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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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TGR-1202 hydrochloride
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 -
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 -
GDC-0084
Catalog No. A16272 PI3K inhibitorGDC-0084 is a phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. 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
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 -
PQR309
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 -
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 p110??, p110??, p110??, p110??, and VPS34, respectively. 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 -
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 -
TG 100713
Catalog No. A11956 PI3K inhibitorTG 100713 is an inhibitor of PI3-kinase that inhibits endothelial cell proliferation. 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 -
IPI-145 (Duvelisib, INK1197)
Catalog No. A12422 PI3K-δ/PI3K-γ inhibitorIPI-145, also known as INK-1197, 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. Learn More -
SF1126
Catalog No. A12704 Pan PI3K inhibitorSF1126 is a water soluble, small-molecule prodrug containing the pan-PI3K/mTOR inhibitor LY294002/SF1101 conjugated to the RGD-containing tetra-peptide SF1174 with potential antineoplastic and antiangiogenic activities. Learn More -
GDC-0032 (Taselisib)
Catalog No. A12831 PI3K inhibitorGDC-0032 is a potent, next-generation PI3 inhibitor targeting PI3 alpha. Learn More -
ETP-46464
Catalog No. A13328 ATR inhibitorETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM. Learn More -
PF-04979064
Catalog No. A12935 PI3K/mTOR Dual InhibitorPF-04979064 is a highly potent and orally bioavailable PI3K/mTOR dual inhibitor. Learn More -
NVP-BAG956
Catalog No. A11511 PI3K/PDK-1 InhibitorNVP-BAG956 acts as a potent, reversible, and ATP-competitive PI 3-K/PDK1 dual kinase inhibitor, displaying much reduced potency against VEGFR1 (IC50 = 2.56 uM) and little or no activity toward a panel of 15 other kinases (IC50 >10 uM). Learn More -
GSK2636771
Catalog No. A11784 PI3K InhibitorGSK2636771 is a potent, orally bioavailable, PI3K beta-selective inhibitor. 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 -
BYL719 (Alpelisib)
Catalog No. A11328 PI3K InhibitorBLY719 is an orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. Learn More -
PX-866 (Sonolisib)
Catalog No. A11261 PI3K inhibitorPX-866 is a small-molecule wortmannin analogue inhibitor of the alpha, gamma, and delta isoforms of phosphoinositide 3-kinase (PI3K) with potential antineoplastic activity. Learn More -
PIK-90
Catalog No. A10730 PI3K InhibitorPIK-90 is a synthetic phosphoinositide 3-kinase (PI3K) inhibitor with IC50 values (nM) of 11, 350, 18, and 58 for p110 α, β, γ and δ isoforms, low mTOR activity. Learn More -
PIK-75
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 -
A66
Catalog No. A11202 PI3K inhibitorThe S-enantiomer of A66 is a potent inhibitor of the p110alpha isoform of PI 3-kinase (PIK3CA). Learn More -
D-106669
Catalog No. A11198 PI3K InhibitorD-106669 is a highly potent and selective PI3K inhibitor, (PI3Kα IC50 <10 nM, >3 log selectivity against tyrosine or serine/threonine kinases, except ERK1 and 2).
Learn More -
GNE 477
Catalog No. A14114 PI3K/mTOR inhibitorGNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Kiapp is 21 nM for mTOR. Learn More -
Vps34-IN-2
Catalog No. A16933 Vps34 inhibitorVps34-IN-2 is a novel, potent and selective inhibitor of Vps34 with IC50s of 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively. Learn More -
leniolisib (CDZ 173)
Catalog No. A16796 PI3K inhibitorLeniolisib(CDZ 173) is a potent PI3Kδ selective inhibitor with biochemical IC50 values of 0.244, 0.424, 2.23 and 0.011 μM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. Learn More -
Seletalisib (UCB-5857)
Catalog No. A16797 PI3K inhibitorSeletalisib is a novel small-molecule inhibitor of PI3Kδ with an IC50 value of 12 nM and shows significant selectivity to PI3Kδ with respect to the other class I PI3K isoforms (between 24- and 303-fold). Learn More -
Tenalisib (RP6530)
Catalog No. A16799 dual PI3Kδ/γ inhibitorTenalisib, also known as RP6530, is a potent and selective dual PI3Kδ/γ inhibitor that inhibited growth of B-cell lymphoma cell lines with a concomitant reduction in the downstream biomarker, pAKT. Learn More
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