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Catalog No.
Product Name
Application
Product Information
Citations
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PI3K Inhibitor
NVP-BKM120 Hydrochloride is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. Reduced potency against VPS34, mTOR, DNA-PK, with little activity to PI4Kβ. -
PI3K Inhibitor
PI103 is a potent inhibitor with low IC50 values against recombinant PI3K isoforms p110alpha (IC50= 2 nM), p110beta (IC50= 3 nM), p110delta (IC50= 3 nM), and p110gamma (IC50= 15 nM), less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. -
PI3K Inhibitor
XL147 is a potent, orally bioavailable inhibitor of the class I PI3K family of lipid kinases. -
p110α inhibitor
MLN1117, also known as INK1117 and TAK-117, is an orally bioavailable inhibitor of the class I phosphoinositide 3-kinase (PI3K) alpha isoform with potential antineoplastic activity. -
PI3K-δ/PI3K-γ inhibitor
IPI-145, also known as INK-1197, is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities. -
PI3K inhibitor
GDC-0032 is a potent, next-generation PI3 inhibitor targeting PI3 alpha. -
PI3K inhibitor
PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively. -
PI3K/mTOR Dual Inhibitor
PF-04979064 is a highly potent and orally bioavailable PI3K/mTOR dual inhibitor. -
PI3Kα/β/δ Inhibitor
BAY1082439 is a selective inhibitor of the PI3Kα, β, and δ isoforms, demonstrating oral bioavailability. This compound effectively inhibits both wild-type and mutated forms of PIK3CA, making it a valuable tool in cancer research. Notably, BAY1082439 has shown significant efficacy in suppressing the growth of Pten-null prostate cancer, highlighting its potential in therapeutic applications targeting specific tumors. -
PI3Kα Inhibitor
PI3Kα-IN-9 is a selective inhibitor of PI3Kα, exhibiting an IC50 of 4.4 nM while demonstrating lesser potency against PI3Kγ, PI3Kδ, and PI3Kβ with IC50 values of 128, 146, and 153 nM, respectively. This compound is notable for its long-acting oral activity and ability to induce apoptosis alongside antiproliferative effects in cancer cells. PI3Kα-IN-9 serves as a valuable reagent for cancer research, particularly in studies focused on PI3K signaling pathways. -
PI3k/Akt/mTOR Inhibitor
D-87503 is a potent inhibitor of the PI3K/Akt/mTOR signaling pathway, exhibiting IC50 values of 62 nM for PI3K and 0.76 μM for Erk2. This compound effectively attenuates the activity of downstream substrates, including Akt and Rsk1, making it a valuable tool for studying cellular processes regulated by this pathway. D-87503 has applications in cancer research and investigates the role of PI3K signaling in various physiological conditions. -
PI3Kδ/CK1ε Inhibitor
Umbralisib tosylate is a potent and selective dual inhibitor of PI3Kδ and casein kinase-1-ε (CK1ε), exhibiting an EC50 of 22.2 nM and 6.0 μM, respectively. This compound demonstrates significant immunomodulatory effects on T cells from chronic lymphocytic leukemia (CLL) patients. Umbralisib tosylate is primarily utilized in research focused on hematological malignancies to elucidate its therapeutic potential and mechanisms of action. -
PI3Kδ/CK1ε Inhibitor
Umbralisib sulfate is a potent and selective dual inhibitor of PI3Kδ and casein kinase-1-ε (CK1ε), with EC50 values of 22.2 nM and 6.0 μM, respectively. This compound demonstrates notable immunomodulatory effects on T cells in chronic lymphocytic leukemia (CLL). Umbralisib sulfate is a valuable tool for research into hematological malignancies, facilitating studies on cell signaling pathways and potential therapeutic strategies. -
PI3K/mTOR Inhibitor
Dactolisib hydrochloride is a potent dual inhibitor of class I phosphoinositide 3-kinases (PI3K) and the mammalian target of rapamycin (mTOR), specifically targeting p110α, p110γ, p110δ, and p110β with IC50 values of 4 nM, 5 nM, 7 nM, 75 nM, and 20.7 nM, respectively. This compound effectively inhibits both mTORC1 and mTORC2, making it a valuable tool for studying the PI3K/mTOR signaling pathway. Its applications include cancer research, drug development, and exploring therapeutic strategies for various diseases associated with dysregulated PI3K/mTOR signaling. -
PI3Kα Inhibitor
PI3Kα-IN-14 is a selective inhibitor of the phosphoinositide 3-kinase alpha (PI3Kα) isoform, demonstrating a potent IC50 value of 0.14 nM. This compound effectively reduces mitochondrial membrane potential, leading to cell cycle arrest in the G1 phase and initiating apoptosis in U87-MG glioma cells. PI3Kα-IN-14 exhibits significant anti-proliferative effects across a range of tumor-derived cell lines, including PC-3 (IC50 of 0.28 μM), HCT-116 (IC50 of 0.57 μM), and U87-MG (IC50 of 1.37 μM), making it a valuable tool in cancer research and therapeutic studies targeting PI3K signaling pathways. -
PI3K Inhibitor
TYM-3-98 is a selective inhibitor of PI3Kδ, demonstrating an IC50 of 7.1 nM. This compound effectively inhibits the proliferation of B-lymphoma cells and disrupts the PI3K/AKT/mTOR signaling pathway, leading to the induction of apoptosis. Additionally, TYM-3-98 shows favorable pharmacokinetic properties and exhibits antitumor efficacy in mouse and rat models, while exhibiting minimal toxicity. -
PI3K/VEGFR2 Inhibitor
PI3K/VEGFR2-IN-1 is a highly effective dual inhibitor of PI3K and VEGFR2, exhibiting IC50 values of 2.21 μM and 68 μM, respectively. This compound has been shown to induce apoptosis in various cancer cell lines. It is suitable for research applications focused on cancer biology and therapy development targeting the PI3K/VEGFR2 signaling pathways. -
PI3K Inhibitor
PIK-C98 is a potent and selective inhibitor of phosphoinositide 3-kinases (PI3K), exhibiting IC50 values of 0.59, 1.64, 3.65, and 0.74 μM for the α, β, δ, and γ isoforms, respectively. This compound effectively inhibits all class I PI3Ks while leaving AKT and mTOR activity unaffected. PIK-C98 operates by disrupting the ATP-binding sites of PI3Ks, forming hydrogen bonds and arene-H interactions with target amino acid residues. Its capacity to induce apoptosis via PI3K inhibition makes PIK-C98 a valuable tool for research into multiple myeloma and other related conditions. -
PI3K Inhibitor
Ramentaceone (7-Methyljuglon) is a naphthoquinone that selectively inhibits phosphoinositide 3-kinase (PI3K) activity. This compound effectively reduces PI3K protein expression and decreases Akt protein phosphorylation in breast cancer cells, thereby inducing apoptosis. Ramentaceone's mechanism of action makes it a valuable tool for research in cancer biology and therapeutic development targeting the PI3K/Akt signaling pathway. -
PI3K/EGFR Inhibitor
MTX-216 is a dual ATP-competitive inhibitor targeting PI3K and EGFR. It effectively cosuppresses Ki-67 and phosphorylation of ribosomal S6, leading to apoptosis in NF1LOF cells. Additionally, MTX-216 inhibits SYK kinase activity with an IC50 of 281 nM. This compound is primarily utilized in research related to melanoma. -
PI3K Inhibitor
PI3K-IN-34 is a selective inhibitor of phosphoinositide 3-kinases (PI3Ks), specifically demonstrating IC50 values of 11.73 μM for PI3K-α, 6.09 μM for PI3K-β, and 11.18 μM for PI3K-δ. This compound effectively induces G2/M cell cycle arrest and promotes apoptotic pathways in targeted cells. PI3K-IN-34 is particularly useful in preclinical studies involving leukemia, providing insights into therapeutic strategies for this malignancy. -
PI3Kδ/γ Inhibitor
PI3Kδ/γ-IN-3 is a potent dual inhibitor of PI3Kδ and PI3Kγ, with IC50 values of 1 nM and 16 nM, respectively. This compound effectively induces apoptosis in tumor cells, making it a valuable tool for research in B-cell malignancies. Its oral bioavailability further enhances its utility in preclinical studies aimed at understanding and targeting these pathways in cancer therapy. -
PI3Kα Inhibitor
PI3Kα-IN-7 is a potent inhibitor of the PI3Kα isoform, with additional inhibitory effects on PI3Kβ. This compound is known to reduce mitochondrial membrane potential in cancer cells, leading to the induction of apoptosis. It is valuable for research applications focused on cancer biology and therapeutic development targeting the PI3K signaling pathway. -
PI3K Inhibitor
PI3K-IN-35 is a selective inhibitor of phosphoinositide 3-kinases (PI3Ks) with IC50 values of 13.98, 7.22, and 10.94 μM for PI3K-α, PI3K-β, and PI3K-δ, respectively. This compound effectively induces cell cycle arrest at the G2/M phase and promotes apoptosis, making it a valuable tool for studies in leukemia research. Investigators can utilize PI3K-IN-35 to explore the role of PI3K signaling in cancer progression and therapeutic responses. -
PI3K/HDAC Inhibitor
Fimepinostat mesylate is a potent dual inhibitor targeting class I phosphoinositide 3-kinases (PI3Ks) and histone deacetylases (HDACs). It exhibits IC50 values of 19 nM for PI3Kα, 54 nM for PI3Kβ, 39 nM for PI3Kδ, and 1.7 nM for HDAC1, 5.0 nM for HDAC2, 1.8 nM for HDAC3, and 2.8 nM for HDAC10. This compound is valuable for research applications focusing on cancer biology, epigenetic regulation, and cellular signaling pathways. -
PI3Kδ Inhibitor
WNY1613 is a potent and selective inhibitor of phosphoinositide 3-kinase delta (PI3Kδ) featuring a piperazinone-containing purine scaffold. This compound effectively induces apoptosis in cancer cells and inhibits the phosphorylation of downstream components of the PI3K signaling pathway in non-Hodgkin lymphoma (NHL) cell lines. WNY1613 demonstrates significant anti-NHL activity both in vitro and in vivo, making it a valuable tool for cancer research and therapeutic investigations. -
PI3Kα Inhibitor
XJTU-L453 is a selective inhibitor of PI3Kα, exhibiting an IC50 of 0.4 nM. It effectively suppresses the proliferation of breast cancer cell lines, T47D and MCF7, with IC50 values of 0.2 μM and 0.5 μM, respectively. By inhibiting the PI3K pathway, XJTU-L453 induces cell cycle arrest and promotes apoptosis, demonstrating significant antitumor activity in MCF7 xenograft models. This compound is valuable for research in cancer biology and therapeutic development targeting the PI3K signaling pathway. -
PI3K-α Inhibitor
PI3Kα-IN-27 is a potent inhibitor of the PI3K-α enzyme, exhibiting an IC50 value of 40 nM. This compound effectively targets and inhibits key signaling proteins, including PAK3, p110α, phospho-mTOR, and phospho-ERK1/2, leading to the induction of early apoptosis. Its significant anticancer activity has been demonstrated in various cancer models, including pancreatic, lung, and breast cancers, making it a valuable tool for research in cancer biology and targeted therapies. -
PI3Kδ/CSF1R Inhibitor
JMC14 is a selective PI3Kδ and CSF1R inhibitor, exhibiting IC50 values of 12 nM and 143 nM, respectively. This compound preferentially disrupts PI3Kδ-mediated signaling within cells, demonstrating significant antitumor activity against B-cell lymphomas and triple-negative breast cancer (TNBC) in both in vitro and in vivo models. JMC14 is an important tool for research into antitumor immunity and the mechanisms of cancer progression. -
MAO-B inhibitor
Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C. -
PI3K/mTOR inhibitor
Desmethyl-VS-5584 is a demethyl analogue of VS-5584, which is a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. -
mTOR/PI3K Inhibitor,
GSK2126458 is a highly potent, orally bioavailable inhibitor of PI3Kα and mTOR with in vivo activity in both pharmacodynamic and tumor growth efficacy models. -
PI3Kα inhibitor
Alpelisib hydrochloride (BYL-719 hydrochloride) is a potent, orally active, and selective PI3Kα inhibitor with IC50s of 5 nM, 250 nM, 290 nM and 1200 nM for p110α, p110γ, p110δ, and p110β, respectively. -
multi-kinase inhibitor
Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle. -
multi-kinase inhibitor
Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle. -
PI3Kδ inhibitor
Umbralisib R-enantiomer (TGR-1202 R-enantiomer) is a PI3Kδ inhibitor, which is the less active enantiomer of TGR-1202.
