PI3K Modulator

Sincalide (Cholecystokinin octapeptide, CCK-8) is a rapid-acting amino acid polypeptide hormone analogue of cholecystokinin (CCK) for intravenous use in postevacuation cholecystography. Sincalide is a major bioactive segment of CCK that retains most of the biological activities of CCK. Sincalide can promote gallbladder contraction by injection and helps diagnose gallbladder and pancreas disorders. Sincalide can increase bile secretion, cause the gallbladder to contract and relax the sphincter of Oddi, resulting in bile drainage into the duodenum. Sincalide is a major bioactive segment of CCK that retains most of the biological activities of CCK.

Dihydrocapsaicin, a capsaicin, is a potent and selective TRPV1 (transient receptor potential vanilloid channel 1) agonist. Dihydrocapsaicin reduces AIF, Bax, and Caspase-3 expressions, and increased Bcl-2, Bcl-xL and p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection following ischemic stroke via PI3K/Akt regulation in rat.

Momordin Ic is an orally active triterpenoid saponin that can be isolated from Kochia scoparia. It is also a SUMO specific protease 1 (SENP1) inhibitor, SENP1/c-MYC signaling pathway inhibitor, and apoptosis inducer. Momordin Ic induces autophagy and apoptosis in liver cancer cells through the PI3K/Akt and MAPK signaling pathways mediated by reactive oxygen species. Momordin Ic has the ability to control glucose induced blood glucose elevation, inhibit gastric emptying, resist rheumatoid arthritis, reduce CCl₄ (HY-Y0298) induced hepatotoxicity and anti-tumor activity.

Citronellol ((±)-Citronellol) is an orally active inducer of apoptosis. Citronellol can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis.

Heterophyllin B is an active cyclic peptide isolated from Pseudostellaria heterophylla. Heterophyllin B provides a novel strategy for the treatment of esophageal cancer.

Hederacolchiside A1, isolated from Pulsatilla chinensis, suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K/Akt/mTOR signaling pathway. Hederacolchiside A1 has antischistosomal activity, affecting parasite viability both in vivo and in vitro.

Sincalide ammonium (Cholecystokinin octapeptide ammonium, CCK-8 ammonium) is a rapid-acting amino acid polypeptide hormone analogue of cholecystokinin (CCK) for intravenous use in postevacuation cholecystography. Sincalide ammonium is a major bioactive segment of CCK that retains most of the biological activities of CCK. CCK‐8 can promote gallbladder contraction by injection and helps diagnose gallbladder and pancreas disorders. Sincalide ammonium can increase bile secretion, cause the gallbladder to contract and relax the sphincter of Oddi, resulting in bile drainage into the duodenum. Sincalide ammonium is a major bioactive segment of CCK that retains most of the biological activities of CCK.

Kaempferol 3-neohesperidoside (Kaempferol 3-O-neohesperidoside) is a flavonoid. Kaempferol 3-neohesperidoside mimics insulin action via the PI3K/PKC pathway, significantly promoting glucose uptake and increasing muscle glycogen content in rat soleus muscles. Kaempferol 3-neohesperidoside also exhibits anti-glycation activity. Kaempferol 3-neohesperidoside binds to albumin through hydrogen bonding and hydrophobic interactions, and inhibits the formation of advanced glycation end products. Kaempferol 3-neohesperidoside can be used in studies of diabetes and its related complications.

Citronellol (Standard) is the analytical standard of Citronellol. Citronellol (Standard) is an orally active inducer of apoptosis. Citronellol (Standard) can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol (Standard) can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol (Standard) can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol (Standard) exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis.

6-O-Caffeoylarbutin (Robustaside B) possesses antioxidant activity. 6-O-Caffeoylarbutin ameliorates neurological functions and deficits in ischemic mice.

Anticancer agent 273 (Compound 9q) is a potent anticancer agent found in matrine. Anticancer agent 273 inhibits the proliferation of cancer cells (e.g., HeLa cells with an IC₅₀ value of 4.48 μM). Anticancer agent 273 exerts anticancer effects by modulating the expression of PI3K/AKT and activating transcription factor 4 (ATF4), which promotes endoplasmic reticulum stress and induces apoptosis. Anticancer agent 273 is promising for research of cancers, such as cervical cancer.

TS-IN-5 (Compound 15) is a thymidylate synthase (TS) inhibitor. TS-IN-5 induces Apoptosis by modulating Bax, BCL-2, PI3K, and STAT1 proteins. TS-IN-5 shows antitumor effects against liver, breast and colon cancers.

Momordin Ic (Standard) is the analytical standard of Momordin Ic. This product is intended for research and analytical applications. Momordin Ic is an orally active triterpenoid saponin that can be isolated from Kochia scoparia. It is also a SUMO specific protease 1 (SENP1) inhibitor, SENP1/c-MYC signaling pathway inhibitor, and apoptosis inducer. Momordin Ic induces autophagy and apoptosis in liver cancer cells through the PI3K/Akt and MAPK signaling pathways mediated by reactive oxygen species. Momordin Ic has the ability to control glucose induced blood glucose elevation, inhibit gastric emptying, resist rheumatoid arthritis, reduce CCl4 (HY-Y0298) induced hepatotoxicity and anti-tumor activity.

Dihydrocapsaicin (Standard) is the analytical standard of Dihydrocapsaicin. This product is intended for research and analytical applications. Dihydrocapsaicin, a capsaicin, is a potent and selective TRPV1 (transient receptor potential vanilloid channel 1) agonist. Dihydrocapsaicin reduces AIF, Bax, and Caspase-3 expressions, and increased Bcl-2, Bcl-xL and p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection following ischemic stroke via PI3K/Akt regulation in rat.

Nic-15 (compound 4n) is an anti-constrictive agent used to antagonize the hypovascularity of pancreatic tumors. The hypovascularity allows cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop drug resistance. Nic-15 can regulate the PI3K/Akt/mTOR pathway and alleviate ER stress induced by Gemcitabine (HY-17026). Nic-15 can significantly inhibit the migration and colony formation of MIA PaCa-2 and PANC-1 pancreatic cancer cells. The combination of Nic-15 and Gemcitabine can effectively solve the problem of pancreatic tumor resistance. In an in vivo xenograft model, Nic-15 can significantly enhance the efficacy of Gemcitabine.

Asperosaponin V is an indirect modulator of bone metabolism-related targets (e.g., PI3K/AKT, BMP-2/p38, and ERK 1/2 pathways). Asperosaponin V promotes marrow stromal cell proliferation and induces osteoblast differentiation. Asperosaponin V is promising for research of osteoporosis and fracture healing.

Anticancer agent 235 (Compound 49) is a modulator for PI3K/AKT/mTOR pathway, that promotes the generation of ROS, reduces the mitochondrial membrane potential, and thereby inhibits the proliferation of cancer cells HCT116, Caco-2, AGS and SMMC-772 with IC₅₀ of 0.35-26.9 μM. Anticancer agent 235 arrests the cell cycle at G2/M phase, and induces apoptosis in HCT116.

Dihydrocapsaicin-d₃ is the deuterium labeled Dihydrocapsaicin (HY-N0361). Dihydrocapsaicin, a capsaicin, is a potent and selective TRPV1 (transient receptor potential vanilloid channel 1) agonist. Dihydrocapsaicin reduces AIF, Bax, and Caspase-3 expressions, and increased Bcl-2, Bcl-xL and p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection following ischemic stroke via PI3K/Akt regulation in rat.

Hederacolchiside A1 (Standard) is the analytical standard of Hederacolchiside A1. This product is intended for research and analytical applications. Hederacolchiside A1, isolated from Pulsatilla chinensis, suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K/Akt/mTOR signaling pathway. Hederacolchiside A1 has antischistosomal activity, affecting parasite viability both in vivo and in vitro.