PI3Kα Inhibitor

JMC14 is a selective and orally active PI3Kδ and CSF1R inhibitor with IC₅₀ values of 12 nM and 143 nM, respectively. JMC14 preferentially inhibits PI3Kδ-mediated signaling at the cellular level. JMC14 demonstrates potent antitumor activity against B-cell lymphomas and triple-negative breast cancer (TNBC) in both in vitro and vivo studies. JMC14 can be used for the study of antitumor immunity.

PI3Kγ inhibitor 4 is a potent, selective and orally active inhibitor of PI3Kγ, with an IC₅₀ of 40 nM. PI3Kγ inhibitor 4 shows ∼7, 43, and 18-fold selectivity for PI3Kγ over the α, β, and δ isoforms, respectively. PI3Kγ inhibitor 4 can be used for the research of airway inflammation.

PI3Kα-IN-6 (Compound 5b) is a PI3Kα inhibitor. PI3Kα-IN-6 exhibits anticancer potential and no toxicity in normal cells. PI3Kα-IN-6 increases generation of ROS, reduces mitochondrial membrane potential (MMP) and induces apoptosis.

PI3K/mTOR Inhibitor-9 (Compound 1) is a potent mTOR and PI3K inhibitor with IC₅₀ values of 38 nM, 6.6 μM, 6.6 μM and 0.8 μM against mTOR (phospho-S6 cellular assay), PI3Kα, PI3Kγ and PI3Kδ, respectively.

AM-8508 is an orally bioactive PI3Kδ inhibitor with an IC₅₀ of 0.016 μM. AM-8508 selectively inhibits PI3Kδ, thereby blocking AKT phosphorylation mediated by the B cell receptor. AM-8508 suppresses the formation of antigen-specific IgG and IgM in rats immunized with keyhole limpet hemocyanin. AM-8508 can be used for the research of inflammatory diseases.

AM-1430 is an efficient, highly selective and orally active small molecule inhibitor of PI3Kδ with an IC₅₀ of 4.6 nM. AM-1430 exhibits IC₅₀s for PI3Kα, PI3Kβ and PI3Kγ of 14.18, 2.2 and 3.22 μM, respectively. AM-1430 inhibits B cell proliferation and exhibits excellent in vivo activity in pAKT inhibition models and the hemoglobin (KLH) immune response model. AM-1430 can be used for the study of inflammation and autoimmune diseases.

PI3K-IN-33 (Compound 6e) is a highly selective PI3K inhibitor with IC₅₀ values of 11.73, 6.09 and 11.18 μM for PI3K-α、PI3K-β and PI3K-δ , respectively. PI3K-IN-33 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-33 can be used in leukemia research.

PI3Kα-IN-25 (Compound Djh1) is a selective PI3Kα inhibitor. PI3Kα-IN-25 can be used in triple-negative breast cancer research.

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.

PI3Kα-IN-19 (Compound 1) is a PI3Kα inhibitor with a targeted binding site at the p110α catalytic subunit. PI3Kα is one of the most common dysregulated kinases used in cancer research.

EGFR-IN-217 is an ATP-competitive EGFR kinase inhibitor, with an IC₅₀ of 60.7 nM against EGFR. EGFR-IN-217 exhibits kinase inhibitory activity against PI3K-α and mTOR. EGFR-IN-217 upregulates pro-apoptotic factors including P53, Bax, PUMA, and caspase-7, -8 and -9, and downregulates the anti-apoptotic protein BCL-2, thereby inducing cell apoptosis and cycle arrest. EGFR-IN-217 shows tumor growth inhibitory effects in the solid Ehrlich ascites carcinoma xenograft mouse model. EGFR-IN-217 can be applied in the research of solid Ehrlich ascites carcinoma, hepatocellular carcinoma, and breast cancer.

DHW-221 is a potent orally active dual PI3K/mTOR inhibitor, exhibiting low nanomolar potency against all four Class I PI3K isoforms and mTOR (PI3Kα, IC₅₀ = 0.50 nM; PI3Kβ, IC₅₀ = 1.9 nM; PI3Kγ, IC₅₀ = 1.8 nM; PI3Kδ, IC₅₀ = 0.74 nM; mTOR, IC₅₀ = 3.9 nM). DHW-221 exerts antitumor effects by blocking the PI3K/Akt/mTOR pathway and inducing mitochondrial apoptosis and paraptosis (via Endoplasmic Reticulum (ER) stress and MAPK signaling) and arrests cell cycle, thereby inhibiting cell migration, invasion and angiogenesis. DHW-221 inhibits tumor growth in both the A549/Taxol (HY-B0015) and the HCC827 xenograft mouse models. DHW-221 can be used for non-small cell lung cancer (NSCLC), colon and breast cancer research.

mTOR-IN-31 is a selective mTOR inhibitor with an IC₅₀ of 0.9 nM. mTOR-IN-31 inhibits the proliferation of prostate cancer cells. mTOR-IN-31 is applicable for cancer-related research.

PI3K-IN-38 (compound 123) is an orally active PI3K inhibitor with IC₅₀ of 0.541 µM (PI3K-α). PI3K-IN-38 shows activities of anticancer and anti-inflammatory, which inhibis tumor growth in vivo.

PI3Kα-IN-26 (Compound 11e) is a PI3Kα inhibitor with an IC₅₀ of 75.31 nM. PI3Kα-IN-26 has a broad-spectrum anticancer activity, such as leukemia, colon and breast cancer, without significant cytotoxic effect on the normal Vero cells (mean IC₅₀s of 2.74, 3.50, 3.34 and 85.29 μM, respectively).

LNP23 is a selective PI3Kα inhibitor with an IC₅₀ of 5.15 nM. LNP23 inhibits PI3K/AKT signaling and induces apoptosis and G1 phase arrest in MCF-7 cells. LNP23 also inhibits cancer cell proliferation, colony formation, and migration. LNP23 can be used for breast cancer and lung adenocarcinoma research.

NVP-CLR457 (compound 40) is an orally active, potent and balanced pan-class I PI3K inhibitor. NVP-CLR457 shows a clear dose-dependent PK/PD/efficacy relationship. NVP-CLR457 has antitumor activity.

PI3Kα/CDK7-IN-1 is a dual-target hybrid inhibitor of PI3Kα and CDK7, with IC₅₀ values of 87.9 nM and 638 nM, respectively. PI3Kα/CDK7-IN-1 acts as a cytotoxic agent and cell death inducer that triggers apoptotic death in cancer cells. PI3Kα/CDK7-IN-1 can be used in cancer research such as colorectal cancer.

PI3K-IN-34 (Compound 6g) is a highly selective PI3K inhibitor with IC₅₀ values of 11.73, 6.09 and 11.18 μM for PI3K-α、PI3K-β and PI3K-δ , respectively. PI3K-IN-34 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-34 can be used in leukemia research.

PI3K/HDAC-IN-2 is a potent dual PI3K/HDAC inhibitor with IC₅₀s of 226 nM, 279 nM, 467 nM, 29 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively, and IC₅₀s of 1.3 nM, 3.4 nM, 972 nM, 17 nM, 12 nM for HDAC1, HDAC2, HDC4, HDAC6, HDAC8, respectively. PI3K/HDAC-IN-2 exhibits PI3Kδ and class I and IIb HDAC selectivity. PI3K/HDAC-IN-2 has remarkable anticancer effects.