PI3K

Phosphoinositide 3-kinase

PI3K

PI3K Isoform Specific Products:

PI3K Related Products (311)
PI3K Signaling Pathway
PI3K Isoform Comparison

By Effects:	Inhibitors (284) Agonist (1) Activators (12) Modulators (5)

Cat. No.	Product Name	Effect	Purity

HY-19312

3-Methyladenine	Inhibitor	99.83%
3-Methyladenine (3-MA) is a PI3K inhibitor. 3-Methyladenine is a widely used inhibitor of autophagy via its inhibitory effect on class III PI3K.

HY-10108

LY294002	Inhibitor	99.92%
LY294002 is a broad-spectrum inhibitor of PI3K with IC₅₀s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC₅₀ of 98 nM. LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC₅₀ of 1.4 μM. LY294002 is an apoptosis activator.

HY-15244

Alpelisib	Inhibitor	99.86%
Alpelisib (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. Alpelisib (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. Alpelisib (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC₅₀s of 5/250/290/1200 nM, respectively. Antineoplastic activity.

HY-18085

Quercetin	Inhibitor	98.02%
Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC₅₀ of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.

HY-10197

Wortmannin	Inhibitor	99.85%
Wortmannin (SL-2052; KY-12420) is a potent, selective and irreversible PI3K inhibitor with an IC₅₀ of 3 nM. Wortmannin also blocks autophagy formation, and potently inhibits Polo-like kinase 1 (PlK1) and Plk3 with IC₅₀s of 5.8 and 48 nM, respectively.

HY-N2045

Musk ketone	Activator	99.21%
Musk ketone (MK) is a widely used artificial fragrance. Musk ketone shows mutagenic and comutagenic effects in Hep G2 cells and induces neural stem cell proliferation and differentiation in cerebral ischemia via activation of the PI3K/Akt signaling pathway. In the brain, musk ketone is neuroprotective against stroke injury through inhibition of cell apoptosis.

HY-150019

PI3K-IN-36	Inhibitor
PI3K-IN-36 (compound A36) is a potent PI3K inhibitor. PI3K-IN-36 can be used in research of follicular lymphoma (FL).

HY-128333

PI3K/mTOR Inhibitor-4	Inhibitor
PI3K/mTOR Inhibitor-4 is an orally active pan-class I PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-4 has enzymatic inhibition activity for PI3Kα, PI3Kγ, PI3Kδ and mTOR with IC₅₀ values of 0.63 nM, 22 nM, 9.2 nM and 13.85 nM, respectively. PI3K/mTOR Inhibitor-4 can be used for the research of cancer.

HY-P0175

740 Y-P	Activator	98.85%
740 Y-P (740YPDGFR; PDGFR 740Y-P) is a potent and cell-permeable PI3K activator. 740 Y-P readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone.

HY-111783

AZD-7648	Inhibitor	99.89%
AZD-7648 is a potent, orally active, selective DNA-PK inhibitor with an IC₅₀ of 0.6 nM. AZD-7648 induces apoptosis and shows antitumor activity.

HY-70063

Buparlisib	Inhibitor	99.90%
Buparlisib (BKM120; NVP-BKM120) is a pan-class I PI3K inhibitor, with IC₅₀s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.

HY-101562

Inavolisib	Inhibitor	98.94%
GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC₅₀=0.038 nM). GDC-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. GDC-0077 (RG6114) is more selective for mutant versus wild-type PI3Kα.

HY-13026

Idelalisib	Inhibitor	99.78%
Idelalisib (CAL-101; GS-1101) is a highly selective and orally bioavailable p110δ inhibitor with an IC₅₀ of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.

HY-50673

Dactolisib	Inhibitor	99.94%
Dactolisib (BEZ235) is an orally active and dual pan-class I PI3K and mTOR kinase inhibitor with IC₅₀s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively. Dactolisib (BEZ235) inhibits both mTORC1 and mTORC2.

HY-15346

Copanlisib	Inhibitor	99.50%
Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC₅₀s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity.

HY-100716

Eganelisib	Inhibitor	99.69%
Eganelisib (IPI549) is a potent and selective PI3Kγ inhibitor with an IC₅₀ of 16 nM. Eganelisib shows >100-fold selectivity over other lipid and protein kinases.

HY-50094

Pictilisib	Inhibitor	99.80%
Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with an IC₅₀ of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

HY-12481

SAR405	Inhibitor	98.99%
SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC₅₀=1.2 nM; K_d=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity.

HY-17044

Duvelisib	Inhibitor	99.89%
Duvelisib (IPI-145) is a selectivite p100δ inhibitor with IC₅₀ of 2.5 nM, 27.4 nM, 85 nM and 1602 nM for p110δ, P110γ, p110β and p110α, respectively.

HY-13898

Taselisib	Inhibitor	99.86%
Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with K_is of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, 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 (311)

PI3K Signaling Pathway

PI3K Isoform Comparison

PI3K Related Products (311):