Signaling Pathway

PI3K

PI3K

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PI3K (Phosphatidylinositol-4,5-bisphosphate 3-kinase) are a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. Many of these functions relate to the ability of class I PI 3-kinases to activate protein kinase B (PKB, aka Akt) as in the PI3K/AKT/mTOR pathway. The p110δ and p110γ isoforms regulate different aspects of immune responses. PI 3-kinases are also a key component of the insulin signaling pathway. PI3Ks are a family of related intracellularsignal transducer enzymes capable of phosphorylating the 3 position hydroxyl group of the inositol ring of phosphatidylinositol (PtdIns).

PI3K Inhibitors & Modulators (82)

Product Name Catalog No. Brief Description
3-Methyladenine

HY-19312

3-Methyladenine (3-MA) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM.

A66

HY-13261

A66 is a potent and specific p110α inhibitor with IC50 of 32 nM, >100 fold selectivity for p110α over other class-I PI3K isoforms.

Acalisib

HY-12644

Acalisib (GS-9820) is a potent and selective inhibitor of PI3Kδ with IC50 value of 12.7 nM.

AMG319

HY-12948

AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, also inhibits PI3Kγ with IC50 of 850 nM.

AS-252424

HY-13532

AS-252424 is a potent and selective inhibitor of PI3Kγ with IC50 of 33 nM; >10 fold selectivity for PI3Kγ versus PI3Kα.

AS-605240

HY-10109

AS-605240 is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) (IC50 = 8 nM).

AZD 6482

HY-10344

AZD6482 is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ.

AZD-8835

HY-12869

AZD8835 is a potent and selective inhibitor of PI3Kδ and PI3Kαwith IC50 of 5.7 nM and 6.2 nM, with selectivity against PI3Kβ (IC50 431 nM) and PI3Kγ (IC50 90 nM).

AZD8186

HY-12330

AZD8186 is an isoform-specific small-molecule PI3K inhibitor, potently inhibits PI3Kβ (IC50=4 nM) and PI3Kδ (IC50=12 nM) with selectivity over PI3Kα (IC50=35 nM) and PI3Kγ (IC50=675 nM).

BAY 80-6946

HY-15346

BAY 80-6946(Copanlisib) is a potent and highly selective reversible PI3K inhibitor for PI3Kα/β with IC50 of 0.469 nM/3.72 nM.

BEZ235

HY-50673

BEZ235 (NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM/5 nM/7 nM/75 nM/6 nM, respectively; inhibits ATR with IC50 of 21 nM; shown to be poor inhibitory to Akt and PDK1.

BEZ235 Tosylate

HY-15174

BEZ235 tosylate(NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM/5 nM/7 nM/75 nM/6 nM, respectively; inhibits ATR with IC50 of 21 nM; shown to be poor inhibitory to Akt and PDK1.

BYL-719

HY-15244

BYL719 is a potent and selective PI3Kα inhibitor with IC50 of 5 nM, liitle or no effect on PI3Kβ/γ/δ.

CAL-101

HY-13026

CAL-101 (Idelalisib, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR.

CAL-130

HY-16122A

CAL-130 is a novel phosphoinositide 3-kinase (PI3K) inhibitor.

CAL-130 Hydrochloride

HY-16122B

CAL-130 Hcl is a novel phosphoinositide 3-kinase (PI3K) inhibitor.

CAL-130 Racemate

HY-16122

CAL-130 racemate is a novel phosphoinositide 3-kinase (PI3K) inhibitor.

CAY10505

HY-13530

CAY10505 is a potent and selective PI3Kγ inhibitor with IC50 of 30 nM.

CH5132799

HY-15466

CH5132799 selectively inhibits class I PI3Ks, such as PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ with IC50 values of 0.014, 0.12, 0.50, and 0.36 uM, respectively; shows less inhibition of class II PI3Ks, class III PI3ks, and mTOR.

CNX-1351

HY-16596

CNX-1351 is a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα with IC50 of 6.8 nM; 20-400 times less potent against β, γ, and δ.