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PI3K Phosphoinositide 3-kinases

Cat.No.  Name Information
M2050 GSK2636771 GSK2636771 is a potent, orally available and specific PI3K p110β (PI3K beta, PI3Kβ) inhibitor.
M1925 LY294002 LY294002 is a highly selective PI3K inhibitor with IC50 values of 0.31, 0.73, 1.06 and 6.60 μM for PI3Kβ, PI3Kα, PI3Kδ and PI3Kγ respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM.
M2296 3-Methyladenine (3-MA) 3-Methyladenine (3-MA) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM, respectively.
M1715 GDC-0941 (Pictilisib) GDC-0941 is a selective and potent inhibitor of Class I PI3K, p110a IC50=0.003uM, U87MG IC50=0.95μM.
M1984 PF-04691502 PF-04691502 is a potent and selective, ATP-competitive PI3K/mTOR inhibitor with IC50 of 7.5 nM and 3.8 nM of AKT T308 and AKT S473, respectively.
M2053 Wortmannin (KY 12420) Wortmannin (KY 12420) is a specific, covalent inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase) with IC50 of 3 nM.
M1680 BKM120 (Buparlisib) BKM120 (NVP-BKM120) is a potent and highly specific oral pan-class I PI3K inhibitor.
M1819 A66 A66 is a potent and specific inhibitor of PI3K p110α with IC50 values of 32, 30 and 43 nM for p110α, p110α/E545K and p110α/H1047R.
M1671 BEZ235 BEZ235 (NVP-BEZ235) is a potent dual PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively.
M1773 PI-103 PI-103 is a potent, ATP-competitive PI3K,cell-permeable,inhibitor.The IC50 values are 2, 8, 20, 26, 48, 83, 88, 150 nM for DNA-PK, p110α, mTORC1, PI3-KC2β, p110δ, mTORC2, p110β, and p110γrespectively.
M7555 SAR405 SAR405 is a PIK3C3/Vps34 inhibitor with an IC50 of 1.2 nM. SAR405 also is a proximal inhibitor of the autophagy machinery.
M7538 Tenalisib Tenalisib (RP6530) is a potent and selective dual PI3Kδ/γ inhibitor with IC50 values of 24.5 nM and 33.2 nM for PI3Kδ and PI3Kγ, respectively. Its selectivity over α and β isoforms are more than 300-fold and 100-fold, respectively.
M7139 PI 828 PI 828 is a pI 3-kinase inhibitor, more potent than LY 294002.
M6307 IPI3063 IPI-3063 is a potent and selective p110δ inhibitor with biochemical IC50 of 2.5 ± 1.2 nM and IC50 values for the other class I PI3K isoforms (p110α, p110β, p110γ) are at least 400-fold higher.
M6304 GDC-0084 GDC-0084 is a brain penetrant inhibitor of PI3K and mTOR.
M6225 GNE-317 GNE-317 is a potent, brain-penetrant PI3K inhibitor.
M6175 Serabelisib Serabelisib (INK-1117,MLN-1117,TAK-117) is a potent and selective oral PI3Kα isoform inhibitor (IC50 of 21 nmol/L against PI3Kα) that has demonstrated > 100-fold selectivity relative to other class I PI3K family members (PI3Kβ/γ/δ) and mTOR, and a high degree of selectivity against many other kinase.
M6152 SF2523 SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
M5344 VPS34-IN1 Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks.
M5343 Voxtalisib Analogue Voxtalisib (SAR245409, XL765) Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.
M5337 PI-3065 PI-3065 is a novel potent and selective PI3K p110δ inhibitor with IC50 of 15 nM; exhibits > 100 fold selectivity against p110α, p110β, p110γ, DNA-PK and mTOR
M5335 PF-4989216 PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively.
M5314 AZD-8835 AZD8835 ia a novel mixed inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 nM and 5.7 nM, respectively, also with selectivity against PI3Kβ (IC50=431 nM) and PI3Kγ (IC50=90 nM).
M5268 TGR-1202 (Umbralisib) Umbralisib is the first inhibitor of phosphoinositol 3 kinase (PI3K) δ and casein kinase 1 (CK1) ε.
M5255 GDC-0326 GDC-0326 is Inhibitor of the class I phosphoinositide 3-kinase (PI3K) isoform PI3Kα which has received substantial attention for their potential use in cancer therapy.
M5231 GSK2269557 Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor(pKi = 9.9).
M4692 aurantio-obtusin Aurantio-obtusin is an anthraquinone compound isolated from cassia seeds, which has anti-inflammatory, antioxidant, anticoagulant and antihypertensive effects.
M4184 Cynarin 1, 3-dicaffeoylquinic acid is a derivative of caffeyl quinic acid, which has antioxidant activity and free radical scavenging activity.
M4117 Hederacolchiside-A1 Hederacolchiside A1, isolated from Pulsatilla pulsatilla, induces apoptosis by regulating the PI3K/Akt/mTOR signaling pathway, thereby inhibiting the proliferation of tumor cells. Hederacolchiside A1 has anti-schistosomiasis activity and affects parasite viability in vivo and in vitro.
M3880 Acalisib Acalisib (GS-9820) is an inhibitor of the beta and delta isoforms of the 110 kDa catalytic subunit of class IA phosphoinositide-3 kinases (PI3K) with potential immunomodulating and antineoplastic activities.




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