PI3K | 陶素生化

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
T1056	Isoprenaline hydrochloride	Isoproterenol is a potent beta-adrenergic agonist with the peripheral vasodilator, bronchodilator, and cardiac stimulating properties.
T1826	Voxtalisib Analogue	Voxtalisib (SAR245409, XL765)Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ ,also inhibits DNA-PK and mTOR.
T1827	Buparlisib	Buparlisib is an orally bioavailable specific oral inhibitor of the pan-class I PI3K (IC50s: 52/166/116/nM for p110α, p110β, and p110δ).
T1838	INK 128	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	AZD8055	AZD8055 is an ATP-competitive mTOR inhibitor (IC50: 0.8 nM in MDA-MB-468 cells). It is ~1,000-fold selective for mTOR over all PI3K isoforms.
T1861	Omipalisib	GSK2126458 is a small-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic activity.
T1879	3-Methyladenine	3-Methyladenine (3-MA) is a selective PI3KV inhibitor, and the IC50s against ps34 and PI3Kγ were 25/60 μM in HeLa cells, respectively.
T1894	Idelalisib	Idelalisib is a small molecule inhibitor of the PI3K catalytic subunit p110δ (IC50: 2.5 nM). The selectivity for p110δ is 40- to 300-fold than p110α/β/γ.
T1916	Apitolisib	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
T1921	Alpelisib	Alpelisib is an orally bioavailable PI3Kα inhibitor (IC50: 5 nM in a cell-free assay) with potential antineoplastic activity and minimal effect on PI3Kβ/γ/δ.
T1949	CZC24832	CZC24832 is a selective inhibitor of PI 3-kinase γ.
T1961	Vistusertib	AZD2014 is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity.
T1970	Gedatolisib	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	Duvelisib	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 immunom
T1994	Pictilisib	Pictilisib (GDC-0941) is a potent pan inhibitor of class I catalytic subunits of PI3K (IC50s: 3/33/3/75 nM for p110α/β/δ/γ).
T1999	Taselisib	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 an inhibitor of PI3K (IC50s: 0.5/0.57/0.97 μM for PI3Kα/δ/β in cell-free assays). It 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(
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 neopl
T2084	ETP46464	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	Dactolisib	Dactolisib is an orally bioavailable inhibitor of PI3K and mTOR (IC50s: 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR).
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 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 IC
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	GSK-1059615	GSK1059615 has been used in trials studying the treatment of Lymphoma, Solid Tumours, Endometrial Cancer, Solid Tumor Cancer, and Metastatic Breast Cancer.
T2365	Pilaralisib	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 treat
T2377	XL147 analogue	XL147 analogue is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ.
T2414	Torkinib	Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor (IC50: 8 nM). It also inhibits mTORC1/2 (IC50s: 30/58 nM).
T2418	A66	A66 is a specific and effective p110α inhibitor(IC50=32 nM).
T2433	NU7026	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, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110α(IC50=5.8 nM) and p110γ(IC50=76 nM).
T2672	TG100-115	TG100-115 is a PI3Kγ/δ inhibitor (IC50: 83/235 nM), with fewer effects on PI3Kα/β.
T2682	Acalisib	Acalisib (GS-9820) is a potent and selective inhibitor of PI3Kδ.
T2685	KU55933	KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor.
T3153	Serabelisib	MLN1117 (INK1117) is a p110α/β/γ/δ inhibitor (IC50: 15/4.5/1.9/13.39μM).
T3190	PIK-inhibitors	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
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
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.
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, th
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.
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 autopha
T4220	BQR-695	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	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	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, cell-permeable, ATP-competitive inhibitor of PI3K family members (IC50s: 2/3/3/15/30/23 nM for p110α/β/δ/γ, mTOR, and DNA-PK).
T6168	ZSTK474	PI3K Inhibitor ZSTK474 is an orally available, s-triazine derivative, ATP-competitive phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity.
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.
T6322	Copanlisib	Copanlisib is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. Copanlisib inhibits the activation of the PI3K signaling pathway, which may resul
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.
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
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
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).
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, CO
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	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.
T2P2919	(4S)-4-Hydroxy-L-isoleucine	4-Hydroxyisoleucine (HIL) from fenugreek (Trigonella foenum-graecum) seeds is a potential insulinotropic (anti-diabetic) and anti-obesity amino acid. HIL stimulates glucose-depende
T5S0896	Loureirin A	Loureirin A has an inhibitory effect on platelet activation, perhaps through an impairment of PI3K/Akt signaling.Loureirin A negatively affects agonist-induced platelet aggregation
T4976	TGR-1202	TGR-1202 is a PI3Kδ inhibitor.
T4958	Alkannin	Shikonin is a natural red naphthoquinone pigment, has antimicrobial, anti-tumor, and anti-inflammatory effects; a purified shikonin preparation is widely used for the production of
T6283	Wortmannin	Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-P
T5166	Leniolisib	Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor (IC50: 11 nM).
T5432	IPI-549	IPI-549 is an inhibitor of PI3Kγ (IC50 = 16, 3,200, 3,500, and >8,400 nM for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively)
T5736	CYNARIN	CYNARIN is a natural product. It shows antioxidant and choleretic properties and is a potential immunosuppressive agent.
T5831	Selective PI3Kδ Inhibitor 1	Selective PI3Kδ Inhibitor 1 is a PI3Kδ Inhibitor(IC50 = 0.9 nM).
T6330	PI3Kδ-IN-2	PI3Kδ-IN-2 is a potent and selective inhibitor of PI3Kδ
T6799	IITZ-01	IITZ-01 is potent autophagy inhibitor with single-agent anticancer activity ( IC50 of 2.62 μM for PI3Kγ.)
T7166	GNE-493	GNE-493 is potent, selective, and orally available PI3K and mTOR inhibitor with potential anticancer activity.IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3
T7343	PF-04979064	PF-04979064 is a potent and selective PI3K and mTOR dual kinase inhibitor(Ki of 0.13 nM and 1.42 nM,respectively).