eIF2 Activator

2BAct is a highly selective, orally active, and CNS-penetrant eIF2B (eukaryotic initiation factor 2B) activator with an EC₅₀ of 33 nM. 2BAct prevents neurological defects caused by a chronic integrated stress response. 2BAct displays improved solubility and pharmacokinetics relative to eIF2B activator ISRIB trans-isomer (HY-12495).

HR-19011 is an eIF2α phosphorylation activator targeting heme-regulated inhibitor HRI (EIF2AK1). HR-19011 exhibits growth inhibitory activity against K562 cells with an IC₅₀ value of 3.91 µM. HR-19011 inhibits the growth of hematologic malignancies by targeting HRI to activate the integrated stress response via the HRI-eIF2α-ATF4 axis. HR-19011 shows good safety in vivo. HR-19011 can be used for research on hematologic malignancies (leukemia).

Plecstatin-1 hydrochloride is a metal complex that drives the aggregation and collapse of the plectin network, and disrupts the cytoskeletal structures of α‑tubulin and F‑actin. Plecstatin-1 hydrochloride triggers oxidative stress, mediates the phosphorylation of eIF2α, and induces molecular features associated with immunogenic cell death, including calreticulin membrane exposure, membrane localization of HSP70/HSP90, ATP secretion, and HMGB‑1 release. Plecstatin-1 hydrochloride induces apoptosis via the intrinsic mitochondrial pathway and exerts anti-invasive activity. Plecstatin-1 hydrochloride inhibits sphere proliferation and reduces clonogenicity in the 3D tumor spheroid model of colon cancer cells. Plecstatin-1 hydrochloride is applicable to relevant research on colorectal cancer.

BQZ-485 is a GDI2 inhibitor and a paraptosis inducer with antitumor activity. BQZ-485 binds to the Rab-binding platform domain of GDI2, disrupts the interaction between GDI2 and Rab1A, and impairs the membrane recycling of Rab1A. BQZ-485 blocks vesicle trafficking from the endoplasmic reticulum to the Golgi apparatus, and induces endoplasmic reticulum expansion, endoplasmic reticulum fusion, endoplasmic reticulum stress, unfolded protein response and cytoplasmic vacuolization. BQZ-485 is applicable to pancreatic cancer-related research.

1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) is an ER stress inducer that targets proteins such as PKR-like ER kinase PERK to induce cytotoxicity. 1,2,4-Trihydroxybenzene selectively activates eIF2α phosphorylation, activates the PERK-eIF2α signaling pathway and induces stress granule formation. 1,2,4-Trihydroxybenzene subsequently exacerbates oxidative stress and causes DNA double-strand breaks, destroying organelles such as mitochondria and ER, and inducing cell death. 1,2,4-Trihydroxybenzene also has the potential to exhibit anti-tumor effect, increase blood pressure, and relieve spasm.

ML291 is a UPR (unfolded protein response)-inducing sulfonamidebenzamide. ML291 overwhelms the adaptive capacity of the UPR and induces apoptosis in a variety of solid cancer models. ML291 can activate the PERK/eIF2a/CHOP (apoptotic) arm of the UPR and reduce leukemic cell burden.

Plecstatin‑1 is a metal complex that drives the aggregation and collapse of the plectin network, and disrupts the cytoskeletal structures of α‑tubulin and F‑actin. Plecstatin-1 triggers oxidative stress, mediates the phosphorylation of eIF2α, and induces molecular features associated with immunogenic cell death, including calreticulin membrane exposure, membrane localization of HSP70/HSP90, ATP secretion, and HMGB‑1 release. Plecstatin-1 induces apoptosis via the intrinsic mitochondrial pathway and exerts anti-invasive activity. Plecstatin‑1 inhibits sphere proliferation and reduces clonogenicity in the 3D tumor spheroid model of colon cancer cells. Plecstatin-1 is applicable to relevant research on colorectal cancer.

PTC-IN-1 is a human ribosomal peptidyl transferase center (PTC) inhibitor. PTC-IN-1 forms stable interactions with 28S rRNA and undergoes steric-hindrance electrostatic interactions with nascent polypeptide chains, thereby inducing context-dependent translation arrest. PTC-IN-1 activates the ribotoxic stress response through phosphorylation of p46 and p54 JNK, triggers ribosome collisions, and activates the integrated stress response via phosphorylation of eIF2α. PTC-IN-1 inhibits the proliferation of cancer cells. PTC-IN-1 can be used in the research of triple-negative breast cancer, prostate cancer, colorectal cancer.

eIF2B activator-1 (Compound 7a) is a eIF2B activator with a pEC₅₀ value of 7.3. eIF2B activator-1 exhibits significant hERG inhibitory activity, with a pIC₅₀ value of 5.7. eIF2B activator-1 can be used in research related to Huntington's disease, Parkinson's disease, and amyotrophic lateral sclerosis (ALS).

CDC25A/NF-κB-IN-1 is an effective dual-target inhibitor of CDC25A and NF-κB, and is a prodrug of Pt(IV). CDC25A/NF-κB-IN-1 has anticancer activity and low cytotoxicity to normal cells. CDC25A/NF-κB-IN-1 can trigger a variety of anticancer mechanisms, including S phase cell cycle arrest, mitochondrial endogenous apoptosis, endoplasmic reticulum stress, autophagy-dependent ferroptosis. CDC25A/NF-κB-IN-1 has good safety and can be used for ovarian cancer research.

Lard oil is an orally active biochemical reagent. Lard oil upregulates PERK, eIF2a, CHOP, OPN, TLR2, TLR4, TNF-α, and downregulates GRP78 and IRE1a. Lard oil induces responses such as body fat accumulation, elevated serum insulin levels, increased HOMA-IR, hepatic ectopic lipid deposition, hepatic endoplasmic reticulum stress, and hepatic inflammation. Lard oil can be used in studies related to diet-induced obesity, insulin resistance, and non-alcoholic fatty liver disease.

1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) (Standard) is the analytical standard of 1,2,4-Trihydroxybenzene (HY-W010451). This product is intended for research and analytical applications. 1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) is an ER stress inducer that targets proteins such as PKR-like ER kinase PERK to induce cytotoxicity. 1,2,4-Trihydroxybenzene selectively activates eIF2α phosphorylation, activates the PERK-eIF2α signaling pathway and induces stress granule formation. 1,2,4-Trihydroxybenzene subsequently exacerbates oxidative stress and causes DNA double-strand breaks, destroying organelles such as mitochondria and ER, and inducing cell death. 1,2,4-Trihydroxybenzene also has the potential to exhibit anti-tumor effect, increase blood pressure, and relieve spasm.