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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AM-1430
0 ImagesCat. No.: HY-115814CAS No.: 1975263-74-1AM-1430 is an efficient, highly selective and orally active small molecule inhibitor of PI3Kδ with an IC50 of 4.6 nM. AM-1430 exhibits IC50s for PI3Kα, PI3Kβ and PI3Kγ of 14.18, 2.2 and 3.22 μM, respectively. AM-1430 inhibits B cell proliferation and exhibits excellent in vivo activity in pAKT inhibition models and the hemoglobin (KLH) immune response model. AM-1430 can be used for the study of inflammation and autoimmune diseases.
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PI3K-IN-33
0 ImagesCat. No.: HY-147898CAS No.: 2458163-92-1
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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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PROTAC PI3Kα/δ degrader-1
0 ImagesCat. No.: HY-182083PROTAC PI3Kα/δ degrader-1 is an orally active PI3Kα/δ PROTAC degrader, with an IC50 of 0.34 nM for PI3Kα and 1.85 nM for PI3Kδ. PROTAC PI3Kα/δ degrader-1 inhibits the proliferation and migration of cancer cells, induces G1-phase cell cycle arrest and PI3Kα degradation. PROTAC PI3Kα/δ degrader-1 suppresses tumor growth in breast cancer xenograft mouse models. PROTAC PI3Kα/δ degrader-1 can be used for the research of breast cancer.
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DHW-221
0 ImagesCat. No.: HY-130133CAS No.: 2378831-21-9DHW-221 is a potent orally active dual PI3K/mTOR inhibitor, exhibiting low nanomolar potency against all four Class I PI3K isoforms and mTOR (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM; mTOR, IC50 = 3.9 nM). DHW-221 exerts antitumor effects by blocking the PI3K/Akt/mTOR pathway and inducing mitochondrial apoptosis and paraptosis (via Endoplasmic Reticulum (ER) stress and MAPK signaling) and arrests cell cycle, thereby inhibiting cell migration, invasion and angiogenesis. DHW-221 inhibits tumor growth in both the A549/Taxol (HY-B0015) and the HCC827 xenograft mouse models. DHW-221 can be used for non-small cell lung cancer (NSCLC), colon and breast cancer research.
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PI3Kδ-IN-28
0 ImagesCat. No.: HY-184125PI3Kδ-IN-28 is an orally active and selective PI3Kδ inhibitor with an IC50 of 6.1 nM. PI3Kδ-IN-28 inhibits pro-inflammatory M1 macrophage polarization, promotes anti-inflammatory M2 phenotype, and alleviates pulmonary edema and inflammatory infiltration. PI3Kδ-IN-28 is applicable to research related to acute lung injury.
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PI3Kδ-IN-11
0 ImagesCat. No.: HY-143472CAS No.: 2413257-51-7PI3Kδ-IN-11 is a highly potent and selective PI3Kδ inhibitor with IC50 value of 27.5 nM. PI3Kδ-IN-11 dose-dependently blocks the activity of PI3K/Akt pathway. PI3Kδ-IN-11 can be used for researching B or T cell-related malignancies.
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PI3Kδ/BET-IN-1
0 ImagesCat. No.: HY-172130CAS No.: 3054869-10-9PI3Kδ/BET-IN-1 (compound 10b) shows excellent and balanced activities against PI3Kδ (IC50 = 112 nM) and BRD4-BD1 (IC50 = 19 nM) and exhibits strong antiproliferative activities in DLBCL cells.
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LNP23
0 ImagesCat. No.: HY-189462CAS No.: 3136664-01-9LNP23 is a selective PI3Kα inhibitor with an IC50 of 5.15 nM. LNP23 inhibits PI3K/AKT signaling and induces apoptosis and G1 phase arrest in MCF-7 cells. LNP23 also inhibits cancer cell proliferation, colony formation, and migration. LNP23 can be used for breast cancer and lung adenocarcinoma research.
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NVP-CLR457
0 ImagesCat. No.: HY-146260CAS No.: 1453082-52-4NVP-CLR457 (compound 40) is an orally active, potent and balanced pan-class I PI3K inhibitor. NVP-CLR457 shows a clear dose-dependent PK/PD/efficacy relationship. NVP-CLR457 has antitumor activity.
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PI3K-IN-34
0 ImagesCat. No.: HY-147899CAS No.: 2458163-94-3
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PI3K/HDAC-IN-2
0 ImagesCat. No.: HY-146159CAS No.: 2361418-65-5PI3K/HDAC-IN-2 is a potent dual PI3K/HDAC inhibitor with IC50s of 226 nM, 279 nM, 467 nM, 29 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively, and IC50s of 1.3 nM, 3.4 nM, 972 nM, 17 nM, 12 nM for HDAC1, HDAC2, HDC4, HDAC6, HDAC8, respectively. PI3K/HDAC-IN-2 exhibits PI3Kδ and class I and IIb HDAC selectivity. PI3K/HDAC-IN-2 has remarkable anticancer effects.
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Pabgraminone C
0 ImagesCat. No.: HY-184119CAS No.: 3061276-55-6Synonyms: IM502Pabgraminone C (IM502) is a Fungal metabolite and PI3Kγ inhibitor with an IC50 of 61.7 nM against PI3Kγ. Pabgraminone C shifts the STAT signaling pathway in cells from an immunosuppressive STAT3/STAT6-dominant profile to an immunostimulatory STAT1/STAT2-dominant profile, driving cells toward a pro-inflammatory phenotype. Pabgraminone C reprograms cells from an immunosuppressive state to an immunostimulatory state, reversing their suppressive effect on anti-tumor immunity. Pabgraminone C inhibits established tumor growth and metastasis across multiple cancer types. Pabgraminone C overcomes resistance to PD-1 checkpoint blockade strategies. Pabgraminone C can be used in research related to liver cancer, melanoma, and colorectal cancer.
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PI3Kα-IN-29
0 ImagesCat. No.: HY-179623PI3Kα-IN-29 is a potent, orally active and selective PI3Kα with an IC50 of 2.5 nM. PI3Kα-IN-29 exhibits >400-fold selectivity over PI3Kβ/δ/γ/mTOR. PI3Kα-IN-29 selectively degrades the H1047R mutant p110α protein and inhibits PI3Kα kinase activity. PI3Kα-IN-29 suppresses PI3K/AKT/mTOR signaling, induces G1 arrest, and inhibits migration. PI3Kα-IN-29 inhibits tumor growth in a T47 mouse model. PI3Kα-IN-29 can be used for the research of breast cancer.
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PIK-39
0 ImagesCat. No.: HY-116882CAS No.: 371242-53-4PIK-39 is a selective PI3Kδ inhibitor with an IC50 of 0.30 μM. PIK-39 has a propeller-like structure that induces conformational changes in the ATP-binding region of its target. PIK-39 is applicable to the research of autoimmune diseases.
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(R)-IHMT-PI3Kδ-372
0 Images(R)-IHMT-PI3Kδ-372 (R-18) is a potent and selective PI3Kδ inhibitor with an IC50 of 19 nM. (R)-IHMT-PI3Kδ-372 (R-18) can be used in chronic obstructive pulmonary disease (COPD) research.
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PI3K/mTOR-IN-20
0 ImagesCat. No.: HY-180556PI3K/mTOR-IN-20 is a selective dual PI3K/mTOR inhibitor. PI3K/mTOR-IN-20 demonstrates nanomolar antiproliferative effects with IC50s of 0.380 and 0.090 μM for MRC-5 and Mlg2908 cells. PI3K/mTOR-IN-20 reduces Ashcroft scores, hydroxyproline content, collagen deposition, and downregulates fibrosis-related proteins, while restoring lung architecture in a Bleomycin-induced pulmonary fibrosis model. PI3K/mTOR-IN-20 shows a favorable safety profile with steady weight recovery and no distinct liver or kidney toxicity. PI3K/mTOR-IN-20 can be used for fetal lung fibroblasts research.
