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PI3K
| Cat. No. | Product Name | CAS No. | Information |
|---|---|---|---|
| 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. |
| CSN23147 | TC KHNS 11 | 1431540-99-6 | TC KHNS 11 is a potent and selective PI 3-kinase δ inhibitor that is orally bioavailable. |
| 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 |
| CSN23870 | PX 866 | 502632-66-8 | Sonolisib (PX-866), an improved Wortmannin analogue, is an oral, irreversible, and pan-isoform inhibitor of PI3K (IC50=0.1 nM (p110α), 1.0 nM (p120γ), 2.9 nM (p110δ)). Antitumor activity[1][2]. |
| CSN22559 | SF2523 | 1174428-47-7 | SF2523 blocks BRD4 binding to MYCN promoter PS1/PS2. |
| CSN19738 | Seletalisib | 1362850-20-1 | Seletalisib is a potent and selective PI3 kinase inhibitor, which may be useful for the treatment of immune-inflammatory diseases, such as psoriasis amd primary Sjogrens syndrome. |
| 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.. |
| CSN17243 | PQR309 | 1225037-39-7 | PQR309 is a potent brain-penetrant orally bioavailable pan-class I PI3KmTOR inhibitor with IC50s of 33 nM 451 nM 661 nM 708 nM and 89 nM for PI3K PI3K PI3K PI3K and mTOR respectively |
| CSN16214 | PKI-587 | 1197160-78-3 | PKI-587 is a highly potent dual PI3K/mTOR kinase inhibitor with IC50 of 0.4 nM, 5.4 nM and 1.6 nM for PI3Kα, PI3Kγ and mTOR, respectively. |
| 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. |
| CSN20258 | PI3Kδ Inhibitor C52 | 1911564-39-0 | PI3K inhibitor C52 is a potent, selective, and efficacious PI3K inhibitor with improved Caco-2 permeability, reduced Caco-2 efflux, reduced hERG PC activity, and increased selectivity profile while maintaining potency in the CD69 hWB assay, and is very potent in PKPD assays and highly efficacious in a mouse collagen-induced arthritis model. |
| CSN13877 | PI-3065 | 955977-50-1 | PI-3065 is a selective p110 inhibitor with IC50 of 15 nM, 70-fold selectivity over other PI3K family members. |
| CSN13906 | PI-103 HCl | 371935-79-4 | PI-103 HCl is a potent PI3K/Akt and mTOR inhibitor with IC50 values of 2 nM for recombinant PI3K isoform p110α and 30 nM for mTOR. |
| CSN17801 | ON 146040 | 1404231-34-0 | ON 146040 is the first dual PI3K and BCR-ABL inhibitor that targets the STAT3 and STAT5 pathways and inhibits PI3K isoforms with IC50 of 1420 nM |
| CSN13693 | NVP-BKM120 HCl | 1312445-63-8 | NVP-BKM120 HclBKM120 is a selective PI3K inhibitor of p110 with IC50 of 52 nM166 nM116 nM262 nM respectively Reduced potency against VPS34 mTOR DNAPK with little activity to PI4K |
| 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. |
| CSN12216 | Wortmannin | 19545-26-7 | KY 12420 is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. It also blocks autophagosome formation and potently inhibits DNA-PKATM with IC50 of 16 nM and 150 nM in cell-free assays. |
| 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. |
| CSN17123 | GNE-477 | 1032754-81-6 | GNE-477 is a potent and efficacious dual PI3KmTOR inhibitor with IC50 of 4 nM for PI3K Ki of 21 nM for mTOR |
| CSN17784 | GNE-317 | 1394076-92-6 | GNE-317 is a potent PI3KmTOR inhibitor that can cross the bloodbrain barrier and shows potent suppression of the PI3K pathway in the brain of mice with intact BBB |
| 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. |
| CSN24837 | Erucic acid | 112-86-7 | Erucic acid is a monounsaturated omega-9 fatty acid used as mineral oil and a precursor to biodiesel fuel. |
| CSN13707 | Duvelisib | 1201438-56-3 | Duvelisib is a selective PI3K inhibitor with Ki and IC50 of 23 pM243 pM and 1 nM50 nM, highly selective for PI3K than other protein kinases. |
| CSN15881 | CZC-24832 | 1159824-67-5 | CZC-24832 is the first selective PI3K inhibitor with IC50 of 27 nM, with 10-fold selectivity over PI3K and 100-fold selectivity over PI3K and 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. |
| CSN13168 | BKM-120 | 944396-07-0 | BKM120 is a selective PI3K inhibitor of p110 with IC50 of 52 nM166 nM116 nM262 nM in cell-free assays respectively |
| 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) . |
| CSN13098 | AS-605240 | 648450-29-7 | AS-605240 selectively inhibits PI3K with IC50 of 8 nM over 30-fold and 75-fold selective for PI3K than PI3K and PI3K in cell-free assays respectively |
| CSN19171 | AS-604850 | 648449-76-7 | AS-604850 is a selective, ATP-competitive PI3K inhibitor with IC50 of 250 nM, showing over 80-fold selectivity for PI3K than PI3K, and being 18-fold selective for PI3K than PI3K. |
| CSN13709 | Alpelisib | 1217486-61-7 | Alpelisib is a potent and selective PI3Kα inhibitor with IC50 of 5 nM, liitle or no effect on PI3Kβ/γ/δ. |
| 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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