PERK Inhibitor

PERK Inhibitors (23):

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	98.58%
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-157231A

HC-5404-Fu	Inhibitor
HC-5404-Fu is a PERK inhibitor with an antitumor activity. HC-5404-Fu inhibits endoplasmic reticulum stress response signalling. HC-5404-Fu sensitizes renal cell carcinoma cells to vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitors (TKIs). HC-5404-Fu is promising for research of renal cell carcinoma, gastric cancer, metastatic breast cancer, small cell lung cancer, and other solid tumors.

HY-N0231R

Bavachalcone (Standard)	Inhibitor
Bavachalcone (Standard) is the analytical standard of Bavachalcone. This product is intended for research and analytical applications. Bavachalcone is a potent inducer of apoptosis. Bavachalcone exerts anticancer activity by promoting autophagy and apoptosis in HepG2 cells. Bavachalcone acts as an anti-neuroinflammatory and antidepressant through the NF-κB pathway. Bavachalcone inhibits osteoclasts by interfering with ERK and Akt signaling pathways and the expression of c-Fos and NFATc1. Bavachalcone exhibits a significant inhibitory effect on baculovirus-expressed BACE-1 in vitro.

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-135220

PERK-IN-2	Inhibitor	99.00%
PERK-IN-2 is a potent PERK inhibitor with an IC₅₀ of 0.2 nM.

HY-N0231

Bavachalcone	Inhibitor	99.95%
Bavachalcone is a potent inducer of apoptosis. Bavachalcone exerts anticancer activity by promoting autophagy and apoptosis in HepG2 cells. Bavachalcone acts as an anti-neuroinflammatory and antidepressant through the NF-κB pathway. Bavachalcone inhibits osteoclasts by interfering with ERK and Akt signaling pathways and the expression of c-Fos and NFATc1. Bavachalcone exhibits a significant inhibitory effect on baculovirus-expressed BACE-1 in vitro.

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-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-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 K_i 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 KRAS^G12C 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 KRAS^G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway.

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.

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