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| Catalog No. | Inhibitor Name | PI3K | p110α | p110β | p110δ | p110γ | C2α | C2β | Vps34 | Other Targets |
|---|---|---|---|---|---|---|---|---|---|---|
| A10133 | Dactolisib (BEZ235, NVP-BEZ235) | **** | ** | *** | *** | mTOR (p70S6K),ATR | ||||
| A10421 | Pictilisib (GDC-0941) | **** | ** | **** | ** | * | mTOR | |||
| A10547 | LY294002 | * | * | * | ||||||
| A10172 | Idelalisib (CAL-101, GS-1101) | * | * | **** | ** | * | DNA-PK | |||
| A11016 | Buparlisib (BKM120, NVP-BKM120) | ** | * | ** | * | * | mTOR | |||
| A10726 | PI-103 | **** | **** | **** | *** | DNA-PK,mTOR | ||||
| A10923 | TGX-221 | * | **** | ** | ||||||
| A10463 | IC-87114 | * | ** | * | ||||||
| A11161 | Wortmannin | **** | DNA-PK,ATM,MLCK | |||||||
| A10995 | XL147 analogue | *** | ** | *** | *** | |||||
| A11014 | ZSTK474 | *** | *** | *** | **** | ** | ||||
| A11328 | Alpelisib (BYL719) | **** | ||||||||
| A10088 | AS-605240 | ** | * | * | *** | |||||
| A10729 | PIK-75 HCl | *** | * | ** | DNA-PK | |||||
| A11151 | 3-Methyladenine (3-MA) | * | * | |||||||
| A11202 | A66 | *** | * | * | PI4Kβ | |||||
| A10731 | PIK-93 | *** | * | ** | *** | * | ** | * | PI4KIIIβ,DNA-PK,ATM | |
| A11035 | Omipalisib (GSK2126458, GSK458) | **** | **** | **** | **** | mTORC1,mTORC2 | ||||
| A10730 | PIK-90 | *** | * | ** | *** | |||||
| A11024 | PF-04691502 | **** | **** | **** | **** | P-Akt (S473),P-Akt (T308),mTOR | ||||
| A10112 | AZD6482 | * | *** | ** | * | DNA-PK | ||||
| A11023 | Apitolisib (GDC-0980, RG7422) | **** | *** | *** | *** | mTOR | ||||
| A10438 | GSK1059615 | **** | **** | **** | **** | mTOR | ||||
| A12422 | Duvelisib (IPI-145, INK1197) | *** | **** | **** | **** | |||||
| A11079 | Gedatolisib (PF-05212384, PKI-587) | **** | **** | mTOR | ||||||
| A10922 | TG100-115 | * | * | ** | ** | |||||
| A11099 | AS-252424 | * | *** | Casein Kinase 2 | ||||||
| A11162 | BGT226 (NVP-BGT226) | **** | ** | *** | mTOR | |||||
| A11153 | CUDC-907 | *** | ** | *** | * | HDAC1,HDAC3,HDAC10 | ||||
| A10728 | PIK-294 | * | *** | ** | ||||||
| A11197 | AS-604850 | * | ** | |||||||
| A11766 | Copanlisib (BAY 80-6946) | **** | **** | **** | *** | |||||
| A11064 | YM201636 | * | PIKfyve | |||||||
| A11169 | CH5132799 | *** | ** | * | *** | |||||
| A10727 | PIK-293 | * | * | ** | * | |||||
| A11089 | PKI-402 | **** | *** | *** | *** | mTOR | ||||
| A11956 | TG100713 | ** | ** | *** | ** | |||||
| A12480 | VS-5584 (SB2343) | **** | *** | **** | **** | mTOR | ||||
| A12831 | Taselisib (GDC 0032) | **** | *** | **** | **** | * | * | |||
| A11363 | CZC24832 | * | * | *** | ||||||
| A16332 | IPI-549 | * | * | * | *** | |||||
| A16277 | TGR-1202 | *** | ||||||||
| A16272 | GDC-0084 | **** | ** | **** | *** | mTOR | ||||
| A16352 | AZD8835 | *** | * | **** | ** | |||||
| A15868 | PIK-III | * | * | * | *** | |||||
| A15874 | VPS34-IN1 | *** | ||||||||
| A16276 | Voxtalisib (XL765, SAR245409) | *** | ** | ** | *** | DNA-PK,mTOR | ||||
| A15901 | AMG319 | * | * | *** | * | |||||
| A15759 | AZD8186 | *** | **** | *** | * | |||||
| A12889 | PF-4989216 | **** | ** | **** | ** | |||||
| A15283 | Pilaralisib (XL147) | ** | *** | *** | *** | |||||
| A14338 | PI-3065 | * | * | *** | * | |||||
| A13021 | HS-173 | **** | ||||||||
| A10766 | Quercetin | * | * | * | PKC,Src,Sirtuin | |||||
| A11784 | GSK2636771 | |||||||||
| A11196 | CAY10505 | |||||||||
| A16126 | LY3023414 | DNA-PK,mTOR kinase | ||||||||
| A13992 | GNE-317 | |||||||||
| A14441 | Acalisib (GS-9820) | |||||||||
| A16273 | NVP-QAV-572 | |||||||||
| A16266 | ON 146040 | *** | *** | |||||||
| A15992 | PQR309 | |||||||||
| A15529 | MLN1117 (Serabelisib) | *** | ||||||||
| A15030 | CAL-130 | |||||||||
| A14379 | Panulisib (P7170, AK151761) | ALK1, mTOR, DNA-PK | ||||||||
| A13879 | CNX-1351 | **** | ||||||||
| A11198 | D-106669 | **** | ||||||||
| A11261 | PX-866 (Sonolisib) | **** | * | **** | *** | |||||
| A11511 | NVP-BAG956 | *** | * | *** | ** | PDK1 | ||||
| A12935 | PF-04979064 | **** | **** | **** | **** | mTOR | ||||
| A13328 | ETP-46464 | * | mTOR, DNA-PK, ATR, ATM | |||||||
| A14432 | GNE-493 | **** | *** | *** | *** | mTOR |
Notes:
1.Hover mouse over "" to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of "" is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
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LY294002
Catalog No. A10547 PI3K InhibitorLY294002 is a PI3k inhibitor (cell IC50 about 10 μM) and a casein kinase II inhibitor. Learn More -
BEZ235 (NVP-BEZ235, Dactolisib)
Catalog No. A10133 PI3K/mTOR InhibitorBEZ235 (NVP-BEZ235) inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes. Learn More -
BKM120 (NVP-BKM120, Buparlisib)
Catalog No. A11016 PI3K InhibitorBKM120 (NVP-BKM120) is a bioavailable specific oral pan-class I phosphatidylinositol 3-kinase (PI3K) kinase inhibitor. Learn More -
GDC-0941 (Pictilisib)
Catalog No. A10421 PI3K inhibitorGDC-0941 is a potent, selective, orally bioavailable inhibitor of class I PI3 kinase (PI3K) , with IC50 values (nM) of 3, 33, 3, 75, 1230 and 580 for p110 α, β, δ and γ isoforms, DNA-PK and mTOR respectively. Learn More -
ZSTK474
Catalog No. A11014 PI3K inhibitorZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol 3 kinase isoforms. Learn More -
PI-103
Catalog No. A10726 PI3K InhibitorPI-103 is a potent, cell-permeable, ATP-competitive inhibitor of phosphatidylinositol 3-kinase (PI3K) family members with selectivity toward DNA-PK, PI3K (p110α), and mTOR. Learn More -
XL147 analogue
Catalog No. A10995 PI3K InhibitorXL147 is a potent, selective and orally bioavailable small molecule inhibitor of class I phosphatidylinositol 3 kinase (PI3K) with potential antineoplastic activity. Learn More -
CAL-101 (GS-1101, Idelalisib)
Catalog No. A10172 PI3K inhibitorCAL-101 is an isoform-selective inhibitor of PI3K that induces apoptosis of chronic lymphocytic leukemia (CLL) cells. Learn More -
GSK1059615
Catalog No. A10438 mTOR/PI3K InhibitorGSK1059615 is a potent, reversible, ATP-competitive, thiazolidinedione inhibitor of PI3Kα (IC50 = 2 nM). Learn More -
TGX-221
Catalog No. A10923 PI3K InhibitorTGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β. Learn More -
PIK-93
Catalog No. A10731 PI3K inhibitorPIK 93 selectively inhibits the type III PI 4-kinase enzyme, and small interfering RNA-mediated down-regulation of the individual PI 4-kinase enzymes. Learn More -
YM201636
Catalog No. A11064 PI3K InhibitorYM201636 is a cell-permeable and selective inhibitor of PIKfyve (IC50 = 33 nM). Learn More -
NU-7441 (KU-57788)
Catalog No. A11098 DNA-PK inhibitorNU-7441 (KU-57788) is a potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor. The IC50 values are 14, 1700, 5000, >100000 and >100000 nM for DNA-PK, mTOR, PI 3-K, ATM and ATR respectively. Learn More -
CUDC-907 (Fimepinostat)
Catalog No. A11153 PI3K/HDAC inhibitorCUDC-907 (Fimepinostat) is a single small molecule inhibitor that targets both PI3K and HDAC. CUDC-907 is more efficacious than either a single PI3K or HDAC inhibitor reference compound or a combination of the two single agents at maximally tolerated doses. Learn More -
Wortmannin
Catalog No. A11161 PI3K inhibitorWortmannin is a potent, selective, cell-permeable and irreversible inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase) (IC50 = 2 - 4 nM) which also potently inhibits polo-like kinase 1 (PLK1) (IC50 = 5.8 nM).
Learn More -
PP121
Catalog No. A11207 PI3K InhibitorPP121 is a dual inhibitor of receptor tyrosine kinases (RTKs) (IC50 < 0.02 μM for Abl, Src, VEGFR-2 and PDGFR) and PI 3-K family kinases (IC50 < 0.06 μM for p110α, DNA-PK and mTOR). Learn More -
PIK-75 hydrochloride
Catalog No. A10729 PI3K InhibitorPIK-75 is an imidazopyridine that selectively inhibits p110α with an IC50 value of 5.8 nM.2 It inhibits p110γ and p110β considerably less effectively with IC50 values of 0.076 µM and 1.3 µM, respectively. Learn More -
BYL719 (Alpelisib)
Catalog No. A11328 PI3K InhibitorBLY719 is an orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. Learn More -
BAY 80-6946 (Copanlisib)
Catalog No. A11766 PI3K inhibitorBAY 80-6946 is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. Learn More -
GSK2636771
Catalog No. A11784 PI3K InhibitorGSK2636771 is a potent, orally bioavailable, PI3K beta-selective inhibitor. Learn More -
CZC24832
Catalog No. A11363 PI3K inhibitorCZC24832 is a selective inhibitor of PI 3-Kinase γ (IC50 = 1.0 μM in a PI 3-Kγ-dependent fMLP-induced neutrophil migration assay). Learn More -
VS-5584
Catalog No. A12480 PI3K/mTOR inhibitorVS-5584 is a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. Learn More -
HS-173
Catalog No. A13021 PI3K InhibitorHS-173, a novel phosphatidylinositol 3-kinase (PI3K) inhibitor, has anti-tumor activity through promoting apoptosis and inhibiting angiogenesis. Learn More -
PI-3065
Catalog No. A14338 p110δ inhibitorPI-3065 is a small molecule and selective inhibitor of p110δ kinase with an Ki value of 1.5nM and IC50 value of 5nM Learn More -
Panulisib (P7170, AK151761)
Catalog No. A14379 PI3K inhibitorPanulisib is a potent and selective imidazoquinoline based PI3K inhibitor with potential anticancer activity. Learn More -
AZD8186
Catalog No. A14164 PI3K inhibitorAZD8186 is and inhibitor of the beta isoform of phosphoinositide-3 kinase (PI3K), with potential antineoplastic activity. Learn More -
CAL-130
Catalog No. A15030 PI3K inhibitorCAL-130 is a novel phosphoinositide 3-kinase (PI3K) inhibitor. It is reported that combined inhibition of PI3Kδ/γ as therapy for T cell acute lymphoblastic leukemia (T-ALL). Learn More -
CAL-130 Hydrochloride
Catalog No. A15031 PI3K inhibitorCAL-130 Hydrochloride is a novel phosphoinositide 3-kinase (PI3K) inhibitor. It is reported that combined inhibition of PI3Kδ/γ as therapy for T cell acute lymphoblastic leukemia (T-ALL). Learn More -
LY 303511
Catalog No. A15147 PI3K inhibitorLY303511, an inactive analogue of LY294002, is a mTOR inhibitor that did not inhibit PI3-K. Learn More -
NVP-BKM120 Hydrochloride
Catalog No. A15195 PI3K InhibitorNVP-BKM120 Hydrochloride is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. Reduced potency against VPS34, mTOR, DNA-PK, with little activity to PI4Kβ. Learn More -
PI-103 Hydrochloride
Catalog No. A15212 PI3K InhibitorPI103 is a potent inhibitor with low IC50 values against recombinant PI3K isoforms p110alpha (IC50= 2 nM), p110beta (IC50= 3 nM), p110delta (IC50= 3 nM), and p110gamma (IC50= 15 nM), less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. Learn More -
XL-147 (Pilaralisib)
Catalog No. A15283 PI3K InhibitorXL147 is a potent, orally bioavailable inhibitor of the class I PI3K family of lipid kinases. Learn More -
AZD8186
Catalog No. A15759 PI3K inhibitorAZD8186 is an isoform-specific small-molecule PI3K inhibitor, potently inhibits PI3Kβ (IC50=4 nM) and PI3Kδ (IC50=12 nM) with selectivity over PI3Kα (IC50=35 nM) and PI3Kγ (IC50=675 nM). Learn More -
Acalisib (GS-9820)
Catalog No. A14441 PI3Kδ InhibitorAcalisib is an inhibitor of the beta and delta isoforms of the 110 kDa catalytic subunit of class IA phosphoinositide-3 kinases (PI3K) with potential immunomodulating and antineoplastic activities. Learn More -
AMG319
Catalog No. A15901 PI3Kδ inhibitorAMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2. Learn More -
PF-4989216
Catalog No. A12889 PI3K inhibitorPF-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. Learn More -
PQR309 (Bimiralisib)
Catalog No. A15992 PI3K inhibitorPQR309 is an orally bioavailable pan inhibitor of phosphoinositide-3-kinases (PI3K) and inhibitor of the mammalian target of rapamycin (mTOR), with potential antineoplastic activity. Learn More -
GNE-317
Catalog No. A13992 PI3K inhibitorGNE-317 is a potent PI3K inhibitor that can cross the Blood brain barrier; shows potent suppression of the PI3K pathway in the brain of mice with intact BBB. Learn More -
LY3023414
Catalog No. A16126 PI3K/mTOR Dual InhibitorLY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK, extracted from patent WO/2012097039A1, compound example 1, has an IC50 of 64.9 nM, 42.1 nM, 10.6 nM, 19.1 nM for Akt1(pT308), Akt1 (pS473), P70S6(pT389), S6RP(pS240/242). Learn More -
ON 146040
Catalog No. A16266 dual PI3K and BCR-ABL inhibitorON 146040 is the first dual PI3K and BCR-ABL inhibitor that targets the STAT3 and STAT5 pathways; inhibits PI3K α/δ isoforms with IC50 of 14/20 nM. Learn More -
PI4KIIIbeta-IN-10
Catalog No. A16269 PI4KIIIβ inhibitorPI4KIIIbeta-IN-10 is the most potent PI4KIIIbeta inhibitor currently reported, with very minor off-target inhibition of PI4KIIIbeta related lipid kinases (IC50 = 3.6 nM). Learn More -
PI4KIIIbeta-IN-9
Catalog No. A16270 PI4KIIIβ inhibitorPI4KIIIbeta-IN-9 is a potent PI4KIIIbeta inhibitor (IC50 of 7 nM) and is >140-fold selective over PI3Kgamma and >20-fold selective over PI3Kδ, and shows no inhibition of vps34 at concentrations up to 20 uM. Learn More -
ETP-46321
Catalog No. A16271 PI3K α/δ inhibitorETP-46321 is a potent and orally bioavailable PI3K α/δ inhibitor with potent biochemical and cellular activity and good pharmacokinetic properties (PK) after oral dosing. Learn More -
NVP-QAV-572
Catalog No. A16273 PI3K inhibitorNVP-QAV-572 is a potent PI3K kianse inhibitor with IC50 of 10 nM. Learn More -
PI3K-alpha inhibitor 1
Catalog No. A16274 PI3Kα inhibitorPI3Kα inhibitor 1 is a PI3Kα inhibitor extracted from patent US/20120088764A1, compound 243, has an IC50 < 0.1 uM, PI3Kα inhibitor 1 also inhibits HDAC (0.1 uM ≤ IC50 ≤ 1 uM) . Learn More -
PI3K-gamma inhibitor 1
Catalog No. A16275 -
SAR245409 (XL765, Voxtalisib)
Catalog No. A16276 PI3K/mTOR dual inhibitorSAR245409 is a PI3K/mTOR dual kinase inhibitor XL765 is an orally bioavailable small molecule targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) kinases in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. Learn More -
TGR-1202 (Umbralisib)
Catalog No. A16277 PI3Kδ inhibitorTGR-1202 is an orally available, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 and 24.3 nM respectively. Learn More -
TGR-1202 hydrochloride (Umbralisib HCl)
Catalog No. A16278 PI3Kδ inhibitorTGR-1202 hydrochloride is an orally available, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 and 24.3 nM respectively. Learn More -
AZD8835
Catalog No. A16352 PI3Kα/PI3Kδ inhibitorAZD8835 is a potent and selective inhibitor of PI3Kα and PI3Kδ with IC50 of 5.7 nM and 6.2 nM, with selectivity against PI3Kβ (IC50 431 nM) and PI3Kγ (IC50 90 nM). Learn More
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