PI3K Inhibitor

MPT0L145 is a PIK3C3/FGFR inhibitor, with a K_d value of 0.53 nM for PIK3C3. MPT0L145 decreases the phosphorylation of FGFR1, FGFR3 and their downstream proteins (FRS2, ERK and Akt). MPT0L145 induces G0/G1 cell cycle arrest and decreased protein levels of cyclin E. MPT0L145 promotes mitochondrial dysfunction, ROS production, and DNA damage. MPT0L145 is an autophagy inhibitor. MPT0L145 significantly sensitizes cancer cells to targeted or chemotherapeutic agents. MPT0L145 can be used for cancer research, such as bladder cancer and NSCLC.

PI3Kα-IN-8 (Compound 9g) is a selective PI3Kα inhibitor with an IC₅₀ of 0.012 μM. PI3Kα-IN-8 increases intracellular reactive oxygen species level, decreases mitochondrial membrane potential and induces apoptosis.

PI3Kα-IN-1 is a PI3Kα inhibitor (IC₅₀ < 0.5 nM), and also inhibits mTOR (IC₅₀: 104 nM).

Alpelisib GMP is Alpelisib (HY-15244) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Alpelisib (BYL-719) is an orally active PI3Kα-selective inhibitor that blocks the conversion of PIP2 to PIP3, thereby inhibiting pathways including PI3K/AKT/mTOR, MAPK/ERK, Notch and JAK-STAT. Alpelisib also induces apoptosis, G0/G1 phase arrest and senescence; it significantly inhibits the proliferation, self-renewal, stemness and epithelial-mesenchymal transition (EMT) of tumor cells, reduces cancer stem cell populations and decreases the expression of stem cell markers. Alpelisib not only enhances the sensitivity to Eribulin (HY-13442) and exerts a synergistic effect with Paclitaxel (HY-B0015), but may also induce drug resistance by upregulating the SGK3/GSK3β/β-catenin signaling pathway. Alpelisib can be applied to research related to breast cancer, gastric cancer and lipomas associated with PTEN hamartoma tumor syndrome.

PI-540 is a bicyclic thienopyrimidine derivative and an orally active PI3K inhibitor. PI-540 has anti-cancer cell proliferation properties and high tissue distribution. PI-540 can inhibit different isoforms of PI3K, with IC₅₀s of 10 nM (P110α), 3510 nM (P110β), 410 nM (P110δ), and 33110 nM (P110γ). PI-540 also inhibits mTOR (IC₅₀: 61 nM) and DNA-PK (IC₅₀: 525 nM).

KRASG12C IN-16 (Compound SK-17) is a selective, covalent and an orally active KRAS^G12C inhibitor. KRASG12C IN-16 induces Apoptosis. KRASG12C IN-16 effectively prevents the activation of MAPK and PI3K/mTOR signaling pathways. KRASG12C IN-16 displays anti-tumor activity against pancreatic cancer.

PI3Kδ-IN-26 (Compound 58) is a selective and orally active PI3Kδ inhibitor with an IC₅₀ of 14  nM. PI3Kδ-IN-26 significantly attenuates the inflammatory responses in house dust mite (HDM) induced chronic asthma mouse models. PI3Kδ-IN-26 can be used for inflammatory, autoimmune and hyperproliferative diseases research.

PI3K/VEGFR2-IN-1 is a potent dual PI3K/VEGFR2 inhibitor with IC₅₀ values of 2.21 and 68 μM for PI3K and VEGFR2, respectively. PI3K/VEGFR2-IN-1 induces apoptosis. PI3K/VEGFR2-IN-1 can be used in research of cancer.

LTURM 36 (20i) is a PI3K inhibitor, with IC₅₀ values ​​of 0.64 μM and 5.0 μM for PI3Kδ and PI3Kβ, respectively. LTURM 36 can be used in anticancer research.

PI3K/AKT-IN-6 is an orally effective PI3K/AKT signaling pathway inhibitor and anti-inflammatory agent. PI3K/AKT-IN-6 inhibits the production of pro-inflammatory cytokines TNF-α and IL-6, and downregulates the expression of inflammatory mediators COX-2 and iNOS. PI3K/AKT-IN-6 improves related symptoms in colitis mice. PI3K/AKT-IN-6 can be used for the research of inflammatory diseases such as colitis.

(R)-HM5023507 (Compound 470) is a potential PI3K inhibitor. (R)-HM5023507 can be used for the research of cancer, inflammatory, allergic and autoimmune diseases and leukemia etc.

PI4KIII beta inhibitor 4 (Compound 16) is a selective PI4KIIIβ inhibitor with an IC₅₀ of 0.005 μM. PI4KIIIβ inhibitor 4 induces tumor cell apoptosis, cell cycle arrest, and autophagy by inhibiting the PI3K/AKT pathway. PI4KIIIβ inhibitor 4 can be used in the study of cancer.

CC-M-1 is a potent and selective PI3K/mTOR inhibitor. CC-M-1 inhibits PI3Kα/β/γ/δ and mTOR with IC₅₀ values of 0.68, 1.02, 1.03, 8.03, and 15 nM, respectively. CC-M-1 inhibits the proliferation of colorectal cancer cell lines, including HCT-116 (IC₅₀ = 0.38 μM) and HT-29 (IC₅₀ = 1.70 μM). CC-M-1 can be used for colorectal cancer (CRC) research.

Topoisomerase I/II inhibitor 3 (compound 7) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 3 can inhibit cell proliferation, invasion and migration, and induce apoptosis by inhibiting PI3K/Akt/mTOR signaling pathway. Topoisomerase I/II inhibitor 3 can be used for liver cancer research.

PI3Kδ-IN-14 (Compound (S)-29) is a selective PI3Kδ inhibitor (IC₅₀: 0.8 nM, K_d: 84.8 nM). PI3Kδ-IN-14 binds to the ATP-binding site of the kinase domain of PI3Kδ. PI3Kδ-IN-14 has anti-inflammatory activity by inhibiting the PI3K/AKT pathway. PI3Kδ-IN-14 ameliorates acute lung injury (ALI).

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

Flavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer.

Plantamajoside (Standard) is the analytical standard of Plantamajoside. This product is intended for use in research and analytical applications. Plantamajoside is an orally active phenylpropanoid glycoside. Plantamajoside can be isolated from Plantago asiatica L.(Plantaginaceae). Plantamajoside inactivates NF-κB, PI3K/akt, induces Apoptosis, and improves Autophagy. Plantamajoside regulates MAPK, integrin-linked kinase/c-Src. Plantamajoside inhibits multiple cancers, improves lung and kidney damage. Plantamajoside has neuroprotective and anti-inflammatory effects.

BAY1082439 (Standard) is the analytical standard of BAY1082439 (HY-100886). This product is intended for research and analytical applications. BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth.

Umbralisib (hydrochloride) (Standard) is the analytical standard of Umbralisib (hydrochloride). This product is intended for research and analytical applications. Umbralisib (TGR-1202) hydrochloride is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib hydrochloride exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib hydrochloride can be used for haematological malignancies reseach.