PKC Inhibitor

SAMβA is conjugated to the cell permeable peptide TAT47-57. SAMβA, a rationally designed selective antagonist of Mfn1-βIIPKC association. SAMβA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats.

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.

NPC-15437 dihydrochloride is a selective, penetrable and reversible protein kinase C (PKC) inhibitor, with an IC₅₀ of 19 μM. NPC-15437 dihydrochloride interferes with mechanisms underlying memory consolidation.

Isojacareubin can be isolated from Hypericum japonicum. Isojacareubin covalently inhibits SARS-CoV-2 3CLpro. Isojacareubin also has anti-helicobacter activity. Isojacareubin inhibits PKC, and suppresses hepatocellular carcinoma metastasis and induces apoptosis.

Prkch Mouse Pre-designed siRNA Set A contains three designed siRNAs for Prkch gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Flosequinan is a balanced vasodilator. Flosequinan not only significantly reduces systemic vascular resistance, but also significantly reduces the beating component of left ventricular afterload, characteristic impedance and arterial wave reflection, which can be used in the research of acute heart failure.

K-252c, a staurosporine analog isolated from Nocardiopsis sp., is a cell-permeable PKC inhibitor, with an IC₅₀ of 2.45 µM. K-252c induces apoptosis in human chronic myelogenous leukemia cancer cells. K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase.

PRKCH Human Pre-designed siRNA Set A contains three designed siRNAs for PRKCH gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

N-myristoyl-RKRTLRRL inhibits binding of PKC substrates. N-myristoyl-RKRTLRRL inhibits Ca²⁺- and phosphatidylserine (PS)-dependent histone phosphorylation with IC₅₀ of 5 μM. histone phosphorylation with IC₅₀ of 80 μM.

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. Ro 31-8220 can also inhibit the expression of MKP-1, induce the expression of c-Jun, and activate JNK, and these effects possess pharmacological properties independent of PKC.

Fasudil (Hydrochloride) (Standard) is the analytical standard of Fasudil (Hydrochloride). This product is intended for research and analytical applications. Fasudil (HA-1077; AT877) Hydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an K_i of 0.33 μM for ROCK1, IC₅₀s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil Hydrochloride is also a potent Ca²⁺ channel antagonist and vasodilator.

Bisindolylmaleimide I (Standard) is the analytical standard of Bisindolylmaleimide I. This product is intended for research and analytical applications. 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.

Midostaurin (Standard) is the analytical standard of Midostaurin. This product is intended for research and analytical applications. 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.

Fasudil (HA-1077; AT877) mesylate is a nonspecific and orally active RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an K_i of 0.33 μM for ROCK1, IC₅₀s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil mesylate is also a potent Ca²⁺ channel antagonist and vasodilator.

Mitoxantrone hydrochloride liposome is a liposome-encapsulated Mitoxantrone hydrochloride (HY-13502A) (a topoisomerase II inhibitor). Compared to regular Mitoxantrone hydrochloride, Mitoxantrone hydrochloride liposome enhances antitumor activity and prolongs drug circulation time in the body.

Forskolin (Coleonol) (GMP) is a potent adenylate cyclase activator with an IC₅₀ of 41 nM and an EC₅₀ of 0.5 μM for type I adenylyl cyclase. Forskolin (GMP) is also an inducer of intracellular cAMP formation. Forskolin (GMP) induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR. Forskolin (GMP) exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin (GMP) also induces autophagy.

Ruboxistaurin-d₆ (hydrochloride) is the deuterium labeled Ruboxistaurin hydrochloride. Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin hydrochloride exhibits ATP dependent competitive inhibition of PKC beta I with an IC₅₀ of 4.7 nM. Ruboxistaurin hydrochloride inhibits PKC beta II with an IC₅₀ of 5.9 nM.

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.

Fasudil (HA-1077; AT877) hydrochloride semihydrate is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an K_i of 0.33 μM for ROCK1, IC₅₀s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil hydrochloride semihydrate is also a potent Ca²⁺ channel antagonist and vasodilator.

Clenbuterol (Standard) is the analytical standard of Clenbuterol. This product is intended for research and analytical applications. Clenbuterol (NAB-365) is a β2-adrenergic receptor agonist with an EC50 of 31.9 nM. Clenbuterol is a very potent inhibitor of the lipopolysaccharide (LPS)-induced release of TNF-α and IL-1β. Clenbuterol can inhibit the inflammatory process. Clenbuterol is a bronchodilator.