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 (202)
Related Products (202)
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IHMT-PI3Kδ-372
0 ImagesIHMT-PI3Kδ-372 is a potent and selective PI3Kδ inhibitor with an IC50 of 14 nM. IHMT-PI3Kδ-372 shows high selectivity over other class I PI3Ks (56～83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (COPD) research.
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CHMFL-PI4K-127
0 ImagesCHMFL-PI4K-127 (compound 15g) is an orally active, potent and high selective PfPI4K (Plasmodium falciparum PI4K kinase) inhibitor, with an IC50 of 0.9 nM. CHMFL-PI4K-127 exhibits potent activity against 3D7 Plasmodium falciparum, with an EC50 of 25.1 nM. CHMFL-PI4K-127 shows antimalaria efficacy.
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PI3Kδ-IN-16
0 ImagesPI3Kδ-IN-16 is a potent and selective PI3Kδ inhibitor with an IC50 value of 0.9 nM. PI3Kδ-IN-16 has a strong anti-proliferative effect on SU-DHL-6 cells, causing cell cycle arrest and inducing apoptosis. PI3Kδ-IN-16 tightly bins to PI3Kδ protein with a planar-shaped conformation. The kinase activity of PI3Kδ-IN-16 which is ~378-fold over PI3Kα, 412-fold over PI3Kβ, and 10-fold over PI3Kγ. PI3Kδ-IN-16 can be used for the study of hematologic malignancies.
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Umbralisib tosylate
0 ImagesCat. No.: HY-12279ACAS No.: 1532533-72-4Synonyms: TGR-1202 tosylate; RP5264 tosylateUmbralisib (TGR-1202) tosylate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib tosylate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib tosylate can be used for haematological malignancies reseach.
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Umbralisib sulfate
0 ImagesCat. No.: HY-12279BCAS No.: 1532533-75-7Synonyms: TGR-1202 sulfate; RP-5264 sulfateUmbralisib (TGR-1202) sulfate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib sulfate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib sulfate can be used for haematological malignancies reseach.
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LAS191954
0 ImagesCat. No.: HY-101114CAS No.: 1403947-26-1LAS191954 is a potent, selective and orally active PI3Kδ inhibitor for inflammatory diseases treatment, with an IC50 of 2.6 nM.
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PI3K/HDAC-IN-1
0 ImagesCat. No.: HY-128582CAS No.: 2361418-52-0
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CHF-6523
0 ImagesCat. No.: HY-162878CAS No.: 2500579-21-3CHF-6523 is an orally active PI3Kδ inhibitor that can be used in research related to chronic obstructive pulmonary disease (COPD).
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PI3K-IN-6
0 ImagesCat. No.: HY-101115CAS No.: 1842380-77-1PI3K-IN-6 (compound 20a) is an oral active and highly selective phosphoinositide 3-kinase (PI3K) β/δ inhibitor, with IC50 values of 7.8 nM/5.3 nM for PI3K β/δ, respectively. PI3K-IN-6 (compound 20a) has potential top treat phosphatase and tensin homolog (PTEN) feficient tumors.
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PI3Kdelta inhibitor 1
0 ImagesCat. No.: HY-112439CAS No.: 2242109-74-4PI3Kdelta inhibitor 1 (Compound 5d) is a potent, selective and orally available PI3Kδ inhibitor with an IC50 of 1.3 nM.
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PI3K-IN-9
0 ImagesCat. No.: HY-133029CAS No.: 2360875-63-2PI3K-IN-9 (compound 1-14) is a potent and selective PI3Kδ inhibitor with an IC50 of 8.9 nM.
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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.
