) is the recombinant human-derived CD3 zeta/CD247 protein, expressed by E. coli , with N-GST labeled tag. The total length of CD3 zeta/CD247 Protein, Human (GST) is 113 a.a., with molecular weight of 28-43 KDa.
The maleylacetoacetate isomerase/GSTZ1 protein is a member of the GST superfamily and detoxifies electrophilic molecules. It converts maleylacetoacetate to fumarylacetoacetate, a key step in phenylalanine/tyrosine degradation. Maleylacetoacetate isomerase/GSTZ1 Protein, Human (N-His) is the recombinant human-derived Maleylacetoacetate isomerase/GSTZ1 protein, expressed by E. coli , with N-6*His labeled tag. The total length of Maleylacetoacetate isomerase/GSTZ1 Protein, Human (N-His) is 215 a.a., with molecular weight of ~25 kDa.
IL-37 protein is an important immunoregulatory cytokine that suppresses innate inflammation and immune responses and reduces excessive inflammation. It signals intracellularly through nuclear translocation of SMAD3 and extracellularly through binding to its receptors, consisting of IL18R1 and IL18RAP. IL-37 Protein, Human is the recombinant human-derived IL-37 protein, expressed by E. coli , with tag free. The total length of IL-37 Protein, Human is 166 a.a., with molecular weight of ~18-20 kDa.
IL-37 protein is an important immunoregulatory cytokine that suppresses innate inflammation and immune responses and reduces excessive inflammation. It signals intracellularly through nuclear translocation of SMAD3 and extracellularly through binding to its receptors, consisting of IL18R1 and IL18RAP. Animal-Free IL-37 Protein, Human (His) is the recombinant human-derived animal-FreeIL-37 protein, expressed by E. coli , with C-His labeled tag. The total length of Animal-Free IL-37 Protein, Human (His) is 166 a.a., with molecular weight of ~19.49 kDa.
The PNPLA2 protein catalyzes the hydrolysis of triglycerides, preferably long-chain fatty acid esters, in lipid droplets. PNPLA2 Protein, Human (His-SUMO) is the recombinant human-derived PNPLA2 protein, expressed by E. coli , with N-SUMO, N-6*His labeled tag. The total length of PNPLA2 Protein, Human (His-SUMO) is 504 a.a., with molecular weight of ~71.3 kDa.
IL-37 Protein, a crucial immune regulatory cytokine, suppresses innate inflammatory and immune responses, mitigating excessive inflammation. It signals intracellularly via nuclear translocation with SMAD3 and extracellularly by binding to its receptor, composed of IL18R1 and IL18RAP. IL-37 inhibits pro-inflammatory cytokines, sparing anti-inflammatory ones, and hinders dendritic cell activation. It interacts with SMAD3, binds IL18R1 (with lower affinity than IL18), and forms a complex with TMED10 for secretion. IL-37 Protein, Human (166a.a) is the recombinant human-derived IL-37 protein, expressed by E. coli , with tag free. The total length of IL-37 Protein, Human (166a.a) is 166 a.a., with molecular weight of ~18.7 kDa.
The GRIN1 protein is a component of the NMDA receptor complex that forms heterotetrameric ligand-gated ion channels with high calcium permeability. GRIN1 Protein, Human (His) is the recombinant human-derived GRIN1 protein, expressed by E. coli , with N-6*His labeled tag. The total length of GRIN1 Protein, Human (His) is 541 a.a., with molecular weight of ~64.6 kDa.
Phospho-PKC zeta (T560) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 68 kDa, targeting to Phospho-PKC zeta(T560). It can be used for WB,IHC-P assays with tag free, in the background of Human, Mouse.
Adipose Triglyceride Lipase Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 55 kDa, targeting to Adipose Triglyceride Lipase. It can be used for WB assays with tag free, in the background of Human, Mouse, Rat.
ZAP70 Antibody (YA651) is a non-conjugated and Mouse origined monoclonal antibody about 70 kDa, targeting to ZAP70 (4B2). It can be used for WB,IP assays with tag free, in the background of Human.
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