- Cat. No.
- A14336
Valrubicin
Valrubicin is a semisynthetic derivative of the antineoplastic anthracycline antibiotic doxorubicin.
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Protein kinase C (PKC) inhibitors and activators act on a family of lipid-regulated serine/threonine kinases. Conventional PKC isoforms require calcium and diacylglycerol, novel isoforms need only diacylglycerol, and atypical isoforms respond to neither. Tumor-promoting phorbol esters mimic diacylglycerol and were shown in 1982 to activate PKC directly. 12-O-tetradecanoyl phorbol-13-acetate (TPA) is the standard activator of this kind, and ingenol mebutate also activates several isoforms. Staurosporine was first described as a PKC inhibitor but blocks a wide range of protein kinases. Enzastaurin is selective for PKCβ, while GO6983 and Ro 31-8220 mesylate inhibit multiple conventional and novel isoforms.
Valrubicin is a semisynthetic derivative of the antineoplastic anthracycline antibiotic doxorubicin.
PKC (19-36), pseudosubstrate peptide inhibitor of protein kinase C (IC50 = 0.18 uM).
Protein Kinase C (19-31), this peptide derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, it was used as protein kinase C substrate peptide for testing the protein kinase C activity.
TAS 301 is an inhibitor of smooth muscle cell migration and proliferation.
Synonyms: Dephnoretin; Thymelol
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.
Synonyms: (-)-Ingenol
Ingenol is a potent activator of protein kinase C (PKC), exhibiting a Ki value of 30 μM. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Ingenol can be utilized to explore the role of PKC in various signaling pathways and to investigate its potential therapeutic applications in oncology.
Synonyms: (+)-Decursin
Decursin is an anticancer agent, with potential anti-inflammatory activity.
PKC-IN-1 is a poent PKC beta II inhibitor with Ki of 14.9 nM; compound example H6 from patent WO 2008096260 A1.
NSC305787 is a small molecule inhibitor of PKC, with IC50 of 8.3 uM, 9.4 uM, 55 uM for PKC phosphorylation of recombinant ezrin, of moesin, and of radixin.
Synonyms: LY-333531
LY333531 is a β-specific protein kinase C inhibitor. It competitively and reversibly inhibits PKCβ1 and PKCβ2 with IC50 values of 4.7 and 5.9 nM respectively.
Synonyms: HA100
HA-100 is an isoquinoline compound with an added piperazinylsulfonyl group that acts as an inhibitor of protein kinases (PKs), including PKA, PKC, and PKG (IC50 = 8, 12, and 4 μM, respectively).
Synonyms: B-106
BJE6-106 (B106) is a potent, selective 3rd generation PKCδ inhibitor with an IC50 of 0.05 μM and targets selectivity over classical PKC isozyme PKCα (IC50=50 μM).
PKC-theta inhibitor 1 is the PKCθ inhibitor with an Ki value of 6 nM, inhibits IL-2 production in vivo with an IC50 of 0.19 μM.
Synonyms: 7-epi-Hydroxystaurosporine
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.
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.
Synonyms: LXS 196
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. It can be used for the treatment of uveal melanoma.
PKC-theta inhibitor is a selective PKC-θinhibitor, with an IC50 of 12 nM.
CMPD101, is a novel membrane-permeable, small-molecule inhibitor of both GRK2 and GRK3 with IC50s of 18 nM and 5.4 nM. CMPD101 also inhibits ROCK-2 and PKCα (IC50s=1.4 μM and 8.1 μM, respectively).
Synonyms: FR236924
DCP-LA (FR236924), a linoleic acid derivative, selectively and directly activates PKCε.
Synonyms: Phorbol dibutyrate; PDBu
Phorbol 12,13-dibutyrate (Phorbol dibutyrate) is a PKC activator and a potent skin tumor promoter.
Synonyms: Mallotoxin; NSC 56346; NSC 94525
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.
Synonyms: DCPLA methyl ester
DCPLA-ME, the methyl ester form of DCPLA, is a potent PKCε activator for use in the treatment of neurodegenerative diseases.
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Synonyms: SQ23377
Ionomycin (SQ23377) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus.
Synonyms: Bisindolylmaleimide IX
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.