PI3K Inhibitor

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.

mTOR inhibitor-16 (Compound 9f) is a selective inhibitor for mTOR. mTOR inhibitor-10 inhibits mTOR and PI3K-α, with IC₅₀ of 1.25 and 82 nM. mTOR inhibitor-10 inhibits proliferation of LNCaP with IC₅₀ of 140 nM.

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.

Sorafenib (tosylate) (Standard) (Bay 43-9006 (tosylate) (Standard)) is the analytical standard of Sorafenib (tosylate) (HY-10201A). This product is intended for research and analytical applications. Sorafenib (Bay 43-9006) tosylate is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib tosylate induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib tosylate inhibits tumor growth and metastasis in mouse and rat models. Sorafenib tosylate can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.

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.

Endoxifen Z-isomer methanesulfonate is an orally active selective PKCβ1 inhibitor with an IC₅₀ of 360 nM against human PKCβ1. It also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer methanesulfonate binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer methanesulfonate inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. It can be used in research related to ER⁺ breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors.

Izorlisib (CH5132799) methanesulfonate is an orally active, selective Class I PI3K inhibitor with an IC₅₀ value of 14 nM against PI3Kα. Izorlisib methanesulfonate specifically inhibits Class I PI3K (particularly PI3Kα and its mutants) and blocks the PI3K/Akt/mTOR pathway; this leads to cell cycle arrest at the G1 phase and apoptosis without triggering feedback activation of Akt by competitively binding to the ATP-binding site of PI3K. Izorlisib methanesulfonate can be used in research on cancers harboring PIK3CA mutations or PTEN loss (such as breast, ovarian, prostate, and endometrial cancers).

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.

AM-0687 is a selective inhibitor for PI3Kδ with an IC₅₀ of 2.9 nM. AM-0687 decreases the levels of IgG and IgM specific antibodies, inhibits the anti-IgM/CD40L-induced proliferation of human B cell (IC₅₀=0.8 nM) and the phosphorylation of AKT (IC₅₀=0.7 nM), and exhibits anti-inflammatory efficacy.

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.