PI3K

Strictinin is an orally active phenolic compound. Strictinin reduces xanthine oxidase activity, uric acid production, and the activation of ERK1/2, JNK, NF-κB, and NLRP3 inflammasome components in hepatocytes treated with Xanthine (HY-W017389). Strictinin decreases elevated serum uric acid levels and enhanced xanthine oxidase activity in mice treated with potassium oxonate. Strictinin acts as a ROR1 inhibitor and exhibits anticancer activity against highly aggressive non-androgen-dependent prostate cancer. Strictinin induces cancer cell apoptosis (apoptosis), arrests cell cycle, and inhibits cancer cell migration, invasion, and epithelial-mesenchymal transition. Strictinin modulates gut microbiota, inhibits bacterial growth and biofilm formation, accelerates small intestinal transit, and blocks viral entry and replication. Strictinin can be used in research related to hyperuricemia, androgen receptor-negative non-androgen-dependent prostate cancer, triple-negative breast cancer, bacterial infections, constipation, coronavirus infections, dental caries, and infections caused by influenza A, influenza B, and human parainfluenza virus type 1.

Quercetin-d₅ is a deuterium labeled Quercetin. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC₅₀ of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.

Pegloxenatide (Polyethylene glycol loxenatide) is a long-acting glucagon-like peptide-1 receptor (GLP-1RA) agonist. Pegloxenatide has various activities such as lowering blood glucose, lowering blood lipids, improving body weight, anti-inflammation, promoting wound healing, protecting the liver, and protecting the heart. Pegloxenatide can be used in the research of type 2 diabetes and its multiple complications.

PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC₅₀ of 1.7 nM.

Phellodendrine is an orally active plant alkaloid. Phellodendrine inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway.

pan-KRAS-IN-5 is a pan-KRAS translation inhibitor by targeting 5′-UTR RNA G-quadruplexes (rG4s). pan-KRAS-IN-5 strongly binds to and stabilizes KRAS rG4s, inhibits KRAS translation, and blocks the MAPK and PI3K-AKT pathways. pan-KRAS-IN-5 induces cell cycle arrest, prompts apoptosis in KRAS-driven cancer cells. pan-KRAS-IN-5 inhibits tumor growth and KRAS expression in KRAS-mutant xenograft. KRAS-IN-5 can be used for KRAS-driven cancer research.

(S)-Zovegalisib ((S)-RLY-2608) is an S-enantiomer of of Zovegalisib (HY-153306). Zovegalisib is an orally active first-in-class allosteric mutant-selective inhibitor of PI3Ka with anti-tumor activity.

Hyaluronic acid, low endotoxin (Hyaluronan, low endotoxin) is a biopolymer composed of repeating disaccharide units containing low levels of endotoxin. Hyaluronic acid is a major component of the extracellular matrix (ECM). It is synthesized on the plasma membrane. Hyaluronic acid exerts its effects by binding to receptors CD44 and RHAMM. Hyaluronic acid activates PI3K-Akt signaling. Hyaluronic acid also enhances cell invasion and angiogenesis by promoting or stimulating the binding of proteolytic MMP-9 to the cell surface. Elevated hyaluronic acid levels are associated with tumor cell growth, adhesion, migration, invasion, and angiogenesis in digestive system cancers. Hyaluronic acid is involved in tissue remodeling and rapid cell proliferation in several physiological processes, including embryonic morphogenesis and wound healing. Hyaluronic acid can be used as a regulator of cancer-associated lymphangiogenesis. Hyaluronic acid can be used as a drug delivery carrier for sodium butyrate, enhancing its anti-proliferative activity against breast cancer cell lines. Hyaluronic acid can lubricate the corneal endothelium. Hyaluronic acid can improve tissue hydration and enhance the resistance of cells to mechanical damage. Hyaluronic acid has been conjugated with antibodies to ensure that the active compound continues to exert its effects at the site of inflammation. Hyaluronic acid can be used in research in the fields of osteoarthritis, ophthalmology, cosmetic dermatology, oncology, and liver diseases.

Erucic acid (Standard) is the analytical standard of Erucic acid. This product is intended for research and analytical applications. Erucic acid, a monounsaturated fatty acid (MUFA), is isolated from the seed of Raphanus sativus L. Erucic acid can readily cross the blood-brain barrier (BBB), it has been reported to normalize the accumulation of very long-chain fatty acids in the brain. Erucic acid can improve cognitive impairment and be effective against dementia.

KS-133 is a bicyclic peptide with VIPR2 antagonistic activity that can cross the blood-brain barrier. KS-133 selectively blocks VIPR2-mediated Gq/Ca, Gs/cAMP, cAMP/PKA/ERK and PI3K/AKT/GSK3β signaling pathways. KS-133 inhibits VIPR2 agonist-induced CREB phosphorylation in the prefrontal cortex of mice. KS-133 shifts the polarization direction of macrophages toward M1. KS-133 attenuates cancer cell proliferation and reduces the cell cycle distribution level at the S-M phase. KS-133 exerts antitumor effects in a mouse model of colorectal cancer. KS-133 reverses cognitive decline in mouse models of psychiatric disorders. KS-133 can be used for research related to schizophrenia, colorectal cancer and breast cancer.

PI3K/mTOR Inhibitor-13 sodium is an orally active dual inhibitor of phosphoinositol 3-kinase (PI3K) and mTOR kinase. PI3K/mTOR Inhibitor-13 sodium has potential applications in sexual diseases, solid tumor and idiopathic pulmonary fibrosis (IPF).

PI3K-IN-36 (compound A68) is a potent PI3K inhibitor. PI3K-IN-36 can be used in research of follicular lymphoma (FL).

4′-Hydroxywogonin (8-Methoxyapigenin), a flavonoid, could be isolated from a variety of plants including Scutellaria barbata and Verbena littoralis. 4′-Hydroxywogonin has anti-inflammatory activity via TAK1/IKK/NF-κB, MAPKs and PI3/AKT signaling pathways. 4′-Hydroxywogonin inhibits angiogenesis by disrupting PI3K/AKT signaling. 4′-Hydroxywogonin inhibits cell proliferation and induces apoptosis.

RMC-4998 formic is an orally active inhibitor targeting the active or GTP-bound state of the KRAS^G12C mutant. RMC-4998 formic can form a ternary complex with intracellular CYPA and the activated KRAS^G12C mutant, with an IC₅₀ value of 28 nM. RMC-4998 formic can inhibit ERK signaling in KRAS^G12C mutant cancer cells and induce apoptosis. RMC-4998 formic can be used for non-small cell lung cancer (NSCLC) research.

Pichromene (S14161) is an anticancer agent and weak PI3K inhibitor. Pichromene can effectively inhibit tumor growth in leukemia mouse models and can be used in cancer research.

Gedatolisib-d₈ (PKI-587-d₈) is the deuterium labeled Gedatolisib (HY-10681). Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC₅₀s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2.

Hirsutenone is an active botanical diarylheptanoid present in Alnus species and exhibits many biological activities, including anti-inflammatory, anti-tumor promoting and anti-atopic dermatitis effects. Hirsutenone attenuates adipogenesis by binding directly to PI3K and ERK1 in a non-ATP competitive manner. Hirsutenone can be used for the study of obesity.

Esculetin (Standard) is the analytical standard of Esculetin. This product is intended for research and analytical applications. Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities.

Anti-CD3 Antibody (UCHT-1) is an antibody targeting CD3. Anti-CD3 Antibody (UCHT-1) activates the phospholipase C and phosphatidylinositol 3-kinase (PI3K) signaling pathways, elevates intracellular calcium levels, regulates the T3 epitope, and triggers T lymphocyte proliferation. Anti-CD3 Antibody (UCHT-1) also inhibits lymphocyte proliferation, abolishes IL-2 production, and blocks the expression of IL-2 receptors. Anti-CD3 Antibody (UCHT-1) is applicable to research related to graft-versus-host disease, acute myeloid leukemia, and B-cell acute lymphoblastic leukemia.

Doxycycline-d₃ hyclate (major) is the deuterium labeled Doxycycline hyclate (HY-N0565B). Doxycycline hyclate is an orally active highly lipophilic, tissue-permeable MMP inhibitor with broad-spectrum antibacterial activity. Doxycycline hyclate is also a semi-synthetic antibiotic with chelating properties, which blocks bacterial protein synthesis and inhibits extracellular matrix degradation through interactions with zinc and calcium atoms. Doxycycline hyclate also inhibits mitochondrial biogenesis, translation, and the expression of respiratory chain proteins. Doxycycline hyclate induces apoptosis, inhibits autophagy and EMT, downregulates stem cell markers, and activates the PI3K-AKT pathway, thereby effectively inhibiting the viability and proliferation of cancer cells such as breast cancer cells. Doxycycline hyclate also promotes the survival and self-renewal of embryonic stem cells and neural stem cells, and reduces the frequency of medium changes in culture. Doxycycline hyclate has been applied in studies related to breast cancer, prostate cancer, bladder cancer, and other cancers.