pi3kδ inhibitor 1

PI3kδ inhibitor 1 is a selective inhibitor of PI3Kδ (IC50 of 3.8 nM).

Selective PI3Kδ Inhibitor 1 is a PI3Kδ Inhibitor( IC50 = 0.9 nM).

PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual inhibitor of PI3K/mTOR (PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ/mTOR with IC50s of 20/376/204/46/186 nM).

PI3Kγ inhibitor 1 is a inhibitor of PI3Kδ and PI3Kγ.

GS-9901 is a selective, orally active and potent PI3Kδ inhibitor (IC50: 1 nM) for the study of non-Hodgkin's lymphoma and chronic lymphocytic leukemia.

ATM Inhibitor-1 is a highly potent, selective, and orally active ATM inhibitor (IC50: 0.7 nM) with anti-tumor activity. It exhibits weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM), and PI3Kδ (IC50, 0.73 μM).

Parsaclisib (INCB050465) is a potent and selective inhibitor of PI3Kδ(IC50 of 1 nM at 1 mM ATP)

PI3Kdelta inhibitor 1 is a potent, selective and orally available inhibitor of PI3Kδ with an IC50 of 1.3 nM.

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

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.

PI3Kδ/HDAC6-IN-1 (Compound 22E) is an orally active dual inhibitor of PI3Kδ and HDAC6, with IC50 values of 2.4 nM and 6.2 nM, respectively. It exhibits potent antiproliferative effects against non-Hodgkin's lymphoma (NHL) cells and demonstrates antitumor activity in vivo without significant toxicity. PI3Kδ/HDAC6-IN-1 induces cell cycle arrest at the G0/G1 phase and triggers apoptosis. Additionally, it inhibits the PI3K/AKT/mTOR signaling pathway and enhances the acetylation levels of α-tubulin and histone H3.

DHW-221 is an orally active dual PI3K/mTOR inhibitor demonstrating potent inhibition at nanomolar levels across 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). By blocking the PI3K/Akt/mTOR pathway, DHW-221 induces mitochondrial apoptosis and paraptosis (through endoplasmic reticulum stress and MAPK signaling) and causes cell cycle arrest, thereby inhibiting cell migration, invasion, and angiogenesis to exert its antitumor effects. It suppresses tumor growth in A549/Taxol and HCC827 mouse models and is applicable in research related to non-small cell lung cancer (NSCLC), colon cancer, and breast cancer[1][2][3].

Parsaclisib hydrochloride (INCB050465 HCl) is a selectve PI3Kδ inhibitor with antitumor activity. Parsaclisib demonstrates potent activity with IC50 values ranging from 0.2 to 2 nM.

(S)-PI3Kα-IN-4, a potent inhibitor of PI3Kα with an IC50 of 2.3 nM, demonstrates 38.3-, 4.25-, and 4.93-fold selectivity over PI3Kβ, PI3Kδ, and PI3Kγ, respectively, and is suitable for cancer research[1]. (S)-PI3Kα-IN-4 (compound 11) is a quinazolin-4(3H)-one derivative with 2-substituted-N-methylpropanamide substitution[1].

FD223 is a potent, selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor with a marked affinity (IC50=1 nM), demonstrating notable selectivity against other isoforms (IC50s: α=51 nM, β=29 nM, γ=37 nM). This compound effectively suppresses the proliferation of acute myeloid leukemia (AML) cell lines by inhibiting p-AKT Ser473, thereby inducing G1 phase cell cycle arrest. FD223 holds promise for leukemia research, particularly in AML[1].

DS-7423 is a dual PI3K and mTOR inhibitor, with IC50 values of 15.6 nM and 34.9 nM for PI3Kα and mTOR, respectively, and exhibits anti-tumor activity[1][2]. It increases TP53 expression, the level of p-TP53 on Ser-46, and induces apoptosis-related TP53 target genes (TP53AIP1 and PUMA) in OCCC cells[1]. DS-7423 also inhibits other isoforms of class I PI3K with IC50 values of 1,143 nM for PI3Kβ, 249 nM for PI3Kγ, and 262 nM for PI3Kδ[2]. [1]. Katsutoshi Oda, et al. Characterization of TP53 and PI3K signaling pathways as molecular targets in gynecologic malignancies. J Obstet Gynaecol Res. 2016 Jul;42(7):757-62. [2]. Tomoko Kashiyama, et al. Antitumor activity and induction of TP53-dependent apoptosis toward ovarian clear cell adenocarcinoma by the dual PI3K/mTOR inhibitor DS-7423. PLoS One. 2014 Feb 4;9(2):e87220.

PI3K/mTOR Inhibitor-9 (Compound 1) is a potent inhibitor of both mTOR (IC50: 38 nM) and PI3K, including PI3Kα (IC50: 6.6 nM), PI3Kγ (IC50: 6.6 nM), and PI3Kδ (IC50: 0.8 nM).

PI3K/AKT-IN-1 is a dual PI3K and AKT inhibitor with anti-cancer activity. It inhibits PI3Kγ, PI3Kδ, and AKT, suppressing the PI3K/AKT pathway and inducing caspase 3-dependent apoptosis, suitable for cancer research.

PI3Kδ/γ-IN-3 (Compound 58) is an orally active dual inhibitor of PI3Kδ (IC50: 1 nM) and PI3Kγ (IC50: 16 nM), effective in inducing apoptosis of tumor cells and applicable to B-cell malignant tumor studies.

PI3Kδ/γ-IN-2 is a potent, orally bioavailable dual inhibitor of PI3Kδ (IC50: 1 nM) and PI3Kγ (IC50: 4.3 nM), with potential for use in anti-B-cell malignancy studies.

PI3Kδ/γ-IN-1 is a potent, selective inhibitor of the PI3Kδ/γ subtypes, with an IC₅₀ of 4.2 nM for PI3Kδ and 7.5 nM for PI3Kγ. PI3Kδ/γ-IN-1 is primarily used for mechanistic studies of hematological malignancies such as leukemia and lymphoma.

Umbralisib Tosylate (TGR-1202) is a potent, selectively dual inhibitor targeting PI3Kδ and casein kinase-1-ε (CK1ε), demonstrating oral activity. With EC50 values of 22.2 nM and 6.0 μM for PI3Kδ and CK1ε respectively, it shows unique immunomodulatory effects on T cells in chronic lymphocytic leukemia (CLL). This compound is utilized in the research of hematological malignancies.

Umbralisib (TGR-1202) sulfate, an orally active compound, serves as a potent, selective inhibitor targeting both PI3Kδ and casein kinase-1-ε (CK1ε), with EC50 values of 22.2 nM and 6.0 μM, respectively. It demonstrates unique immunomodulatory effects on T cells in chronic lymphocytic leukemia (CLL) and is applicable in the research of hematological malignancies.

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].