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PI3K
T0579 Myricetin Myricetin is a naturally-occurring flavonoid found in many grapes, berries, fruits, vegetables, herbs, as well as other plants. Walnuts are a rich dietary source. It has been shown that myricetin has antioxidant properties.
T1056 Isoprenaline hydrochloride Isoproterenol Hydrochloride is a synthetic catechol compound and potent beta-adrenergic agonist with the peripheral vasodilator, bronchodilator, and cardiac stimulating properties.
T1826 SAR245409 (XL765) Voxtalisib (SAR245409, XL765)Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ ,also inhibits DNA-PK and mTOR.
T1827 NVP-BKM120 Buparlisib is an orally bioavailable specific oral inhibitor of the pan-class I phosphatidylinositol 3-kinase (PI3K) family of lipid kinases with potential antineoplastic activity. Buparlisib has been used in trials studying the treatment and basic science of Lymphoma, Metastases, Lung Cancer, Solid
T1838 INK-0128 INK 128 is an orally bioavailable inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2) with potential antineoplastic activity.
T1859 AZD-8055 AZD8055 is an ATP-competitive mTOR inhibitor (IC50: 0.8 nM in MDA-MB-468 cells) with excellent selectivity ( about 1,000-fold) against ATM/DNA-PK and PI3K isoforms.
T1861 GSK2126458 GSK2126458 is a small-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic activity.
T1879 3-Methyladenine (3-MA) 3-Methyladenine (3-MA) is a selective Vps34 and PI3Kγ inhibitor (IC50: 25/60 μM in HeLa cells); blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also suppress the formation autophagosome.
T1894 CAL-101 CAL-101 (Idelalisib, GS-1101) is a small molecule inhibitor of the delta isoform of the 110 kDa catalytic subunit of class I phosphoinositide-3 kinase (PI3K) with IC50 of 2.5 nM. The selectivity for p110δ is 40- to 300-fold than p110α/β/γ, and 400- to 4000-fold than C2β, hVPS34, DNA-PK, and mTO
T1916 Apitolisib (GDC-0980, RG7422) Apitolisib, an effective, class I PI3K inhibitor for PI3Kα(IC50=5 nM), PI3Kβ(IC50=27 nM), PI3Kδ(IC50=7 nM), PI3Kγ (IC50=14 nM), is used in trials study of solid cancers, breast cancer, prostate cancer, renal cell carcinoma, and endometrial carcinoma, among others.
T1921 BYL-719(Alpelisib) Alpelisib is an orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity with IC50 of 5 nM in a cell-free assay, and minimal effect on PI3Kβ/γ/δ.
T1949 CZC24832 CZC24832 is a selective inhibitor of PI 3-kinase γ.
T1961 AZD2014 AZD2014 is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity.
T1970 PKI-587 Gedatolisib is a highly effective dual inhibitor targeting the PI3Kα/γ (IC50: 0.4/5.4 nM)and mTOR (IC50: 1.6 nM) in the PI3K/mTOR signaling pathway.
T1988 IPI-145 Duvelisib is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities.
T1994 GDC-0941 Pictilisib has been used in trials studying the treatment of Solid Cancers, Breast Cancer, Advanced Solid Tumours, Metastatic Breast Cancer, and Non-Hodgkin's Lymphoma, Solid Cancers, among others.
T1999 GDC-0032 Taselisib is an orally bioavailable inhibitor of the class I phosphatidylinositol 3-kinase (PI3K) alpha isoform (PIK3CA), with potential antineoplastic activity.
T2008 LY294002 LY294002 is a specific synthetic molecule known to inhibit PI3Kα/δ/β (IC50: 0.5/0.57/0.97 μM, in cell-free assays); also blocks autophagosome formation.
T2061 APY0201 APY0201 is a effective, highly specific, ATP-competitive PIKfyve inhibitor (IC50: 5.2 nM). It can interrupt the conversion of phosphatidylinositol 3-phosphate (PtdIns3P) to PtdIns(3,5)P2.
T2073 GSK-2636771 GSK2636771, an effective, specific, orally bioavailable, PI3Kβ inhibitor, has been used in cancer, lymphoma, solid neoplasm, recurrent solid neoplasm, and advanced malignant neoplasm.
T2083 PI-3065 PI-3065 is a novel potent and selective PI3K p110δ inhibitor.
T2084 ETP-46464 ETP-46464 is an effective and specific ATR inhibitor (IC50: 25 nM).
T2174 Quercetin Quercetin, a natural flavonoid present in vegetables, fruit, and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor.
T2235 BEZ235 Dactolisib is an orally bioavailable imidazoquinoline targeting the phosphatidylinositol 3 kinase (PI3K) and the mammalian target of rapamycin (mTOR), with potential antineoplastic activity.
T2248 AS-605240 AS-605240 is an effective and specific inhibitor of PI3Kγ (IC50/Ki: 87.8 nM).
T2256 CNX-1351 CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor.
T2287 PIK-75 Hydrochloride PIK-75, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110α(IC50=5.8 nM) and p110γ(IC50=76 nM).
T2297 PIK-294 PIK-294 is a excellently specific p110δ inhibitor(IC50=10 nM).
T2308 HS-173 HS-173 is an effective PI3Kα inhibitor (IC50: 0.8 nM).
T2357 GSK1059615 GSK1059615 has been used in trials studying the treatment of Lymphoma, Solid Tumours, Endometrial Cancer, Solid Tumor Cancer, and Metastatic Breast Cancer.
T2365 XL-147 Pilaralisib is an orally available small molecule that selectively inhibits the activity of phosphoinositide-3 kinase (PI3K). Pilaralisib has been used in trials studying the treatment of Cancer, Lymphoma, Solid Tumors, Glioblastoma, and Breast Cancer, among others.
T2377 XL147 analogue XL147 analogue is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ.
T2414 PP 242 PP 242 is a specific and ATP competitive mTOR inhibitor (IC50=8 nM).
T2418 A66 A66 is a specific and effective p110α inhibitor(IC50=32 nM).
T2433 NU 7026 NU7026 is an effective DNA-PK inhibitor (IC50: 0.23 μM, in cell-free assays), 60-fold selective for DNA-PK than PI3K and no inhibition against both ATM and ATR.
T2461 PIK-90 PIK-90, a DNA-PK and PI3K inhibitor, suppresses p110α( IC50=11 nM), p110γ(IC50=18 nM) and DNA-PK(IC50=13 nM) .
T2616 PIK-93 PIK-93 is the first potent, synthetic PI4K inhibitor with IC50 of 19 nM; inhibits PI3Kα with IC50 of 39 nM.
T2619 CH5132799 CH5132799 has been used in trials studying the treatment of Solid Tumors.
T2660 IC-87114 IC-87114 is a specific PI3Kδ inhibitor(IC50=0.5 μM).
T2661 TGX-221 TGX-221, an effective, specific, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, is utilized for cancer treatment.
T2667 PIK75 PIK-75 Hydrochloride is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM in cell-free assays.
T2672 TG100-115 TG100-115 is a PI3Kγ/δ inhibitor (IC50: 83/235 nM), with fewer effects on PI3Kα/β.
T2682 Acalisib (GS-9820) Acalisib (GS-9820) is a potent and selective inhibitor of PI3Kδ.
T2685 KU-55933 KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor.
T3153 MLN1117 MLN1117 (INK1117) is a p110α/β/γ/δ inhibitor (IC50: 15/4.5/1.9/13.39μM).
T3190 PIK-inhibitors(p110α-IN-1) PIK-inhibitors is a pan PI3K inhibitors,an analog of PI-103.
T3348 PIK-293 PIK-293 is a PI3K inhibitor, for PI3Kδ( IC50=0.24 μM), and less potent for PI3Kα/β/ γ.
T3351 CC-223 CC-223 is an orally available mTOR inhibitor with potential antitumor activity. CC-223 inhibits the activity of mTOR, which may result in the induction of tumor cell apoptosis and a decrease in tumor cell proliferation. CC-223 is a potent mTOR kinase inhibitor (IC50: 16 nM), with >150-fold sensitivi
T3410 Momordin Ic Momordin Ic might represent a potential anticancer activity, by inducing apoptosis through oxidative stress-regulated mitochondrial dysfunction involving the MAPK and PI3K-mediated iNOS and HO-1 pathways. Also, Momordin Ic accelerates gastrointestinal transit partially by stimulating synthesis of 5-
T3541 CC-115 CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM).
T3556 NIH-12848 NIH-12848 is a putative inhibitor of phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ) with an IC50 of 1 μM.
T3656 PKI-402 PKI-402 is a potent dual pan-PI3K/mTOR inhibitor targeting PI3Kα/β/γ/δ and mTOR with IC50 of 2 nM/7 nM/16 nM/14 nM and 3 nM, respectively; also potent to PI3Kα mutants E545K and H1047R.
T3692 GNE 477 GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor.
T3705 GDC-0084 GDC-0084 (RG7666) is a PI3K inhibitor with potential antineoplastic activity. GDC-0084 specifically inhibits PI3K in the PI3K/AKT kinase (or protein kinase B) signaling pathway, thereby inhibiting the activation of the PI3K signaling pathway. This may result in the inhibition of both cell growth and
T3985 GDC-0326 GDC-0326 is a potent and selective inhibitor of α-Isoform of Phosphoinositide 3-Kinase (PI3Kalpha inhibitor).
T3986 SF2523 SF2523 is a highly selective and potent inhibitor.
T4079 LY-294002 hydrochloride <p>LY294002 is a synthetic molecule inhibitor of PI3Kα/δ/β (IC50: 0.5/0.57/0.97 μM, in cell-free assays); more stable than Wortmannin in solution, and also is a blocker of autophagosome formation.</p>
T4199 Desmethyl-VS-5584 Desmethyl-VS-5584 is a dimethyl analog of VS-5584, which is a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer.
T4219 Autophinib Autophinib is a potent autophagy inhibitor with a novel chemotype with IC50 values of 90 and 40 nM for autophagy in starvation induced autophagy assay and rapamycin induced autophagy assay.
T4220 BQR-695 (Synonyms: NVP-BQR695) BQR-695 is a phosphatidylinositol 4-kinase (PI4K) inhibitor with IC50s of 80 and 3.5 nM for human PI4KIIIβ and Plasmodium variant of PI4KIIIβ, respectively.
T4296 MTX-211 MTX-211, an inhibitor of EGFR and PI3K, is used for the therapy of cancer and other diseases.
T6030 XL388 XL388 is a highly effective, specifc, ATP-competitive inhibitor of mTOR ( IC50: 9.9 nM), 1000-fold selectivity than the closely related PI3K kinases.
T6045 Torin 1 Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K.
T6072 BGT226 (NVP-BGT226) BGT226 (NVP-BGT226) is a class I PI3K/mTOR inhibitor for PI3Kα/β/γ (IC50: 4/63/38 nM) .
T6087 AZD6482 AZD 6482 is a potent and selective p110β inhibitor with IC50 of 0.69 nM and a PI3Kβ inhibitor with IC50 of 10 nM.
T6103 VS-5584 (SB2343) VS-5584 is a pan-PI3K/mTOR kinase inhibitor.
T6110 YM201636 YM201636 (IC50=33 nM), a specific PIKfyve inhibitor, is less effective to p110α and insensitive to Fabl, which is yeast orthologue.
T6143 PI-103 PI-103 is a potent and multi-targeted PI3K inhibitor.
T6168 ZSTK474 PI3K Inhibitor ZSTK474 is an orally available, s-triazine derivative, ATP-competitive phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity.
T6173 BI 2536 BI2536 is an effective Plk1 inhibitor (IC50: 0.83 nM). It has 4- and 11-fold greater selectivity than Plk2 and Plk3.
T6208 AS-252424 AS-252424 is a potent and selective inhibitor of PI3Kγ with IC50 of 33 nM; >10 fold selectivity for PI3Kγ versus PI3Kα.
T6251 PF-04691502 PF-04691502 is a potent and selective inhibitor of PI3K and mTOR kinases with antitumor activity.
T6276 NU7441 NU7441 (KU-57788) is a highly effective and specific DNA-PK inhibitor with IC50 of 14 nM. And NU7441 can inhibit PI3K with IC50 of 5 μM.
T6319 OSI-027 OSI-027 is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. Phase 1.
T6322 BAY 80-6946 Copanlisib is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. Copanlisib inhibits the activation of the PI3K signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signalin
T6394 AS-604850 AS-604850 is a specific and ATP-competitive PI3Kγ inhibitor (IC50: 250 nM), 18-fold more selective for PI3Kγ than PI3Kα, and over 80-fold selectivity for PI3Kγ than PI3Kδ/β.
T6433 CAY10505 CAY10505, a form of dehydroxyl of AS-252424, is a PI3Kγ inhibitor (IC50: 33 nM).
T6510 GDC-0349 GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.
T6557 KU-0060648 KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ with IC50 of 0.59 μM.
T6704 TG100713 TG100713 is a pan-PI3K inhibitor against PI3Kγ, PI3Kδ, PI3Kα and PI3Kβ with IC50 of 50 nM, 24 nM, 165 nM and 215 nM, respectively.
T6730 WAY-600 WAY-600 is a potent, ATP-competitive and selective inhibitor of mTOR with IC50 of 9 nM; blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) but not P-AKT(T308); selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
T6731 WYE-354 WYE-354(IC50=5 nM) is an effective, selective and ATP-competitive mTOR inhibitor. It blocks mTORC2/P-AKT(S473) and mTORC1/P-S6K(T389), not P-AKT(T308). The selectivity for mTOR is higher than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
T6732 WYE-687 WYE-687 is an ATP-competitive and selective inhibitor of mTOR with IC50 of 7 nM; blocks mTORC1/pS6K(T389) and mTORC2/P-AKT(S473) but no effect observed on P-AKT(T308). Selectivity for mTOR is greater than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
T6757 AMG319 AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2.
T6773 AZD8186 AZD8186 is an effective and specific PI3Kβ/δ inhibitor (IC50: 4/12 nM).
T6774 AZD8835 AZD8835 is a mixed inhibitor of PI3Kα/δ (IC50: 6.2/5.7 nM), also with selectivity against PI3Kβ/γ (IC50: 431/90 nM).
T6817 Deguelin Deguelin is a PI3K/AKT Inhibitor, which is a natural product isolated from plants in the Mundulea sericea family.
T6845 GNE-317 GNE-317, a PI3K/mTOR inhibitor, can pass through the blood-brain barrier (BBB).
T6850 GSK2292767 GSK2292767 is a potent and selective PI3Kδ inhibitor.
T6883 LY3023414 LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, DNA-PK, and mTOR. LY3023414 has been used in trials studying the treatment of Neoplasm, Solid Tumor, COLON CANCER, BREAST CANCER, and Advanced Cancer, among others.
T6938 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.
T6945 PIK-III PIK-III, a selective inhibitor of VPS34 enzymatic activity, inhibits autophagy and results in the stabilization of autophagy substrates.
T7014 Voxtalisib (XL765, SAR245409) Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.
T7015 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.
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