pki

High affinity PKA inhibitor (Ki = 2.3 nM).

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 hydrochloride is a potent and orally available dual PI3K/mTOR inhibitor. Its IC₅₀ values against PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR are 8 nM, 24 nM, 74 nM, 77 nM and 0.42 nM respectively. It also exerts inhibitory activity against E545K and H1047R mutants with IC₅₀ values of 14 nM and 11 nM, and exhibits significant antitumor effects in in vivo models.

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.

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

Gedatolisib (PF-05212384) is a highly effective dual inhibitor targeting the PI3Kα/γ (IC50: 0.4/5.4 nM)and mTOR (IC50: 1.6 nM) in the PI3K/mTOR signaling pathway.

SU11274 (Met Kinase Inhibitor)(IC50=10 nM) is a specific Met inhibitor. It shows no significant effects on PGDFRβ, EGFR or Tie2.

PKA Inhibitor Fragment (6-22) amide TFA (PKA Inhibitor Fragment (6-22) amide TFA) is a highly potent inhibitor of cAMP-dependent protein kinase A (PKA) with a Ki of 2.8 nM and reverses the pain-relieving effects of low levels of morphine in mice.

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].

Necrostatin-1 (Nec-1) is a specific RIP1 inhibitor and necrotic apoptosis inhibitor, which inhibits TNF-α-induced necrotic apoptosis and also inhibits IDO.