pki

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

Pipamperone (McN-JR 3345) binds 5-HT2A closely as receptor.

Seltorexant hydrochloride is a selective, orally active and high-affinity antagonist of OX2R with pKi values of 8.0 and 8.1 for human and rat OX2R.

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 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).

PKI (5-24) Acetate is a 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].

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.

Agomelatine (L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors (Kis: 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2), and Agomelatine (S-20098). L(+)-Tartaric acid also functions as a selective 5-HT2C receptor antagonist (pKis: 6.4 and 6.2 at native porcine and cloned human 5-HT2C receptors), actively supporting research into melatonergic signaling pathways, receptor-mediated regulation, and novel psychiatric therapeutics by enabling precise modulation of circadian and serotonergic systems in cellular models to improve neuropharmacological understanding and experimental reproducibility across neuroscientific and clinical translational studies.