PI3K
| 货号 | 产品名 | CAS号 | 信息 |
|---|---|---|---|
| FB11376 | 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. |
| FB02823 | Vps34-IN-1 | 1383716-33-3 | 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. |
| FB07161 | 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 17.9 μM for 9 cancer cell lines. |
| FB10132 | TGR-1202 R-Enantiomer | 1532533-69-9 | TGR-1202 R-enantiomer is the R-enantiomer of TGR-1202. TGR-1202 is a potent PI3Kδ inhibitor. |
| FB03282 | TGR-1202 HCl | 1532533-78-0 | TGR-1202 HCl is an orally available, next generation PI3Kdelta inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 and 24.3 nM respectively. |
| FB05547 | Tenalisib | 1639417-53-0 | Tenalisib is a potent and selective dual PI3Kδ/γ inhibitor with IC50 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. |
| FB12699 | TC KHNS 11 | 1431540-99-6 | TC KHNS 11 is a potent and selective PI 3-kinase δ inhibitor that is orally bioavailable. |
| FB18842 | 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. |
| FB00960 | 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. |
| FB15371 | 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]. |
| FB11018 | SN32976 | 1246202-11-8 | SN32976 is a selective inhibitor of PI3K and mTOR with preferential activity to PI3Kα, in comparison to established pan PI3K inhibitors. |
| FB12128 | SF2523 | 1174428-47-7 | SF2523 blocks BRD4 binding to MYCN promoter PS1/PS2. |
| FB10863 | 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 Sjogren's syndrome. |
| FB11321 | S14161 | 883046-50-2 | S14161 is a small molecule inhibitor of cyclins D1-D3 expression that inhibits phosphoinositide 3-kinase activity and arrests cells at the G0/G1 phase in a dose-dependent manner (concentrations tested from 5-10 μM). |
| FB15274 | PWT33597 mesylate | 1246203-36-0 | PWT33597 is a dual inhibitor of PI3K alpha and mTOR with selectivity for PI3K alpha (IC50 = 26 nM) over PI3K delta (IC50 = 291 nM) but also displaying activity against mTOR in biochemical assays (IC50 = 21 nM). It had good pharmacokinetic properties in multiple preclinical species. |
| FB11823 | PQR530 | 1927857-61-1 | PQR530 is a potent, oral and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, exhibiting antitumor activity. |
| FB10193 | PIK-III | 1383716-40-2 | PIK-III, which is a selective inhibitor of VPS34 enzymatic activity, inhibits autophagy and de novo lipidation of LC3 and leads to the stabilization of autophagy substrates. |
| FB17693 | 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. |
| FB09917 | PIK-293 | 900185-01-5 | PIK-293 is a PI3K inhibitor, mostly for PI3Kδ with IC50 of 0.24 μM, 500-, 100- and 50-fold less potent to PI3Kα/β/γ, respectively. |
| FB11185 | PI3Kδ Inhibitor C52 | 1911564-39-0 | PI3Kδ inhibitor C52 is a potent, selective, and efficacious PI3Kδ 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 PK/PD assays and highly efficacious in a mouse collagen-induced arthritis model. |
| FB02745 | PI3Kdelta Inhibitor 1 | 1332075-63-4 | PI3Kdelta inhibitor 1 is a potent and selective inhibitor of isoform of PI3Kδ and useful for treating disorders mediated by lipid kinases such as inflammation, immunol disorders, and cancer. |
| FB15660 | 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. |
| FB12067 | Parsaclisib | 1426698-88-5 | Parsaclisib is a potent and selective PI3Kδ inhibitor, with an IC50 of 1 nM at 1 mM ATP, and shows appr 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases. |
| FB03169 | 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 α/δ isoforms with IC50 of 14/20 nM. |
| FB07166 | NVP-QAV-572 | 957209-68-6 | NVP-QAV-572 is a potent PI3K kianse inhibitor with IC50 of 10 nM. |
| FB15651 | ME-401 | 1595129-71-7 | ME-401 is a potent and selective P110δ inhibitor. |
| FB11660 | LX2343 | 333745-53-2 | LX2343 is a BACE1 enzyme inhibitor with an IC50 value of 11.43±0.36 μM. LX2343 acts as a non-ATP competitive PI3K inhibitor with an IC50 of 15.99±3.23 μM. LX2343 stimulates autophagy in its promotion of Aβ clearance. |
| FB12448 | LTURM 36 | 1879887-94-1 | LTURM 36 is a PI 3-kinase δ inhibitor with IC50 of 0.64 μM. |
| FB10885 | Leniolisib | 1354690-24-6 | Leniolisib is a potent and selective PI3Kδ inhibitor currently in used for the treatment of immunodeficiency disorders. |
| FB09913 | IPI-549 | 1693758-51-8 | IPI-549 is a selective phosphoinositide-3-kinase (PI3K)-γ inhibitor with IC50 of 16 nM as an immuno-oncology clinical candidate. |
| FB00871 | IPI-3063 | 1425043-73-7 | IPI-3063 is a potent and selective PI3K p110δ inhibitor with an IC50 of 2.5 ± 1.2 nM. |
| FB12029 | IP3K Inhibitor | 519178-28-0 | IP3K Inhibitor is a IP3K inhibitor with an IC50 of 10.2 μM. |
| FB04757 | 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. |
| FB10208 | GSK2292767 | 1254036-66-2 | GSK2292767 is a potent and selective PI3Kδ inhibitor. |
| FB01403 | 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. |
| FB03152 | GNE-317 | 1394076-92-6 | GNE-317 is a potent PI3K/mTOR inhibitor that can cross the blood–brain barrier and shows potent suppression of the PI3K pathway in the brain of mice with intact BBB. |
| FB07164 | GDC-0941 Dimethanesulfonate | 957054-33-0 | GDC-0941 dimethanesulfonate is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold). |
| FB09878 | GDC-0326 | 1282514-88-8 | GDC-0326 is a potent and selective inhibitor of α-Isoform of Phosphoinositide 3-Kinase (PI3Kalpha inhibitor). GDC-0326 achieves a very high level of selectivity over other kinases. |
| FB02821 | GDC-0084 | 1382979-44-3 | GDC-0084 is a brain penetrant inhibitor of PI3K and mTOR. |
| FB12306 | ETP 45658 | 1198357-79-7 | ETP 45658 is a PI 3-kinase inhibitor with IC50s of 22, 30, 129 and 710 nM for PI 3-Kα, PI 3-Kδ, PI 3-Kβ and PI 3-Kγ respectively,and also inhibits DNA-PK and mTOR with IC50s of 70.6 and 152 nM respectively. |
| FB10129 | CAY10505 | 1218777-13-9 | CAY10505 is dehydroxyl of AS-252424, which is a PI3Kγ inhibitor with IC50 of 33 nM. |
| FB06149 | CAL-130 Racemate | 474012-90-3 | CAL-130 racemate is a phosphoinositide 3-kinase (PI3K) inhibitor. It is reported that combined inhibition of PI3Kγ/δ as therapy for T cell acute lymphoblastic leukemia (T-ALL). |
| FB03208 | CAL-130 | 1431697-74-3 | CAL-130 is a phosphoinositide 3-kinase (PI3K) inhibitor. It is reported that combined inhibition of PI3Kγ/δ as therapy for T cell acute lymphoblastic leukemia (T-ALL). |
| FB03209 | CAL-130 HCl | 1431697-78-7 | CAL-130 HCl is a phosphoinositide 3-kinase (PI3K) inhibitor. It is reported that combined inhibition of PI3Kγ/δ as therapy for T cell acute lymphoblastic leukemia (T-ALL). |
| FB17548 | 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. |
| FB10158 | AS-604850 | 648449-76-7 | AS-604850 is a selective, ATP-competitive PI3Kγ inhibitor with IC50 of 250 nM, showing over 80-fold selectivity for PI3Kγ than PI3Kδ/β, and being 18-fold selective for PI3Kγ than PI3Kα. |
| FB17653 | 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 . |
| FB06881 | Acalisib | 870281-34-8 | Acalisib is a potent and selective inhibitor of PI3Kδ with IC50 value of 12.7 nM. |
| FB10204 | 740 Y-P | 1236188-16-1 | 740 Y-P is cell-permeable peptide activator of PI3K. |
| FB09858 | 3-Methyladenine | 5142-23-4 | 3-Methyladenine is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM. |