p62 Activator

Clemastine (HS-592; Meclastine) fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .

EAD1 trihydrochloride is a Chloroquine (HY-17589A) analog with anticancer activity. EAD1 trihydrochloride blocks autophagy, leading to the intracellular accumulation of autophagosome-related proteins LC3-II and p62. EAD1 trihydrochloride induces cancer cell apoptosis and inhibits cancer cell proliferation. EAD1 trihydrochloride can be used in the research of lung cancer and pancreatic cancer.

Bifendate (DDB), extracted from Schisandrae chinensis, is an orally active anti-HBV agent against chronic hepatitis B. Bifendate inhibits ATG5-dependent autophagy and attenuates oleic acid-induced lipid accumulation with anti-oxidant properties in vitro. Bifendate can decrease alanine transaminase (ALT) level in mice. Bifendate attenuates hepatic steatosis in cholesterol/bile salt- and high-fat diet-induced hypercholesterolemia in mice. Bifendate potently increases the activity of cytochrome proteins (CYPs) and reverse P-gp-mediated multi-drug resistance (MDR).

Clemastine (HS-592; Meclastine) is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation.

Perfluoroundecanoic acid is a perfluoroalkyl substance (PFAS). Perfluoroundecanoic acid is an orally active oxidative stress inducer. Perfluoroundecanoic acid promotes macrophage M2 polarization, activates Wnt/β-catenin signaling and enhances β-catenin nuclear accumulation. Perfluoroundecanoic acid -induced M2 phenotype macrophage accelerates tumor progression in vitro and in vivo. Perfluoroundecanoic acid induces DNA damage, reproductive and pathophysiological dysfunctions via oxidative stress in male Swiss mice. Perfluoroundecanoic acid inhibits Leydig cell development in pubertal male rats via inducing oxidative stress and autophagy. Perfluoroundecanoic acid accelerates insulitis development in a mouse model of type 1 diabetes. Perfluoroundecanoic acid can be used for the study of ovarian cancer, type 1 diabetes and inflammation.

SW083688 is a selective TAOK2 inhibitor with an IC₅₀ of 1.3 μM. SW083688 increases the abundance of p62 protein, inhibits autophagosome maturation, and blocks Autophagic flux. SW083688 is applicable for the research of non-small cell lung cancer and pancreatic cancer.

Clemastine (HS-592; Meclastine)-d₅ fumarate is the deuterium labeled Clemastine fumarate. Clemastine fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .

Clemastine (HS-592; Meclastine) fumarate (Standard) is the analytical standard of Clemastine fumarate. This product is intended for research and analytical applications. Clemastine fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .

EAD1 is a Chloroquine (HY-17589A) analog with anticancer activity. EAD1 blocks autophagy, leading to the intracellular accumulation of autophagosome-related proteins LC3-II and p62. EAD1 induces cancer cell apoptosis and inhibits cancer cell proliferation. EAD1 can be used in the research of lung cancer and pancreatic cancer.

Ginnalin A (Acertannin) is a Nrf2 activator. Ginnalin A shows antiproliferative activity against HCT116, SW480 and SW620 cells with IC₅₀ values of 24.8, 22.0, and 39.7 μM, respectively. Ginnalin A can induce cancer cells S phase arrest. Ginnalin A can activate the p62-Keap1-Nrf2 signaling pathway, significantly upregulate the mRNA and protein expression of Nrf2, HO-1, and NQO1, and promote the transport of Nrf2 from the cytoplasm to the nucleus. Ginnalin A can be used for the research of colon cancer.

ATB1071 is a brain-penetrant and orally active p62/SQSTM1 activator. ATB1071 binds to the p62-ZZ domain, promotes PB1-dependent p62 self-polymerization, and activates p62-mediated mitophagy. ATB1071 can be used for the research of Leigh syndrome, cerebral ischemia-reperfusion injury^[1].

EAD1 TFA is a Chloroquine (HY-17589A) analog with anticancer activity. EAD1 TFA blocks autophagy, leading to the intracellular accumulation of autophagosome-related proteins LC3-II and p62. EAD1 TFA induces cancer cell apoptosis and inhibits cancer cell proliferation. EAD1 TFA can be used in the research of lung cancer and pancreatic cancer.

Bifendate (DDB), extracted from Schisandrae chinensis, is an orally active anti-HBV agent against chronic hepatitis B. Bifendate inhibits ATG5-dependent autophagy and attenuates oleic acid-induced lipid accumulation with anti-oxidant properties in vitro. Bifendate can decrease alanine transaminase (ALT) level in mice. Bifendate attenuates hepatic steatosis in cholesterol/bile salt- and high-fat diet-induced hypercholesterolemia in mice. Bifendate potently increases the activity of cytochrome proteins (CYPs) and reverse P-gp-mediated multi-drug resistance (MDR).