Eukaryotic Initiation Factor (eIF) Modulator

NYX-2925 is an orally active, blood-brain barrier-permeable NMDAR modulator, with EC₅₀ values of 55 pM, 28 fM, 11 pM and 55 pM against NR2A, NR2B, NR2C and NR2D, respectively. NYX-2925 enhances synaptic plasticity, long-term potentiation, metaplasticity, structural plasticity, learning ability, memory capacity and circadian rhythm amplitude. NYX-2925 regulates the signaling pathways of Src kinase, EIF2, mTOR, CDK5 and protein kinase A (PKA). NYX-2925 increases the levels of PSD-95, GluA1, activated Src and synaptic GluN2B. NYX-2925 is used in the research of neuropathic pain, fibromyalgia, painful diabetic peripheral neuropathy, post-traumatic stress disorder, cognitive impairment, depression, age-related cognitive decline and NMDAR-mediated central nervous system diseases.

AMC-01 is a potent chemical probe that regulates eIF2-α activity. AMC-01 induces protein kinase RNA activation (PKR) kinase and nuclear factor κb (NF-κB). AMC-01 inhibits apoptosis.

Comtifator (Example 77) is a modulator of the integrated stress response pathway. Comtifator can be studied in research for diseases associated with integrated stress response.

PRXS571 is a potent modulator of the neuronal integrated stress response (ISR) and can be used in neural-related research.

RAPT-37-Me is a GCN2-targeting agent with IC₅₀ values of 0.002μM, ＞ 10 μM,4.40 μM and 1.31 μM for GCN2, PERK, HRl and PKR, respectively.

ISR modulator-1 (Compound 212) is a modulator for integrated stress response pathway (ISR)

ETC-501 is a blood-brain barrier-permeable, orally active, and selective MNK1/MNK2 inhibitor, with an IC₅₀ of 0.033 μM against MNK1 and 0.111 μM against MNK2. ETC-501 inhibits glioblastoma cell proliferation, impairs DNA damage repair function, delays cell cycle progression, and suppresses ribosome biogenesis. ETC-501 enhances Temozolomide (HY-17364)-induced cellular senescence, attenuates the senescence-associated secretory phenotype, and increases cellular sensitivity to Navitoclax (HY-10087). ETC-501 is applicable to research related to glioblastoma.

ISR activator-4 is an eIF2B modulator and integrated stress response (ISR) activator with a human eIF2B EC₅₀ of 2.2 μM. ISR activator-4 stabilises the inactive I-state of eIF2B, favours formation of the inhibitory eIF2B-eIF2(αP) complex, and attenuates eIF2B's guanine nucleotide exchange factor activity. ISR activator-4 can be used for the research of cancer, neurologic and metabolic disorders.

EMD-C02602 is a GCN2-targeting agent with IC₅₀ values of 0.023 μM, 4.52 μM, ＞ 10 μM and 0.048 μM for GCN2, PERK, HRland PKR, respectively.

ISR activator-5 is an eIF2B modulator and integrated stress response (ISR) activator. ISR activator-5 stabilises the inactive I-state of eIF2B, inhibits protein synthesis, and activates canonical ISR pathways without inducing eIF2α phosphorylation. ISR activator-5 can be used for the research of cancer, neurologic and metabolic disorders.

AMG-34 is a GCN2-targeting agent with IC₅₀ values of 0.395 μM, 0.010 μM, 1.07 μM and ＞ 10 μM for GCN2, PERK, HRland PKR, respectively.

MNK/PIM-IN-2 is a Mnk/Pim kinase inhibitor with an IC₅₀ of 32 nM for Mnk1, 3 nM for Mnk2, and 37 nM for Pim1. MNK/PIM-IN-2 reduces the levels of p-eIF4E and p-4EBP1. MNK/PIM-IN-2 induces cell cycle arrest, apoptosis (apoptosis) and exerts antiproliferative effects in leukemia cells. MNK/PIM-IN-2 can be used in studies related to leukemia.