pi-3

Tandutinib (CT53518) (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 μM), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR, and KDR.

Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3' hydroxyl position of PIs to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits, whereas PI3Kγ is a class 1B PI3K composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit. PI3Kα inhibitor 2 is a selective inhibitor of PI3Kα with IC50 values of 2, 16, 660, and 220 nM for the α, β, γ, and 2Cβ isoforms, respectively. It inhibits PKA, KDR, PKCα, and cyclin E/Cdk2 significantly less effectively (IC50 = 91, 3.4, 466, and 28 μM, respectively). PI3Kα inhibitor 2 inhibits A375 melanoma cell proliferation with an IC50 value of 580 nM.

NVS-PI3-4 is a highly selective inhibitor of the enzyme PI3Kγ. It is specifically designed for use in scientific investigations related to allergies, inflammatory conditions, and cancerous diseases[1][2].

KP-23172 is a inhibitor of PI3-K/Akt pathway.

PI3K-IN-60 (Compound 34) is a selective PI3Kγ inhibitor for studying autoimmune diseases and cancers such as multiple sclerosis, breast cancer, and pancreatic ductal adenocarcinoma.

PI3-Kinase inhibitor targets PI3Kγ with an IC50 of 1.5 nM and shows selectivity over PI3Kα, PI3Kβ, and PI3Kδ, exhibiting IC50 values of 3,333 nM, >10,000 nM, and >1,000 nM, respectively. At 100 mg/kg, it reduces tumor growth in a 4T1 murine mammary cancer model. In a mouse model of experimental autoimmune encephalomyelitis (EAE), it lessens disease severity when administered at doses of 20 or 80 mg/kg.

CPI-360 is a small molecule EZH2 inhibitor (IC50: 0.002 μM, EC50: 0.080 μM) that shows antitumor activity in an EZH200-dependent tumor xenograft model.

PI-3065 is a novel potent and selective PI3K p110δ inhibitor.

DPI-3290 is a specific agonist of opioid receptors (Ki: 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively) with potent antinociceptive activity. DPI-3290 is one of a series of novel centrally acting agents.

IPI-3063 is an effective and selective inhibitor of PI3K p110δ (IC50: 2.5 ± 1.2 nM).

GPI-3000 is an NMDA receptor antagonist with potential neuroprotective properties. It may enhance recovery from metabolic damage and has applications in research on metabolic and neurological disorders.

SCPI-3 is a potent and competitive inhibitor of mosquito sterol carrier protein-2 (SCP-2), with inhibition concentrations of AeSCP-2IC50 = 0.159 µM and AeSCP-xIC50 = 0.285 µM. It physiologically impacts cholesterol metabolism in cultured insect cells, showing an IC50 of 3.09 µM in Aag-2 cells. SCPI-1 exhibits insecticidal activity against Aedes aegypti, with an LD50 of 12.3 µM.

RBPI-3 is a canonical poly(ADP-ribose) glycohydrolase.

FAPI-34, a fibroblast-activating protein (FAP) inhibitor, boasts advantageous pharmacokinetic and biochemical attributes.

EPI-326 is a selective bispecific antibody that targets and degrades both oncogenic mutant and wild-type EGFR. EPI-326 binds specifically to tumor tissue, induces EGFR endocytosis and lysosomal degradation, clears EGFR protein, and blocks oncogenic signaling. EPI-326 is being investigated for use in the treatment of advanced solid tumors.

2-Epi-3a-epiburchellin is a natural product for research related to life sciences. The catalog number is TN2756 and the CAS number is 57457-99-5.

Tetrahydroepiberberine, an isoquinoline alkaloid, has antifungal and selective inhibition against the PI-3 virus activities.

LY294002 (SF 1101) is a broad-spectrum inhibitor of PI3K, inhibiting PI3Kα, PI3Kδ, and PI3Kβ (IC50=0.5/0.57/0.97 μM). LY294002 is also an inhibitor of DNA-PK (IC50=1.4 μM) and an inhibitor of CK2 (IC50=98 nM). LY294002 activates apoptosis and autophagy.

Quercetin, a flavonoid natural product, is a SIRT1 activator. It is also a PI3K inhibitor, inhibiting PI3Kγ, PI3Kδ, and PI3Kβ with IC50 values of 2.4, 3.0, and 5.4 μM, respectively. Recognized as a heat shock protein inhibitor, Quercetin can significantly reduce exosome release in TII models by downregulating Hsp70 or Hsp90.

Recilisib (ON 01210) is a radioprotectant that activates AKT and PI3K activities in cells.

Inavolisib (GDC-0077) is an orally available selective PI3Kα inhibitor with an IC50 value of 0.038 nM.It exerts its activity by binding to the ATP-binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3.

3-Methyladenine (3-MA) is a PI3K inhibitor that selectively inhibits class IB PI3Kγ (IC50 = 60 μM) and class III VPS34 (IC50 = 25 μM). 3-Methyladenine inhibits autophagy.

Alpelisib (BYL-719) is a PI3Kα inhibitor (IC50=5 nM) with selective, potent, and oral activity, inhibiting PI3Kβ/γ/δ with low activity (IC50=250/290/1200 nM). Alpelisib demonstrates antitumor activity and specifically targets PIK3CA mutant tumors.

Cytochalasin D is an actin inhibitor, the removal of actin stress fibers is crucial for the chondrogenic differentiation. It may be an inhibitor of some fertilization processes such as sperm penetration or sperm head decondensation. Cytochalasin D inhibit