PI3K

Phosphoinositide 3-kinase

PI3K

PI3K Isoform Specific Products:

PI3K Isoform Comparison

PI3K Related Products (1024)
Antibodies (16)
PI3K Signaling Pathway
PI3K Isoform Comparison

By Effects:	Inhibitors (796) Agonists (8) Degraders (5) Controls (4) Substrate (1) Ligands (8) Antagonist (1) Activators (114) Modulators (22) Inducers (3)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-106591A

4-Vinylcyclohexene dioxide	Activator	98.57%
4-Vinylcyclohexene dioxide (4-Vinylcyclohexene diepoxide) is an orally active metabolite of 4-vinylcyclohexene. 4-Vinylcyclohexene dioxide induces Apoptosis, increases intracellular ROS, and activates the PI3K/Akt/mTOR pathway. 4-Vinylcyclohexene dioxide selectively damages small ovarian follicles, inhibits granulosa cell function, and disrupts the male reproductive system. 4-Vinylcyclohexene dioxide can be used in the study of premature ovarian insufficiency, reproductive toxicity, and related fertility disorders.

HY-N2515

Ginsenoside Rk1	Inhibitor	99.90%
Ginsenoside Rk1 is a unique component created by processing the ginseng plant (mainly Sung Ginseng, SG) at high temperatures. Ginsenoside Rk1 has anti-inflammatory effect, suppresses the activation of Jak2/Stat3 signaling pathway and NF-κB. Ginsenoside Rk1 has anti-tumor effect, antiplatelet aggregation activities, anti-insulin resistance, nephroprotective effect, antimicrobial effect, cognitive function enhancement, lipid accumulation reduction and prevents osteoporosis. Ginsenoside Rk1 induces cell apoptosis by triggering intracellular reactive oxygen species (ROS) generation and blocking PI3K/Akt pathway.

HY-15245

GSK2636771	Inhibitor	99.88%
GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with a K_i of 0.89 nM and an IC₅₀ of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.

HY-12037A

Rigosertib	Inhibitor	99.01%
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. Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC₅₀ of 9 nM.

HY-N0031

Plantamajoside	Inhibitor	99.80%
Plantamajoside is an orally active phenylpropanoid glycoside. Plantamajoside can be isolated from Plantago asiatica L.(Plantaginaceae). Plantamajoside inactivates NF-κB, PI3K/akt, induces Apoptosis, and improves Autophagy. Plantamajoside regulates MAPK, integrin-linked kinase/c-Src. Plantamajoside inhibits multiple cancers, improves lung and kidney damage. Plantamajoside has neuroprotective and anti-inflammatory effects.

HY-157122

VJDT	Inhibitor	99.68%
VJDT is a TREM1 inhibitor that can effectively block TREM1 signaling. VJDT inhibits tumor cell proliferation and migration and induces cell cycle arrest. VJDT has immunomodulatory and antitumor activities, and can be used for the research of tumors such as melanoma.

HY-14860

1-Deoxynojirimycin	Activator	99.94%
1-Deoxynojirimycin (Duvoglustat) is a potent and orally active α-glucosidase inhibitor. 1-Deoxynojirimycin suppresses postprandial blood glucose and is widely used for diabetes mellitus. 1-Deoxynojirimycin possesses antihyperglycemic, anti-obesity, and antiviral features.

HY-13532

AS-252424	Inhibitor	99.66%
AS-252424 is a potent and selective PI3Kγ inhibitor with an IC₅₀ of 30±10 nM.

HY-N0284

Esculetin	Inhibitor	99.79%
Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities.

HY-102031

Linperlisib	Inhibitor	98.83%
Linperlisib (YY-20394) is a potent, orally bioavailable and selective inhibitor of PI3Kδ extracted from patent WO 2015055071 A1, compound 10; has an IC₅₀ of 6.4 nM.

HY-101920

Autophinib	Inhibitor	99.95%
Autophinib is a potent, selective autophagy inhibitor with IC₅₀s of 90 nM and 40 nM for starvation- and Rapamycin-induced autophagy, respectively. Autophinib is also an ATP competitive Vacuolar Protein Sorting 34 (VPS34) inhibitor with an IC₅₀ of 19 nM. Autophinib inhibits autophagy induced by starvation or Rapamycin by targeting VPS34.

HY-P1410C

D-GsMTx4 TFA	Inhibitor	99.89%
D-GsMTx4 TFA is a spider peptide and the D enantiomer of GsMTx4 (HY-P1410). D-GsMTx4 TFA inhibits the mechanosensitive ion channel Piezo2. D-GsMTx4 TFA inhibits [Ca²⁺]_i elevation. D-GsMTx4 TFA inhibits mTOR and PI3K-Akt signaling pathways. D-GsMTx4 TFA inhibits mechanical allodynia and thermal hyperalgesia. D-GsMTx4 TFA can be used in researches of mechanical stress, chronic pain and idiopathic pulmonary fibrosis.

HY-N9481

Lipoteichoic acid
Lipoteichoic acid is an orally effect anti-inflammatory and antitumor agent. Lipoteichoic acid is a crucial immune molecule in Gram-positive bacteria that activates the complement system by inducing C3 and inhibiting CD55. Lipoteichoic acid regulates macrophage autophagy through the PI3K/Akt/mTOR pathway. Lipoteichoic acid induces lung damage in mice. Lipoteichoic acid inhibits the production of melanin.

HY-159852

BBO-10203	Ligand	99.12%
BBO-10203 is a potent inhibitor of PI3Kα and KRAS^G12C, selectively and covalently binding to Cys242 in the RAS-Binding Domain of PI3Kα, and inhibiting both the GTP-bound and GDP-bound states of KRAS^G12C with an IC₅₀ of 0.031 nM and an EC₅₀ of 0.02 nM. BBO-10203 disrupts the interaction between RAS isoforms and PI3Kα, leading to the inhibition of RAS-mediated PI3Kα activation, and reduces pERK expression, cell growth, and induces G₁ arrest and apoptosis. BBO-10203 can be used for the research of breast cancer, colorectal cancer, and non-small cell lung cancer.

HY-N0330

Momordin Ic	Modulator	99.78%
Momordin Ic is an orally active triterpenoid saponin that can be isolated from Kochia scoparia. It is also a SUMO specific protease 1 (SENP1) inhibitor, SENP1/c-MYC signaling pathway inhibitor, and apoptosis inducer. Momordin Ic induces autophagy and apoptosis in liver cancer cells through the PI3K/Akt and MAPK signaling pathways mediated by reactive oxygen species. Momordin Ic has the ability to control glucose induced blood glucose elevation, inhibit gastric emptying, resist rheumatoid arthritis, reduce CCl₄ (HY-Y0298) induced hepatotoxicity and anti-tumor activity.

HY-12513

Samotolisib	Inhibitor	98.85%
Samotolisib (LY3023414) potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC₅₀s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. Samotolisib potently inhibits mTORC1/2 at low nanomolar concentrations.

HY-15177

PF-04691502	Inhibitor	99.33%
PF-04691502 is a potent and selective inhibitor of PI3K and mTOR. PF-04691502 binds to human PI3Kα, β, δ, γ and mTOR with K_is of 1.8, 2.1, 1.6, 1.9 and 16 nM, respectively.

HY-15449

Kaempferide	Activator	99.80%
Kaempferide is an orally active flavonol isolated from Hippophae rhamnoides L. Kaempferide has anticancer, anti-inflammatory, antioxidant, antidiabetic, antiobesity, antihypertensive, and neuroprotective activities. Kaempferide induces apoptosis. Kaempferide promotes osteogenesis through antioxidants and can be used in osteoporosis research.

HY-N0716A

Berberine hemisulfate	Activator	99.63%
Berberine hemisulfate is the hemisulfate form of Berberine (HY-N0716). Berberine hemisulfate is an alkaloid isolated from the Chinese herbal medicine Huanglian. Berberine hemisulfate exhibits anti-inflammatory, antibiobic, antitumor, cardiovascular protective and neuroprotective activity.

HY-10114

TGX-221	Inhibitor	99.59%
TGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, used for cancer treatment.

Growth factor RTK SHC SOS GRB2 RAS p85 p110α/δ PTEN SHIP1 or
SHIP2 INPP4B p110β p85 RAC1 or CDC Chemokine GPCR p101 p110γ PDK-1 Akt AS160 eNOS p21 RAS-GTP Insulin/GF Insulin/ IGF receptor GRB10 S6K IRS1 PI3K PTEN ZAP70 TCR CD3 RAF MEK ERK MNK eIF4E RSK MYC AMPK BAD FOXOs GSK-3 BCL-X_L BCL-2 BIM p27 FAS ligand Cyclin D BAX TSC2 TSC1 TBC1D7 RHEB Ribosome mLST8 mTOR SIN1 RICTOR TSC2 TSC1 TBC1D7 RAC1 GSK-3β Axin APC Wnt TLR MYD88 RAC1 PI3K INPP4B SHIP1 or
SHIP2 PTEN 4E-BP ULK1 S6K GRB10 mLST8 mTOR RAPTOR mTORC1 p85 p110δ PI3Kδ DAG PKC CARMA1 MALT1 BCL-10 IKKα IKKβ NEMO IκB p50 p65 NF-κB p85α p110δ PI3Kδ CD81 BCAP LYN BLK SYK BLNK BTK PLCγ2 GADs VAV SLP76 ITK PLCγ1 JAK3 ICOS IL-2 IL-2R BCR CD19 mTORC2

Download PI3K Signaling Pathway Map.

Phosphatidylinositol 3 kinases (PI3Ks) are a family of lipid kinases that integrate signals from growth factors, cytokines and other environmental cues, translating them into intracellular signals that regulate multiple signaling pathways. These pathways control many physiological functions and cellular processes, which include cell proliferation, growth, survival, motility and metabolism^[1].

In the absence of activating signals, p85 interacts with p110 and inhibits p110 kinase activity. Following receptor tyrosine kinase (RTK) or G protein-coupled receptor (GPCR) activation, class I PI3Ks are recruited to the plasma membrane, where p85 inhibition of p110 is relieved and p110 phosphorylates PIP2 to generate PIP3. The activated insulin receptor recruits intracellular adaptor protein IRS1. Phosphorylation of IRS proteins on tyrosine residues by the insulin receptor initiates the recruitment and activation of PI3K. PIP3 acts as a second messenger which promotes the phosphorylation of Akt at Thr308 by PDK-1. RTK activation can also trigger Ras-Raf-MEK-ERK pathway. Activated Akt, ERK and RSK phosphorylate TSC2 at multiple sites to inhibit TSC1-TSC2-TBC1D7, which is the TSC complex that acts as a GTPase-activating protein (GAP) for the small GTPase RHEB. During inhibition of the TSC complex, GTP-loaded RHEB binds the mTOR catalytic domain to activate mTORC1. Glycogen synthase kinase 3β (GSK-3β) activates the TSC complex by phosphorylating TSC2 at Ser1379 and Ser1383. Phosphorylation of these two residues requires priming by AMPK-dependent phosphorylation of Ser1387. Wnt signaling inhibits GSK-3β and the TSC complex, and thus activates mTORC1. mTORC2 is activated by Wnt in a manner dependent on the small GTPase RAC1. Akt activation contributes to diverse cellular activities which include cell survival, growth, proliferation, angiogenesis, metabolism, and migration. Important downstream targets of Akt are GSK-3, FOXOs, BAD, AS160, eNOS, and mTOR. mTORC1 negatively regulates autophagy through multiple inputs, including inhibitory phosphorylation of ULK1, and promotes protein synthesis through activation of the translation initiation promoter S6K and through inhibition of the inhibitory mRNA cap binding 4E-BP1^[1][2][3].

PI3Kδ is a heterodimeric enzyme, typically composed of a p85α regulatory subunit and a p110δ catalytic subunit. In T cells, the TCR, the costimulatory receptor ICOS and the IL-2R can activate PI3Kδ. In B cells, PI3Kδ is activated upon crosslinking of the B cell receptor (BCR). The BCR co-opts the co-receptor CD19 or the adaptor B cell associated protein (BCAP), both of which have YXXM motifs to which the p85α SH2 domains can bind. In lumphocytes, BTK and ITK contribute to the activation of PLCγ and promotes the generation of DAG and the influx of Ca²⁺, which in turn activate PKC and the CARMA1-, BCL 10- and MALT1 containing (CBM) complex. The resulting NF-κB inhibitor kinase (IKK) activation leads to the phosphorylation and the degradation of IκB, and to the nuclear accumulation of the p50-p65 NF-κB heterodimer. MyD88 is an adapter protein that mediates signal transduction for most TLRs and leads to activation of PI3K^[4].

Reference:

[1]. Thorpe LM, et al. PI3K in cancer: divergent roles of isoforms, modes of activation and therapeutic targeting.Nat Rev Cancer. 2015 Jan;15(1):7-24.
[2]. Vanhaesebroeck B, et al. PI3K signalling: the path to discovery and understanding.Nat Rev Mol Cell Biol. 2012 Feb 23;13(3):195-203.
[3]. Fruman DA, et al. The PI3K Pathway in Human Disease.Cell. 2017 Aug 10;170(4):605-635.
[4]. Lucas CL, et al. PI3Kδ and primary immunodeficiencies.Nat Rev Immunol. 2016 Nov;16(11):702-714.

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PI3K

PI3K

PI3K Isoform Specific Products:

PI3K Isoform Specific Products:

PI3K Related Products (1024)

Antibodies (16)

PI3K Signaling Pathway

PI3K Isoform Comparison

PI3K Related Products (1024):