pi3kδ-in-1

PI3Kδ-IN-1 is an efficacious PI3Kδ inhibitor (IC50 of 1.7 nM).

PI3K-IN-1 (Voxtalisib Analogue) is a dual inhibitor of mTOR/PI3K, mostly for p110γ , also inhibits DNA-PK and mTOR.

PARP/PI3K-IN-1 is a novel dual poly (ADP-ribose) polymerase (PARP) and phosphatidylinositol 3-kinase (PI3K) dual inhibitor with anticancer, antitumour and antiproliferative activities for the study of breast, pancreatic and lung cancers.

EGFR/PI3Kα-IN-1 (compound 30k), a dual EGFR/PI3Kα inhibitor, exhibits potent activity with IC 50 values of 3.6 nM (EGFRL858R/T790M) and 30 nM (PI3Kα). It effectively inhibits tumor cell proliferation and demonstrates significant anticancer activity.

PI3Kδ/γ-IN-1 is a selective and efficacious inhibitor of PI3Kδ/γ, suitable for treating hematologic malignancies.

PI3Kβ-IN-1 is a selective, orally active PI3Kβ inhibitor (IC50: 2 nM).

PI3Kα-IN-1 is an inhibitor specifically targeting PI3Kα with an IC50 of less than 0.5 nM, and it also inhibits mTOR with an IC50 of 104 nM [1].

PI3Kδ-IN-12 (compound 13), a PI3Kδ inhibitor with a pIC50 of 5.8, exhibits differential binding affinities with pKi values of 8.0 for PI3Kδ, 6.5 for PI3Kγ, 6.4 for PI3Kβ, and 6.7 for PI3Kα. This compound is used in researching chronic respiratory conditions, including asthma and chronic obstructive pulmonary disease (COPD) [1].

PI3Kδ-IN-14 (Compound (S)-29), a selective PI3Kδ inhibitor with an IC50 of 0.8 nM and a Kd of 84.8 nM, targets the ATP-binding site within the kinase domain of PI3Kδ, exhibiting anti-inflammatory properties by impeding the PI3K/AKT pathway and alleviating acute lung injury (ALI) [1].

Se15, a selective PI3Kδ inhibitor, exhibits potency with an IC50 value of less than 0.1nM and is utilized in autoimmune research [1].

PI3Kδ-IN-17 (Compound S5) is a potent PI3K δ inhibitor with an IC50 value of 2.82 nM, significantly inhibiting SU-DHL-6 cell proliferation with an IC50 of 0.035 μM [1].

PI3Kδ-IN-10 is a highly potent and orally active PI3Kδ inhibitor (IC50 = 2 nM) that robustly suppresses the downstream AKT pathway to induce subsequent apoptosis in hepatocellular carcinoma models.

PI3Kδ-IN-11 is a potent and selective PI3Kδ inhibitor (IC50: 27.5 nM) that dose-dependently blocks PI3K/Akt pathway activity. PI3Kδ-IN-11 can be used in B- or T-cell-associated malignancy studies.

PI3Kδ-IN-16 is a selective and potent PI3Kδ inhibitor with anticancer and antiproliferative activity, induces cell cycle arrest and apoptosis.

PI3Kδ-IN-15 is a selective PI3Kδ inhibitor that inhibits PI3Kδ more than 30-fold more effectively than PI3Kγ, PI3Kβ, and PI3Kα.

MEK/PI3K-IN-1 (compound 6r) is a potent dual inhibitor of MEK and PI3K, exhibiting IC50 values of 124 nM for MEK1, 130 nM for PI3Kα, and 236 nM for PI3Kδ. It effectively reduces pAKT and pERK1/2 levels, demonstrating anti-proliferative effects on various tumor cell lines [1].

PI3K-IN-10 is a potent inhibitor of pan-PI3K (Phosphoinositide 3-kinase).

PI3K-IN-19 hydrochloride (WO2017153220, step 5) acts as a phosphatidylinositol-3-kinase (PI3K) inhibitor.

COX-2/PI3K-IN-1 (compound 5d) is a potent inhibitor of PI3K with an IC50 of 1.14 nM and selectively inhibits COX-2 with a Ki of 3.24 nM.

PI3K/HDAC-IN-1 is a potent dual inhibitor of PI3K and HDAC, with IC50 values of 8.1 nM and 1.4 nM, respectively.

PI3Kδ/BET-IN-1 (compound 10b) exhibits excellent and balanced activity against PI3Kδ (IC50= 112 nM) and BRD4-BD1 (IC50= 19 nM), while also demonstrating strong antiproliferative effects in DLBCL cells.

PI3Kδ-IN-22 (Compound 26) is a selective inhibitor of PI3Kδ with a pKi value of 9.3. It effectively inhibits the PI3Kδ-AKT signaling pathway in THP-1 cells, demonstrating a pIC50 of 9.4. Additionally, PI3Kδ-IN-22 exhibits favorable pharmacokinetic properties in rats.

PROTACPI3Kα degrader-1 is a PI3Kα-targeting PROTAC degrader (DC50= 0.08 μM) that demonstrates notable selectivity in degrading PI3Kα over the PI3Kβ, PI3Kγ, and PI3Kδ isoforms. It degrades PI3Kα effectively in a time- and concentration-dependent manner and significantly inhibits the phosphorylation of AKT at the Ser473 site. Additionally, PROTACPI3Kα degrader-1 exhibits significant in vivo anticancer efficacy in HGC-27 and DOHH2 xenograft models.

(S,R,S)-AHPC-Me-10-bromodecanoic acid is an E3 ligase ligand-linker conjugate composed of VHL ligand 2 and the linker 10-bromoheptanoic acid. This compound can be utilized in the synthesis of PROTACPI3Kδ degrader-1.