pkr

PKR-IN-C16 is a specific protein kinase (PKR) inhibitor. PKR-IN-C16 is able to inhibit the autophosphorylation of PKR and unlock the translation blockade induced by PKR in primary neuronal cultures.PKR-IN-C16 binds the ATP-binding site of PKR and blocks autophosphorylation with an IC50 value of 186-210 nM. PKR-IN-C16 protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress.

PKR activator 1 is a potent activator of pyruvate kinase-R (PKR).

PKR activator 2 is a potent activator of pyruvate kinase-R (PKR).

PKR-IN-2 is a activator of pyruvate kinase (PKR).

PKR-IN-1 (Compound 5s) is a pyruvate kinase (PK) inhibitor with antifungal properties, exhibiting an EC50 of 0.21 μg/mL against Rhizoctonia solani (R. solani).

PKR-IN-C51 is a dose-dependent and ATP-competitive protein kinase R (PKR) inhibitor that inhibits intracellular PKR activation and autophosphorylation in mouse macrophages with an IC50=9 μM and Ki=3.4 μM.Interferon-induced double-stranded RNA-activated protein kinase (PKR) is a widely expressed Ser/Thr kinase.

PKR activator 4 (example 7A), a potent activator of pyruvate kinase R (PKR), holds promise for blood disorder research [1].

PKR Activator 5 (Compound 18) serves as an activator for pyruvate kinase R (PKR), displaying an AC50 value of 28 nM.

PKR1 antagonist 1 (PC1) is an effective antagonist of PKR1. It alleviates both hyperalgesia and allodynia in SNI mice.

PKRA83 is a potent prokineticin (PK2) antagonist that crosses the blood-brain barrier and competes for PK2 binding to its receptors PKR1 and PKR2. PKRA83 effectively inhibits PK2 receptors and acts on PKR1 (IC50: 5.0 nM) and PKR2 (IC50: 8.2 nM). PKRA83 exhibits anti-cancer and anti-angiogenic effects.

PKRA83 hydrochloride hydrate, also known as PKRA7, is a potent prokineticin (PK2) antagonist that competes with PK2 for binding to its receptors, PKR1 and PKR2. It exhibits high inhibitory affinity with IC50 values of 5.0 nM for PKR1 and 8.2 nM for PKR2, displaying anticancer, anti-arthritis, and anti-angiogenic properties. Additionally, this compound is capable of crossing the blood-brain barrier [1] [2] [3].

(Rac)-Etavopivat ((Rac)-FT-4202), an isomer of Etavopivat, is an orally active erythrocyte pyruvate kinase-R (PKR) activator used in sickle cell disease and haemoglobinopathy research [1].

Mitapivat (PKR-IN-1), also known as PKM2 activator 1020 is a PKM2 activator (pyruvate kinase activator) for the treatment of pyruvate kinase deficiency.

GSK2656157 is a highly specific and ATP-competitive PERK inhibitor (IC50: 0.9 nM) in a cell-free assay. The selectivty is 500-fold higher against a panel of 300 kinases.

WAY-354896 is a dual activator that simultaneously stimulates protein kinase R (PKR) and protein kinase R-like endoplasmic reticulum kinase (PERK).

ONO-8130 is an orally available antagonist of EP1 receptor.

Takeda-6d, a novel, potent DFG-out RAF/vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor, inhibits B-RAF and VEGFR2 with IC50 of 7.0nM and 2.2nM.

Bozepinib is an antitumor compound that acts by inducing PKR-mediated apoptosis and synergizing with IFN.

GSK2606414 is a cell-permeable and orally active protein kinase R-like endoplasmic reticulum kinase(PERK)inhibitor with IC50 of 0.4 nM. GSK2606414 inhibits PERK activation in cells and suppresses the growth of human tumor xenografts in mice.

7DG is a selective inhibitor of protein kinase R (PKR).

Etavopivat is a powerful, specific, orally bioavailable activator of pyruvate kinase (PKR) in red blood cells (RBCs). It exhibits potent properties against sickling.

ISRIB (trans-isomer) is a potent inhibitor of PERK (IC50=5 nM) that restores protein translation and prevents SG formation in the presence of P-eIF2α.

BEPP monohydrochloride is a double-strand RNA-dependent protein kinase (PKR) activator.

TEPP-46 (ML265) is an activator of pyruvate kinase M2 (PKM2) (AC50=92 nM), selective for PKM1, PKL and PKR. TEPP-46 has antitumor activity.