PI3Kβ
PI3Kβ is a class I PI3K catalytic isoform that produces PIP3, linking receptor inputs to signaling networks that regulate cell growth, survival, and movement[1]. Mechanistically, PI3Kβ uniquely supports synergistic PIP3 formation when GPCR and RTK pathways are coactivated in myeloid cells, whereas p110α, p110β, and p110δ show partial redundancy downstream of M-CSF alone and p110γ acts nonredundantly downstream of C5a alone[1]. In PTEN-deficient breast tumour models, PI3Kβ inactivation reduced STAT3 signaling, increased immune-stimulatory molecules, and promoted anti-tumour immune responses[2]. Compared with related PI3K isoforms, this evidence positions PI3Kβ as a context-specific integrator of coincident receptor signaling and a disease-relevant driver in PTEN-null tumours[1][2]. For experimental applications, the PI3Kβ-selective inhibitor KIN-193 blocked AKT signaling and tumour growth dependent on p110β activation or PTEN loss, while pharmacological PI3Kβ inhibition also synergized with immunotherapy in PTEN-null breast tumour models[3][2].
References:
- [1]. Houslay DM, et al. Coincident signals from GPCRs and receptor tyrosine kinases are uniquely transduced by PI3Kβ in myeloid cells. Sci Signal. 2016 Aug 16;9(441):ra82. [Content Brief]
- [2]. Bergholz JS, et al. PI3Kβ controls immune evasion in PTEN-deficient breast tumours. Nature. 2023 May;617(7959):139-146. [Content Brief]
- [3]. Ni J, et al. Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent. Cancer Discov. 2012 May;2(5):425-33. [Content Brief]
All Product Categories
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PI3Kβ Related Products (162)
Related Products (162)
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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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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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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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TGX-155
0 ImagesCat. No.: HY-105666CAS No.: 351071-90-4Synonyms: AZ12649385TGX-155 (AZ12649385) is a selective inhibitor of PI3Kβ. TGX-155 has potential applications in antithrombotic therapy.
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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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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.
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MEK/PI3K-IN-2
0 ImagesCat. No.: HY-144693CAS No.: 2281803-33-4
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PP487
0 ImagesCat. No.: HY-15268CAS No.: 1092787-12-6
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LCI40
0 ImagesCat. No.: HY-183770LCI40 is an orally active dual PI3K/BRD4 inhibitor (PI3Kα IC50 = 0.071 μM, PI3Kβ IC50 = 0.17 μM, PI3Kγ IC50 = 0.66 μM, PI3Kδ IC50 = 0.072 μM, BRD4 BD1 IC50 = 0.19 μM, and BRD4 BD2 IC50 = 1.88 μM. LCI40 inhibits phosphorylation of pAKT (S473) and suppresses c-MYC levels in mantle cell lymphoma cells. LCI40 displays immunomodulatory capacity with minimal toxicity to normal mouse immune cells. LCI40 can be used for the research of mantle cell lymphoma.
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PI3K-IN-35
0 ImagesCat. No.: HY-147900CAS No.: 2458163-99-8
