PI3K

Phosphoinositide 3-kinase

PI3K

PI3K Isoform Specific Products:

PI3K Isoform Comparison

PI3K Related Products (525)
Antibodies (15)
PI3K Signaling Pathway
PI3K Isoform Comparison

By Effects:	Inhibitors (449) Ligand (1) Agonist (1) Activators (36) Modulators (15) Inducer (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-10114

TGX-221	Inhibitor	99.74%
TGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, used for cancer treatment.

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-124760

hSMG-1 inhibitor 11e	Inhibitor	99.81%
hSMG-1 inhibitor 11e is a potent and selective hSMG-1 kinase inhibitor with an IC₅₀ of <0.05 nM. hSMG-1 inhibitor 11e shows >900-fold selectivity over mTOR (IC₅₀ of 45 nM), PI3Kα/γ (IC₅₀s of 61 nM and 92 nM) and CDK1/CDK2 (IC₅₀s of 32 μM and 7.1 μM).

HY-12513

Samotolisib	Inhibitor	99.27%
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-P1925A

GO-203 TFA	Inhibitor	99.28%
GO-203 TFA is a potent MUC1-C oncoprotein inhibitor. GO-203 TFA is an all D-amino acid peptide that consists of a poly-R transduction domain linked to a CQCRRKN motif that binds to the MUC1-C cytoplasmic tail and blocks MUC1-C homodimerization. GO-203 TFA downregulates TIGAR (TP53-induced glycolysis and apoptosis regulator) protein synthesis by inhibiting the PI3K-AKT-S6K1 pathway. GO-203 TFA induces the production of ROS and loss of mitochondrial transmembrane potential. GO-203 TFA inhibits the growth of colon cancer cells in vitro and as xenografts in nude mice.

HY-12330

AZD8186	Inhibitor	99.97%
AZD8186 is a PI3K inhibitor, which potently inhibits PI3Kβ (IC₅₀=4 nM) and PI3Kδ (IC50₅₀=12 nM) with selectivity over PI3Kα (IC₅₀=35 nM) and PI3Kγ (IC₅₀=675 nM).

HY-19962

Paxalisib	Inhibitor	99.63%
Paxalisib (GDC-0084) is a brain penetrant inhibitor of PI3K and mTOR, with K_is of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively.

HY-13532

AS-252424	Inhibitor	99.71%
AS-252424 is a potent and selective PI3Kγ inhibitor with an IC₅₀ of 30±10 nM.

HY-12046

PIK-93	Inhibitor	99.81%
PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC₅₀ of 19 nM, and also inhibits PI3Kγ and PI3Kα with IC₅₀ of 16 nM and 39 nM, respectively.

HY-12794

Vps34-PIK-III	Inhibitor	99.63%
Vps34-PIK-III is an orally active and selective VPS34 inhibitor (IC₅₀=18 nM). Vps34-PIK-III effectively inhibits autophagy and can be used as a molecular tool. vps34-PIK-III is also a PI3K inhibitor that inhibits the expression of genes in liver cancer stem cells (CSCs).

HY-10111

TG100-115	Inhibitor	99.41%
TG100-115 is a selective PI3Kγ/PI3Kδ inhibitor with IC₅₀s of 83 and 235 nM, respectively.

HY-100198

PI4KIIIbeta-IN-10	Inhibitor	99.84%
PI4KIIIbeta-IN-10 is a potent PI4KIIIβ inhibitor with an IC₅₀ of 3.6 nM.

HY-12461

WS6	Activator	99.94%
WS6 is an IkB kinase and EBP1 inhibitor, with IC₅₀ values of 0.24 nM, 0.21 nM, and 40.48 nM in MV4-11, MOLM13, and K562 cells, respectively. WS6 promotes the proliferation of alpha and beta cells in the pancreas, has antioxidant and anti-inflammatory activities, and can alleviate depression like behavior in rats^[1][2][4].

HY-13246

Apitolisib	Inhibitor	99.29%
Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC₅₀s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a K_i of 17 nM for mTOR.

HY-102031

Linperlisib	Inhibitor	99.51%
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-12037

Rigosertib sodium	Inhibitor	99.57%
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. Rigosertib sodium is a selective and non-ATP-competitive inhibitor of PLK1 with an IC₅₀ of 9 nM.

HY-17635

Leniolisib	Inhibitor	99.28%
Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor. Leniolisib has the potential for immunodeficiency disorders treatment.

HY-16596

CNX-1351	Inhibitor	99.88%
CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC₅₀ of 6.8 nM.

HY-15174

Dactolisib Tosylate	Inhibitor	99.87%
Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC₅₀ values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.

HY-15900

Voxtalisib	Inhibitor	99.18%
Voxtalisib (XL765) is a potent PI3K inhibitor, which has a similar activity toward class I PI3K (IC₅₀s=39, 113, 9 and 43 nM for p110α, p110β, p110γ and p110δ, respectively), also inhibits DNA-PK (IC₅₀=150 nM) and mTOR (IC₅₀=157 nM). Voxtalisib (XL765) inhibits mTORC1 and mTORC2 with IC₅₀s of 160 and 910 nM, respectively.

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 (525)

Antibodies (15)

PI3K Signaling Pathway

PI3K Isoform Comparison

PI3K Related Products (525):