pki

PKI-166 is an oral inhibitor of EGF-R tyrosine kinase (IC50:0.7 nM) that is both effective and selective. PKI-166 can effectively inhibit the growth and metastasis of various human cancer cells including pancreatic cancer.

PKI-402 is a potent PI3K and mTOR inhibitor. PKI-402 inhibits PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ with IC50s of 2, 3, 7, 14 and 16 nM, respectively.

PKI (5-24) Acetate is a high affinity PKA inhibitor (Ki = 2.3 nM).

PKI 14-22 amide, myristoylated Acetate inhibit cAMP-dependent protein kinase (PKA) and blocks hyperalgesia produced by spinal administration of 8-bromo-cAMP.

PKI-179 is a potent, orally active compound that functions as a dual PI3K mTOR inhibitor. It demonstrates IC50 values of 8 nM for PI3K-α, 24 nM for PI3K-β, 74 nM for PI3K-γ, 77 nM for PI3K-δ, and 0.42 nM for mTOR. Additionally, it is effective against E545K and H1047R mutations, with IC50s of 14 nM and 11 nM, respectively. In vivo studies have shown that PKI-179 possesses anti-tumor capabilities[1][2].

PKI-179 is an orally bioavailable dual inhibitor of PI3K and mammalian target of rapamycin (mTOR). In an in vitro enzymatic assay, it potently inhibits PI3K (IC50s = 8, 24, 17, and 74 nM for isoforms α, β, δ, and γ, respectively), two common PI3Kα mutants, E545K and H1047R (IC50s = 14 and 11 nM, respectively), and mTOR (IC50 = 0.42 nM). PKI-179 is selective for PI3K and mTOR over a panel of 361 other kinases at IC50 values up to 50 μM, hERG (IC50 > 30 μM), and cytochrome P450 (CYP) isoforms (IC50s > 30 μM), but does have activity for CYP2C8 (IC50 = 3 μM). It inhibits proliferation through the Akt/mTOR signaling pathway in MDA-361 breast and PC3MM2 prostate cancer cell lines in vitro (IC50s = 22 and 29 nM, respectively) and inhibits tumor growth in an MDA-361 mouse xenograft model when used at a dose of 50 mg/kg.

Potent EGFR-kinase inhibitor (IC50 = 0.7 nM). Displays >3000-fold selectivity against a panel of serine/threonine kinases. Reduces metastasis and angiogenesis in a mouse model of pancreatic cancer. Antihypertensive and orally bioavailable. Bruns et al (2000) Blockade of the epidermal growth factor receptor signaling by a novel tyrosine kinase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma. Cancer Res. 60 2926 PMID:10850439 |Ulu et al (2013) Epidermal growth factor receptor inhibitor PKI-166 governs cardiovascular protection without beneficial effects on the kidney in hypertensive 5/6 nephrectomized rats. J.Pharmacol.Exp.Ther. 345 393 PMID:23528611 |Kaspersen et al (2012) Activity of 6-aryl-pyrrolo[2,3-d]pyrimidine-4-amines to Tetrahymena. Bioorg.Chem. 44 35 PMID:22832269

PKI(5-24) TFA is a synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase) with potent and competitive inhibition properties, exhibiting a K i of 2.3 nM. It corresponds to residues 5-24 of the natural heat-stable protein kinase inhibitor [1][2].

PKI 14-22 amide, myristoylated TFA is a potent inhibitor of cAMP-dependent protein kinase A (PKA) that diminishes IgG-mediated phagocytic response and inhibits neutrophil adhesion [1].

PKI(5-22)amide, an active inhibitory fragment of the cyclic AMP-dependent protein kinase (PKA) inhibitor, effectively prevents PKA activation. However, it does not reduce the homologous desensitization of CRF1 receptors [1] [2].

PKI (14-24)amide is a potent inhibitor of Protein Kinase A (PKA), effectively inhibiting cyclic AMP-dependent protein kinase activity in cell homogenates [1] [2].

PKI (14-24)amide TFA, a potent inhibitor of Protein Kinase A (PKA), significantly reduces cyclic AMP-dependent protein kinase activity within cellular homogenates, as evidenced by research findings [1] [2].

PKI (5-24), amide (IP20-amide) is a potent inhibitor of cAMP-dependent protein kinase (PKA) with an inhibition constant (K i) of 2.3 nM [1]. This 20-residue peptide mirrors the active segment of the heat-stable inhibitor protein specific to PKA, showcasing significant inhibitory efficacy.

High affinity PKA inhibitor (Ki = 2.3 nM).

Ampkinone is an indirect AMPK activator.

SRPKIN-1 is a covalent and irreversible inhibitor of SRPK1 2 (IC50s: 35.6 and 98 nM, respectively).

PKItide demonstrates an inhibitory concentration 50 (IC50) of 0.2 μM against cAMP-dependent protein kinase (cAMP-PK) [1].

CMF019 is a potent agonist of the Apelin receptor (APJ) with G protein bias. CMF019 binds to APJ (pKis: 8.58, 8.49, and 8.71 for the human, rat, and mouse).

EP1-antagonist-1 (EP1 antagonist 1) is an EP1 antagonist (pKi: 7.54; pIC50: 8.5).

5-HT4 antagonist 1 is an antagonist of 5-HT4 (pKi = 9.6).

Adoprazine (SLV313) is a potential atypical antipsychotic bearing potent D2 receptor antagonist and 5-HT1A receptor agonist properties.

Midaglizole hydrochloride ((±)-DG5128) (DG5128) is a preferred α2-adrenoceptor antagonist. Midazolazole hydrochloride (DG5128) has an affinity for α2-adrenoceptor (pKi = 6.28) 7.4 times higher than that of α1-adrenoceptor.

Donitriptan is a 5-HT receptor agonist with pKis of 9.4 and 9.3 for 5-HT1B and 5-HT1D, respectively.

Pradigastat (LCQ-908) is an orally active, potent and selective diacylglycerol acyltransferase 1 (DGAT1) inhibitor for the treatment of constipation, which may be used in the study of obesity and diabetes.