2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. PERK
  5. PERK Inhibitor

PERK Inhibitor

PERK Inhibitors (22):

Cat. No. Product Name Effect Purity
  • HY-18072
    GSK2606414
    		Inhibitor 99.91%
    GSK2606414 is a cell-permeable and orally available protein kinase R-like endoplasmic reticulum (ER) kinase (PERK) inhibitor with an IC50 of 0.4 nM.
  • HY-12495
    ISRIB (trans-isomer)
    		Inhibitor 99.08%
    ISRIB (trans-isomer) is a potent inhibitor of PERK with an IC50 of 5 nM. ISRIB potently reverses the effects of eIF2α phosphorylation (IC50=5 nM).
  • HY-13820
    GSK2656157
    		Inhibitor 99.66%
    GSK2656157 is a selective and ATP-competitive inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) with an IC50 of 0.9 nM.
  • HY-12661A
    AMG PERK 44
    		Inhibitor 99.81%
    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.
  • HY-157231
    HC-5404
    		Inhibitor
    HC-5404 is a potent and selective PERK inhibitor. HC-5404 has orally activity. HC-5404 significantly blocks metastasis via killing quiescent/slow-cycling ISRhigh.
  • HY-139612
    Opnurasib
    		Inhibitor 98.94%
    Opnurasib (JDQ-443) (NVP-JDQ443) is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). Opnurasib shows antitumor activity.
  • HY-145835
    PERK-IN-5
    		Inhibitor 99.40%
    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.
  • HY-137813
    PERK-IN-4
    		Inhibitor 98.30%
    PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC 50 of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states.
  • HY-135220
    PERK-IN-2
    		Inhibitor 99.00%
    PERK-IN-2 is a potent PERK inhibitor with an IC50 of 0.2 nM.
  • HY-12736A
    GSK143 dihydrochloride
    		Inhibitor 99.73%
    GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC50=7.1). GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.
  • HY-13699
    NBI-42902
    		Inhibitor 98.65%
    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. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases.
  • HY-137813S
    PERK-IN-4-d3
    		Inhibitor
    PERK-IN-4-d3 is the deuterium labeled PERK-IN-4. PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC 50 of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states[1].
  • HY-145835A
    (S)-PERK-IN-5
    		Inhibitor
    (S)-PERK-IN-5 is the S-enantiomer of PERK-IN-5. (S)-PERK-IN-5 (example 39) is a PERK inhibitor, with an IC50 of 0.101-0.250 μM.
  • HY-144323
    YF135
    		Inhibitor
    YF135 is an efficient and reversible-covalent KRASG12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRASG12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway.
  • HY-12736
    GSK143
    		Inhibitor
    GSK143 is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 inhibits phosphorylated Erk (pErk: pIC50=7.1). GSK143 reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.
  • HY-144693
    MEK/PI3K-IN-2
    		Inhibitor
    MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines.
  • HY-18318
    Takeda-6D
    		Inhibitor
    Takeda-6D (compound 6d) is an orally active and potent BRAF/VEGFR2/KDR/Flk-1 inhibitor, with IC50 values of 7.0 and 2.2 nM, respectively. Takeda-6D shows antiangiogenesis by suppressing the VEGFR2/KDR/Flk-1 pathway in 293/VEGFR2/KDR/Flk-1 and VEGF-stimulated HUVEC cells.Takeda-6D shows significant suppression of ERK1/2 phosphorylation. Takeda-6D shows antitumor activity.
  • HY-144692
    MEK/PI3K-IN-1
    		Inhibitor
    MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC50 values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines.
  • HY-124857
    7DG
    		Inhibitor
    7DG (7-Desacetoxy-6,7-dehydrogedunin) is a protein kinase R (PKR) inhibitor. 7DG protects macrophages from lethal toxin-induced pyroptosis.
  • HY-130643
    PERK-IN-3
    		Inhibitor
    PERK-IN-3 is a potent PERK inhibitor with an IC50 of 7.4 nM.