PERK

ISRIB is an inhibitor of the protein kinase R-like endoplasmic reticulum kinase (PERK) signaling pathway. ISRIB effectively reverses the phosphorylation of eukaryotic translation initiation factor 2 alpha (eIF2α), with an IC 50 value of 5nM.

GSK2606414 is an orally active, selective protein kinase R-like endoplasmic reticulum kinase (PERK) inhibitor with an IC 50 value of 0.4 nM.

CCT020312 is a selective protein kinase R-like endoplasmic reticulum kinase (PERK) pathway agonist.

Rehmannioside A is an inhibitor of cytochrome P450 enzymes (CYP3A4, 2C9, and 2D6), with IC 50 values of 10.08, 12.62, and 16.43μM, respectively.

DIM-C-pPhCO2Me is a nuclear receptor 4A1 (NR4A1) antagonist, with a K i value of 0.25μM.

AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC50 of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC50=7300 nM) and B-Raf (IC50 >1000 nM), respectively. AMG PERK 44 induces autophagy.

MK-28 is a potent and selective agonist of pancreatic endoplasmic reticulum kinase (PERK), which functions by modulating the endoplasmic reticulum stress response.

PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model.

PERK-IN-2 is a highly efficient PERK inhibitor with an IC50 value of 0.2 nM.

PERK-IN-6 (Compound 5) is a PERK inhibitor with an IC50 of 2.5 nM.

NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively.

RAS activator compound 1 (Compound 7c) is a RAS activator targeting the guanine nucleotide exchange factor (GEF) son of sevenless homologue 1 ( SOS1 ).

E8431 is a DCSTAMP antagonist with an IC 50 value of 775.8 nM for osteoclastogenesis.

BTX-6654 formate is a SOS1 PROTAC degrader.

CK37 is a competitive choline kinase-α inhibitor.

GSK2656157 is a potent, selective, and cell-permeable ATP-competitive inhibitor of PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) with an IC₅₀ value of 0.9nM.