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PI3K

PI3K

Cat. No. Product Name CAS No. Information
CSN32908 Zandelisib 1401436-95-0 Zandelisib is a potent and selective inhibitor of phosphatidylinositol 3-kinase (PI3K) with IC50 of 3.5 nM for p110δ.
CSN15908 XL765 Analogue 1349796-36-6 XL765 analogue is a dual inhibitor of mTORPI3K, mostly for p110 with IC50 of 9 nM, and also inhibits DNA-PK and mTOR.
CSN16985 XL147   934526-89-3 XL147 is a potent, orally bioavailable inhibitor of the class I PI3K family of lipid kinases with IC50 values of 39 nM383 nM36 nM23 nM for PI3K, respectively and less potent to PI3K.
CSN12670 XL147 Analogue 956958-53-5 XL147 analogue is a selective and reversible class I PI3K inhibitor for PI3K with IC50 of 39 nM36 nM23 nM in cell-free assays, less potent to PI3K.
CSN21430 VPS34 inhibitor 1   1383716-46-8 Vps34-IN1 is a potent inhibitor of the class III phosphoinositide 3-kinase (PI3K) vacuolar protein sorting 34 (Vsp34) with IC50 of 15 nM.
CSN16944 Voxtalisib 934493-76-2 Voxtalisib is a potent and highly selective inhibitor of class I PI3Ks with IC50 of 39110943 nM for PI3K, also inhibits mTOR with IC50 of 160-910 nM.
CSN18633 UNBS5162 956590-23-1 UNBS5162 is a naphthalimide and a hydrolysis product of UNBS3157 that decreases CXCL chemokine expression in experimental prostate cancers and the mean antiproliferative activity IC50 value is 179 M for 9 cancer cell lines
CSN23147 TC KHNS 11 1431540-99-6 TC KHNS 11 is a potent and selective PI 3-kinase δ inhibitor that is orally bioavailable.
CSN28425 SRX3207 2254693-15-5 SRX3207 is an orally active dual Syk/PI3K inhibitor with IC50 value of 30nM for Syk. It potently blocks phosphorylation of Syk at 348 site and Y525/526 site. SRX3207 reduced immunosuppressive macrophage polarization and increased infiltration and cytotoxicity of CD8+ T cells in LLC tumors and increased expression of Ifng and Gzmb in 3207 treated LLC tumors.
CSN17136 Sophocarpine Hydrate 145572-44-7 Sophocarpine, a natural product isolated and purified from the herb of Sophora alopecuroidos L., with anti-viral, anti-cachectic and anti-inflammatory effects, can alleviate liver fibrosis mainly by inhibiting the TLR4 pathway, it may be a potential chemotherapeutic agent for chronic liver diseases, ameliorate the ischemic injury induced by transient focal cerebral ischemia in rats and that this neuroprotective effect may be related to the anti-ASIC1 channel and anti-apoptotic action of sophocarpine, and also alleviate hepatocyte steatosis and the potential mechanism may be the activated signaling pathway of AMPK.
CSN16469 Sophocarpine   6483-15-4 Sophocarpine is a naturally-occuring HERG K channel blocker with IC50 ranging in 100-300 M found from plant Sophora flavescens
CSN22559 SF2523 1174428-47-7 SF2523 blocks BRD4 binding to MYCN promoter PS1/PS2.
CSN15741 RP-5264 1532533-67-7 RP-5264 is an orally available, next generation PI3Kdelta inhibitor, inhibits PI3K activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 and 24.3 nM respectively.
CSN13129 Quercetin Dihydrate   6151-25-3 Quercetin Dihydrate inhibits various proteins including tyrosine protein kinase, mitochondrial phospholipase A2 and phosphodiesterases. It is a flavonoid with anticancer activity via suppressing type II estrogen receptors and blocking cell cycle progression. Quercetin could be found in a wide variety of plant-based foods, such as apples, onions, berries, and red wine etc..
CSN27247 PIK-75   372196-67-3 PIK-75 is a selective p110α inhibitor with IC50 of 5.8 nM with 200-fold more potently than p110β, and also potently inhibits DNA-PK with IC50 of 2 nM.
CSN24179 PI3K/mTOR Inhibitor-2 1848242-58-9 PI3K/mTOR Inhibitor-2 is a dual pan-PI3K/mTOR inhibitor with IC50 values of 3.4/34/16/1nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ and 4.7 nM for mTOR, respectively.
CSN26739 PI3K-IN-2 1403458-28-5 PI3K-IN-2 (compound 10) is a potent and orally active PI3Kβ/δ (IC50=7.1/8.6 nM) inhibitor with excellent selectivity versus PI3Kσ and PI3Kγ (IC50=13/190 nM, respectively)[1].
CSN26213 PI-828 942289-87-4 PI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with IC50s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid kinase assay, respectively.
CSN26226 Mtx-211 1952236-05-3 MTX-211 is a dual inhibitor of EGFR and PI3K, used for the treatment of cancer and other diseases.
CSN17646 MLN1117 1268454-23-4 MLN1117 is a selective p110 inhibitor with IC50 of 15 nM.
CSN24176 ME-401 1595129-71-7 ME-401 is a potent and selective P110δ inhibitor.
CSN11346 LY294002   154447-36-6 LY294002 is the first synthetic molecule known to inhibit p110α, p110β and p110δ with IC50 of 0.5 μM, 0.57 μM, 0.97 μM.
CSN20673 Leniolisib 1354690-24-6 Leniolisib is a potent and selective PI3K inhibitor currently in used for the treatment of immunodeficiency disorders.
CSN26741 LAS191954 free base 1403947-26-1 LAS191954 is a Potent, Selective, and Orally Available PI3Kδ Inhibitor for the Treatment of Inflammatory Diseases. LAS191954 showed PI3Kdelta IC50 = 2.6 nM; M-CSF p-Akt IC50 = 7.8 nM; % Metabolism (R/H) = 20/16; PK i.v. t1/2 (R/D) = 3.1 h/10.2h. LAS191954 showed efficacy at significantly lower doses than Idelalisib. LAS191954 showed a potency on the target of 2.6 nM, with the highest selectivity versus PI3Kα (8.2 μM) and the lowest versus PI3Kγ and PI3Kβ (72 and 94 nM, respectively).
CSN21128 IPI-3063 1425043-73-7 IPI-3063 is a potent and selective PI3K p110 inhibitor with an IC50 of 2.51.2 nM.
CSN22904 IITZ-01   1807988-47-1 IITZ-01 is an inhibitor of lysosomotropic autophagy It can enhance autophagosome accumulation and inhibit autophagosomal degradation that finally resulting in the inhibition of autophagy
CSN14412 Hirsutenone 41137-87-5 Hirsutenone, a natural product isolated and purified from the eaves of Alnus nepalensis, exhibits anti-cancer effect against prostate cancer through a direct physical inhibition of Akt1/2, attenuates adipogenesis by directly targeting PI3K and ERK during MCE in 3T3-L1 preadipocytes, underscoring the potential therapeutic application of Hirsutenone in preventing obesity, and may exert a preventive effect against microbial endotoxin lipopolysaccharide-induced inflammatory skin diseases through inhibition of ERK pathway-mediated NF-kappaB activation. Hirsutenone showed potent PL(pro) inhibitory activity with IC50 value of 4.1µM.
CSN12474 GSK2126458 1086062-66-9 GSK2126458 is a highly selective and potent inhibitor of PI3K with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2 , respectively.
CSN17198 GSK2269557 1254036-71-9 GSK-2269557 has low oral bioavailability (F=2%) and in vivo clearance of 28 mL/min/kg but has a high volume of distribution of 6.3 L/kg.
CSN15869 GDC-0980 1032754-93-0 GDC-0980 is a potent, class I PI3K inhibitor for PI3K with IC50 of 5 nM27 nM7 nM14 nM in cell-free assays
CSN12429 GDC-0941 957054-30-7 GDC-0941 is a potent inhibitor of PI3K with IC50 of 3 nM, with modest selectivity against p110(11-fold) and p110(25-fold).
CSN16999 GDC-0032 1282512-48-4 GDC-0032 is a potent, next-generation isoform-sparing PI3K inhibitor targeting PI3K with IC50 of 0.29 nM0.12 nM0.97nM, 10 fold selective over PI3K.
CSN12930 CAL-101   870281-82-6 CAL-101 is a selective p110 inhibitor with IC50 of 2.5 nM, shown to have 40- to 300-fold greater selectivity for p110 than p110, and 400- to 4000-fold selectivity to p110 than C2, hVPS34, DNA-PK and mTOR.
CSN26528 BGT226 free base 915020-55-2 BGT226 is a phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. PI3K inhibitor BGT226 specifically inhibits PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway, which may trigger the translocation of cytosolic Bax to the mitochondrial outer membrane, increasing mitochondrial membrane permeability; apoptotic cell death may ensue. Bax is a member of the proapoptotic Bcl2 family of proteins.
CSN17405 BEZ235 Tosylate 1028385-32-1 BEZ235 tosylate is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3K, , , , respectively.
CSN12260 BEZ235   915019-65-7 BEZ235 is a dual ATP-competitive PI3K and mTOR inhibitor for p110 and mTOR(p70S6K) with IC50 of 4 nM 5 nM 7 nM 75 nM 6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell.
CSN17605 BEBT-908 1235449-52-1 BEBT-908 is a PI3K inhibitor with an IC50 0.1 M, and also inhibits HDAC (0.1 M IC50 1 M) .
CSN27186 BAY-1082439 1375469-38-7 BAY-1082439 is a highly selective PI3K 110α/β inhibitor. Upon binding to P-gp and BCRP, BAY-1082439 enhanced the ATPase activity of both P-gp and BCRP, implying the potential of BAY-1082439 to increase drug accumulation by blocking the efflux activity of both P-gp and BCRP.
CSN27232 amg511   1253573-53-3 AMG 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 .
CSN12350 Acacetin   480-44-4 Acacetin shows inhibiton of the proliferation and induction apoptosis for cancer cells. It is a flavonoid purified from the bark of acacia farnesiana with anti-peroxidant, antiarthritic, and anti-inflammatory activities,
CSN19389 3-Methyladenine   5142-23-4 3-Methyladenine is a selective PI3K inhibitor for Vps34 and PI3K with IC50 of 25 M and 60 M.
CSN13521 1,3-O-Dicaffeoylquinic Acid 19870-46-3 1,3-O-Dicaffeoylquinic acid is a natural product isolated and purified from the herbs of Cynara scolymus L., which may activates PI3KAkt.
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