PI3K Inhibitor

AM-9635 is a selective PI3Kδ inhibitor with oral bioavailability, good in vitro and in vivo activity and pharmacodynamic properties. AM-9635 inhibits PI3Kδ-dependent B cell receptor-mediated AKT phosphorylation and suppresses the production of specific IgG and IgM antibodies in rats immunized with Aplysia leocyanin (KLH).

Micheliolide is a sesquiterpene lactone with anti-cancer and anti-inflammatory effects, which is derived from Michelia compressa and Michelia champaca. Micheliolide can attenuate high glucose-stimulated NF-κB activation, IκBα degradation, and the expression of MCP-1, TGF-β1, and FN in mouse mesangial cells. Micheliolide inhibits LPS (HY-D1056)-induced activation of NF-κB and PI3K/Akt/p70S6K pathways to play an anti-inflammatory role. Micheliolide inhibits dextran sodium sulphate (DSS) (HY-116282)-induced inflammatory intestinal disease, colitis-associated cancer and rheumatic arthritis.

PI-103 (Standard) is the analytical standard of PI-103. This product is intended for research and analytical applications. PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy.

AZD-7648 (Standard) is the analytical standard of AZD-7648 (HY-111783). This product is intended for research and analytical applications. AZD-7648 is a potent, orally active, selective DNA-PK inhibitor with an IC₅₀ of 0.6 nM. AZD-7648 induces apoptosis and shows antitumor activity.

PIT-1 (Standard) is the analytical standard of PIT-1. This product is intended for research and analytical applications. PIT-1 is a selective PIP3 (phosphatidylinositol 3,4,5-trisphosphate) antagonist. PIT-1 inhibits cancer cell survival and induces apoptosis by inhibition of PIP3 dependent PI3K / Akt signaling. PIT-1 exhibits antitumor activity in vivo.

LY294002 (hydrochloride) (Standard) is the analytical standard of LY294002 (hydrochloride). This product is intended for research and analytical applications. LY294002 hydrochloride is a potent and broad-spectrum PI3K inhibitor, with IC50 values of 0.5, 0.57, and 0.97 μM for P110α, P110δ and P110β, respectively. LY294002 hydrochloride also inhibits CK2 with an IC50 of 98 nM. LY294002 hydrochloride can be used for pancreatic cancer research.

PI3K-IN-11 (compound 13) is a PI3K inhibitor, which selectively inhibits PI3Kα, PI3Kβ, PI3K, and PI3Kδ (IC₅₀s=6.4, 13, 8, and 11 nM, respectively) over mTOR (IC₅₀=2.9 μM). PX-13-17OH is greater than 420-fold selective for PI3K in a panel of 20 lipid and protein kinases. PX-13-17OH inhibits phosphorylation of Akt and S6 kinase (S6K) in PTEN-negative U87MG cells when used at concentrations ranging from 0.03 to 1 μg/mL. It inhibits tumor growth in a U87MG mouse xenograft model when administered at doses ranging from 2.5 to 10 mg/kg.

Polygalacin D3 is a triterpenoid saponin compound that can be extracted from the roots of the balloon flower. Polygalacin D3 can inhibit the proliferation of non-small cell lung cancer (NSCLC) cell lines by blocking the PI3K/Akt pathway, and it induces cell cycle arrest and cell apoptosis.

iMDK (Standard) is the analytical standard of iMDK (HY-110171). This product is intended for research and analytical applications. iMDK is a potent PI3K inhibitor and inhibits the growth factor MDK (also known as midK_ine or MK). iMDK suppresses non-small cell lung cancer (NSCLC) cooperatively with A MEK inhibitor without harming normal cells and mice.

PI-828 (Standard) is the analytical standard of PI-828 (HY-108606). This product is intended for research and analytical applications. PI-828 is a dual PI3K and casein K_inase 2 (CK2) inhibitor with IC₅₀s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid K_inase assay, respectively.

Diphenyl disulfide (Standard) is an analytical standard for diphenyl disulfide (HY-Y1177). This product is intended for research and analytical applications. Diphenyl disulfide (Phenyl disulfide) is an organic disulfide compound. Diphenyl disulfide inhibits the PI3K/AKT/mTOR pathway, and induces ferroptosis (ferroptosis), apoptosis (apoptosis) and autophagy (autophagy) in cancer cells. Diphenyl disulfide downregulates GPX4 expression, inhibits NRF2 phosphorylation, induces lipid peroxidation, promotes xCT ubiquitination, induces proteolytic cleavage of p21 Bax into p18 Bax, and suppresses cell proliferation and viability. Diphenyl disulfide can be used in research related to melanoma and breast cancer.

Neoandrographolide (Standard) is the analytical standard of Neoandrographolide. This product is intended for research and analytical applications. Neoandrographolide is a diterpenoid compound isolated from Andrographis paniculata. Neoandrographolide inhibits osteoclasts differentiation and bone resorption through inhibition of MAPK/NF-κB/PI3K/AKT/GSK3β/PPAR/CAMK signaling pathway. Neoandrographolide inhibits apoptosis in rat embryonic ventricular cardiomyocytes. Neoandrographolide inhibits iNOS and the generation of ROS, activates eNOS, exhibiting anti-inflammatory and hypolipidemic activity.

PI3K/mTOR-IN-21 is a potent dual PI3K/mTOR inhibitor that exhibits favorable overall properties.

Buparlisib (Standard) is the analytical standard of Buparlisib. This product is intended for research and analytical applications. Buparlisib (BKM120; NVP-BKM120) is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.

PF-04979064 (Standard) is the analytical standard of PF-04979064 (HY-100398). This product is intended for research and analytical applications. PF-04979064 is a potent and selective PI3K/mTOR dual kinase inhibitor with Kis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively.

CGS 15943 (Standard) is the analytical standard of CGS 15943. This product is intended for research and analytical applications. CGS 15943 is an orally bioavailable non-xanthine Adenosine Receptor antagonist. Its Ki for human A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively. .

PI3K-IN-1 (Standard) is the analytical standard of PI3K-IN-1. This product is intended for research and analytical applications. PI3K-IN-1 (XL-147 derivative 1) is a potent inhibitor of PI3K. PI3K-IN-1 (25 μM) blocks PI3K/Akt signaling pathways.

Benzoin (Standard) (DL-Benzoin (Standard)) is the analytical standard of Benzoin (HY-B1550). This product is intended for research and analytical applications. Benzoin (DL-Benzoin), a natural balsamic resin, is a PI3Kα inhibitor with anticancer effects. Benzoin inihits the growth of colon cancer cell line (HCT-116). Benzoin can be used as a food additive.

Sipeimine (Standard) is the analytical standard of Sipeimine (HY-N0696R). Sipeimine (Imperialine) is an inhibitor targeting the PI3K/AKT/NF-κB pathway and NLRP3 inflammasome, which can competitively bind to PI3K and p65. Sipeimine inhibits PI3K/AKT phosphorylation, blocks NF-κB nuclear translocation and NLRP3 inflammasome activation. Sipeimine exerts anti-inflammatory activities, inhibits pyroptosis and ferroptosis, and protects the extracellular matrix. Sipeimine can reduce cartilage degradation and synovial inflammation in osteoarthritis and improve PM2.5-induced lung injury. Sipeimine is mainly used in the study of anti-inflammatory and degenerative diseases.

CeY-B1 is a ceramide analog. CeY-B1 inhibits the proliferation, migration and invasion of cervical cancer cells, induces apoptosis and cell cycle arrest. CeY-B1 upregulates ASK1, promotes the phosphorylation of JNK, downregulates Bcl‑2, and inhibits the PI3K/AKT pathway. CeY-B1 suppresses tumor growth in cervical cancer xenograft mouse models. CeY-B1 can be used for relevant research on cervical cancer.