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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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