Toyaburgine is a unique isoquinoline compound that exhibits anti-tumor activity. It packs a punch by disrupting the PI3K/AKT/mTOR signaling pathway, causing significant morphological changes and cell death in MIA PaCa-2 cells. On top of that, it puts the brakes on cell migration and colony formation. This compound is showing a lot of promise in the realm of pancreatic cancer research.

KIM-161 is a PIK3CA inhibitor. KIM-161 has significant antiproliferative activity with IC50 values of 1.428 and 1.562 µM against PI3KCA mutant breast cancer MCF7 and T47D cells, respectively. KIM-161 induces apoptosis and cell cycle arrest by inhibiting the PI3K/AKT/mTOR signaling pathway and inducing ROS production. KIM-161 can be used to study breast cancer and its PI3KCA mutant subtypes.

JZ19 reduces the LDH and ROS levels, and exhibits antioxidant activity against oxygen-glucose deprivation (OGD)-induced cardiomyocyte injury. JZ19 reverses Isoproterenol-induced cardiomyocyte hypertrophy and apoptosis through PI3K-AKT-GSK3β signaling pathway. JZ19 alleviates Isoproterenol-induced heart failure in mouse models.

Hydroxy celecoxib is a Celecoxib. N-Stearoyltyrosine exhibits neuroprotective efficacy in gerbils ischemia-reperfusion model through protection in the CA1 region of the hippocampus. N-Stearoyltyrosine inhibits the free radicals production and improves antioxidant capacity. N-Stearoyltyrosine inhibits the IR-induced apoptosis.

Erufosine is an inhibitor of PI3K/Akt and Ras/Raf/MAPK signaling pathways. Erufosine inhibits the activity of breast cancer cell lines MCF-7 and MDA-MB 231 (IC50: 40.95/40.8 μM). Erufosine reduces the phosphorylation of PI3K (p85), Akt (PKB), and cRaf. Erufosine can be used in the study of breast cancer and myeloid leukemia.

Dactolisib (BEZ235) hydrochloride is an orally active, dual pan-class I PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR with IC50 of 4 nM/5 nM/7 nM/75 nM and 20.7 nM, respectively. Dactolisib hydrochloride (BEZ235) inhibits mTORC1 and mTORC2.

D-106669 (comppun 150) is a potent inhibitor of PI3Kα, with the IC50 of 0.129 μM. D-106669 plays an important role in cancer research.

AS-605240 (potassium) is an orally active PI3Kγ inhibitor (IC50: 8 nM; Ki: 7.8 nM). AS-605240 (potassium) inhibits MCP-1- and CSF1-induced PKB phosphorylation (IC50 values are 0.181 and 0.550 µM, respectively). AS-605240 (potassium) reduces neutrophil recruitment in RANTES (CCL5)- and thioglycolate-induced peritonitis mouse models (EC50 values are 9.1 and 10 mg/kg, respectively). AS-605240 (potassium) ameliorates αCII-IA-induced arthritis in mice.

(S)-RLY-2608 is an S-enantiomer of of RLY-2608, an RNA-degrading chimera which binds to a four-way RNA helix called SL5 in the 5’ UTR of the SARS-CoV-2 RNA genome and inhibits the virus replication in lung epithelial carcinoma cells. RNA recruiter-linker 1 can be utilized in the synthesis of RIBOTAC.

(2S)-SB02024 (SB02877), the S-enantiomer of SB02024 -induced novel object recognition (NOR) models. VU6024578 is blood brain barrier penetrable.

Duvelisib (IPI-145) is a selective inhibitor of the p110δ isoform, exhibiting IC50 values of 2.5 nM, 27.4 nM, 85 nM, and 1602 nM for p110δ, p110γ, p110β, and p110α, respectively, highlighting its specificity and potency.

PI3K-IN-20 is a PI3k inhibitor extracted from WO2017101847 A1, compound 1.

Leniolisib (CDZ173) phosphate is a potent and selective PI3Kδ inhibitor. Leniolisib phosphate has the potential for immunodeficiency disorders treatment.

Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor currently in phase II/III clinical trials for the treatment of immunodeficiency disorders.

Seletalisib (UCB5857) is potent and selective PI3Kδ inhibitor with an IC50 of 12 nM.

IPI-549 is an orally administered immuno-oncology development candidate that selectively inhibits PI3K-gamma.

cyclo-CRVLIR is a cyclic peptide that binds selectively to p110α RAS binding domain (p110α-RBD) with ITC Kd of 3 uM, blocks p110α/RAS interaction in vitro and KRAS cancer cell lines.

TGX286 is a potent, selective p110β inhibitor with IC50 of 7, 17 and 13 nM for p110β WT, p110β D862Q, and p110β E858H, respectively, >100-fold selectivity over p110α.

PITCOIN3 is a potent, highly selective, cell-permeable inhibitor of PI3KC2α catalytic activity with IC50 of 126 nM.

PITCOIN2 (LU-06-006) is a potent selective PI3KC2α inhibitor with IC50 of 126 nM, has selectivity against PI3KC2γ but shows micromolar activity on PI3KC2β.

PF-06862309 (PF-06843195 phosphate ester prodrug) is the in vivo-active, phosphate ester prodrug of PF-06843195, a potent selective PI3Kα inhibitor with Kd of <18 pM.

LP-182 (LP182) is a potent, selective and orally bioavailable multi-functional kinase inhibitor, specifically targets PI3K and MAPK signaling pathways.

LL-00084282 is a potent, selective and efficacious dual PI3Kδγ inhibitor with IC50 of 16.26 and 17.45 nM for PI3Kδ and PI3Kγ, respectively.

LL-00071210 is a potent, selective, orally bioavailable PI3Kδ inhibitor with IC50 values of 24.6 nM and 9.4 nM in biochemical and cellular assays, respectively.

I-229 is a potent and selective inhibitor of Vps34.

HM5023507 is a potemt, selective, orally active dual PI3Kδ/γ inhibitor with IC50 of 4 nM and 5 nM for p110γ and p110δ, respectively.

PF-04691502 is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK.

A66 is a potent and specific p110α inhibitor with IC50 of 32 nM, >100 fold selectivity for p110α over other class-I PI3K isoforms.

GDC-0980 (RG7422) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM, respectively. Also a mTOR inhibitor with Ki of 17 nM, and highly selective versus others PIKK family kinases.

MSC2360844 is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. MSC2360844 shows highly selective against a panel of 278 additional kinases.