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).

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

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

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.

Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K.

AZD-7648 is an inhibitor of DNA-dependent protein kinase (DNA-PK) with the IC50 of 0.63 nM in an enzyme assay,has anti-tumor activity.

RLY-2608 is a selective mutant PI3Kα inhibitor that inhibits tumor growth in a PIK3CA mutant xenograft model.

Taurocholic acid (N-Choloyltaurine) is a bile acid involved in fat emulsification, possessing notable biological and immunomodulatory activities. It can inhibit bile duct injury induced by hepatic artery ligation by upregulating VEGF-A expression and protect cholangiocytes from TNF-α-induced damage via a PI3K-mediated pathway, and is commonly used to induce pancreatitis models.

740 Y-P acetate (740YPDGFR acetate) is a potent and cell-permeable PI3K activator.740 Y-P acetate tends to bind to GST fusion proteins containing the N- and C-terminal SH2 structural domains of p85, but not to GST alone.