PI3Kδ
PI3Kδ is a class I PI3K isoform that generates PIP3, a second messenger used by cell-surface receptors to control immune-cell movement, growth, survival, and differentiation[1]. Mechanistically, PI3Kδ acts in adaptive immunity, and both loss-of-function and gain-of-function defects in this pathway cause primary immunodeficiency, showing that PI3Kδ activity requires precise dynamic regulation[2]. In B-lineage models, p110δ and p110α are essential for pre-B-cell receptor signaling and B-cell development, while p110α, but not p110β, can compensate for p110δ loss during early bone-marrow B-cell development[3]. Compared with related isoforms, PI3Kα and PI3Kβ are relatively ubiquitous, whereas PI3Kδ is mostly confined to myeloid and lymphoid lineages, making high PI3Kδ expression a characteristic of immune cells[1]. In disease and experimental applications, idelalisib is an orally active selective PI3Kδ inhibitor with antitumor activity in previously treated indolent non-Hodgkin lymphoma and relapsed chronic lymphocytic leukemia[4][5]. Therefore, PI3Kδ supports research designs focused on immune signaling, B-cell receptor biology, primary immunodeficiency, inflammatory models, and selective PI3Kδ inhibitor pharmacology[1][2][3][4][5].
References:
- [1]. Vervloessem T, et al. The type 2 inositol 1,4,5-trisphosphate receptor, emerging functions for an intriguing Ca²⁺-release channel. Biochim Biophys Acta. 2015 Sep;1853(9):1992-2005. [Content Brief]
- [2]. Lucas CL, et al. PI3Kδ and primary immunodeficiencies. Nat Rev Immunol. 2016 Nov;16(11):702-714. [Content Brief]
- [3]. Ramadani F, et al. The PI3K isoforms p110alpha and p110delta are essential for pre-B cell receptor signaling and B cell development. Sci Signal. 2010 Aug 10;3(134):ra60. [Content Brief]
- [4]. Gopal AK, et al. PI3Kδ inhibition by idelalisib in patients with relapsed indolent lymphoma. N Engl J Med. 2014 Mar 13;370(11):1008-18. [Content Brief]
- [5]. Furman RR, et al. Idelalisib and rituximab in relapsed chronic lymphocytic leukemia. N Engl J Med. 2014 Mar 13;370(11):997-1007. [Content Brief]
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PI3Kδ Related Products (200)
Related Products (200)
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LY294002
0 ImagesLY294002 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.
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Alpelisib
0 ImagesSynonyms: BYL-719Alpelisib (BYL-719) is an orally active PI3Kα-selective inhibitor that blocks the conversion of PIP2 to PIP3, thereby inhibiting pathways including PI3K/AKT/mTOR, MAPK/ERK, Notch and JAK-STAT. Alpelisib also induces apoptosis, G0/G1 phase arrest and senescence; it significantly inhibits the proliferation, self-renewal, stemness and epithelial-mesenchymal transition (EMT) of tumor cells, reduces cancer stem cell populations and decreases the expression of stem cell markers. Alpelisib not only enhances the sensitivity to Eribulin (HY-13442) and exerts a synergistic effect with Paclitaxel (HY-B0015), but may also induce drug resistance by upregulating the SGK3/GSK3β/β-catenin signaling pathway. Alpelisib can be applied to research related to breast cancer, gastric cancer and lipomas associated with PTEN hamartoma tumor syndrome.
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Pictilisib
0 ImagesSynonyms: GDC-0941Pictilisib (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).
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Idelalisib
0 ImagesSynonyms: CAL-101; GS-1101
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PIK-124
0 ImagesCat. No.: HY-118903CAS No.: 711025-68-2
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AM-8508
0 ImagesCat. No.: HY-120116CAS No.: 1338483-67-2AM-8508 is an orally bioactive PI3Kδ inhibitor with an IC50 of 0.016 μM. AM-8508 selectively inhibits PI3Kδ, thereby blocking AKT phosphorylation mediated by the B cell receptor. AM-8508 suppresses the formation of antigen-specific IgG and IgM in rats immunized with keyhole limpet hemocyanin. AM-8508 can be used for the research of inflammatory diseases.
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T133
0 ImagesCat. No.: HY-181650CAS No.: 3101627-06-6T133 is an orally active ATP-competitive mTOR inhibitor with an IC50 of 0.34 nM and a Ki of 0.17 nM. T133 suppresses phosphorylation of AKT, S6K1, and 4EBP1. T133 inhibits cancer cell proliferation and migration, induces apoptosis, cell cycle arrest, and autophagy. T133 exhibits dose-dependent antitumor efficacy in xenograft mouse models. T133 can be used for the research of cancer, such as gastric cancer and lung cancer.
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Dactolisib
0 ImagesSynonyms: BEZ235; NVP-BEZ235
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Gedatolisib
0 ImagesSynonyms: PKI-587; PF-05212384
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Copanlisib
0 ImagesSynonyms: BAY 80-6946Copanlisib (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.
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Duvelisib
0 ImagesSynonyms: IPI-145; INK1197Duvelisib (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.
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Copanlisib dihydrochloride
0 ImagesSynonyms: BAY 80-6946 dihydrochlorideCopanlisib dihydrochloride (BAY 80-6946 dihydrochloride) 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 dihydrochloride has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib dihydrochloride has superior antitumor activity.
