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
-
PI3Kβ Related Products (162)
Related Products (162)
-
Serabelisib
0 ImagesSynonyms: MLN1117; INK1117; TAK-117Serabelisib (MLN1117) is a selective p110α inhibitor with an IC50 of 15 nM.
-
AZD 6482
0 ImagesSynonyms: KIN-193AZD 6482 (KIN-193) is a potent and selective p110β inhibitor with an IC50 of 0.69 nM.
-
BAY1082439
0 ImagesBAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth.
-
Roginolisib
0 ImagesSynonyms: MSC2360844; IOA-244
-
Pictilisib dimethanesulfonate
0 ImagesSynonyms: GDC-0941 dimethanesulfonate ; GDC-0941 (2 MeSO3H salt)Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
-
AMG 511
0 ImagesAMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model.
-
PI3Kγ inhibitor AZ2
0 ImagesPI3Kγ inhibitor AZ2 is a highly selective PI3Kγ inhibitor (The pIC50 value for PI3Kγ is 9.3). PI3Kγ inhibitor AZ2 can be used for the research of inflammatory and immune diseases.
