PI3K
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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AZD6482
Catalog No. A10112 -
AS-605240
Catalog No. A10088 -
TG100-115
Catalog No. A10922 -
GDC-0980 (Apitolisib, RG7422)
Catalog No. A11023 mTOR/PI3K 抑制剂GDC-0980 (Apitolisib,RG7422)是一种有效的,I型PI3激酶和mTOR激酶抑制剂(TORC1/2),对于p110α,β,δ和γ的体外IC50为5、27、7和14 nM。 了解更多 -
PF-04691502
Catalog No. A11024 PI3K/mTOR 抑制剂PF-04691502是PI3K/mTOR激酶抑制剂,也是在PI3K/mTOR信号传导途径中靶向磷脂酰肌醇3激酶(PI3K)和雷帕霉素(mTOR)哺乳动物靶标的药物。 了解更多 -
GSK2126458 (Omipalisib)
Catalog No. A11035 mTOR/PI3K 抑制剂,GSK2126458 (Omipalisib)是一种高选择性的,有效的p110α/β/γ/δ和 mTORC1/2抑制剂,无细胞试验中Ki分别为0.019 nM/0.13 nM/0.024 nM/0.06 nM和0.18 nM/0.3 nM。 了解更多 -
XL765
Catalog No. A10997 -
PKI-587 ( Gedatolisib )
Catalog No. A11079 PI3K/mTOR 抑制剂PKI-587 (Gedatolisib)是一种高效的PI3K/mTOR激酶抑制剂,可抑制PI3K-α,β,γ,δ亚型和mTOR,IC50分别为0.4、6.0、5.4、6.0和1.6 nM。 了解更多 -
3-Methyladenine
Catalog No. A11151 -
PIK-294
Catalog No. A10728 -
Quercetin (Sophoretin)
Catalog No. A10766 MAO-B 抑制剂Quercetin (Sophoretin)抑制许多酶系统,包括酪氨酸蛋白激酶,磷脂酶A2,磷酸二酯酶,线粒体ATPase,PI 3-激酶和蛋白激酶C。 了解更多 -
Quercetin dihydrate (Sophoretin)
Catalog No. A10765 MAO-B 抑制剂Quercetin dihydrate (Sophoretin)抑制许多酶系统,包括酪氨酸蛋白激酶,磷脂酶A2,磷酸二酯酶,线粒体ATPase,PI 3-激酶和蛋白激酶C。 了解更多 -
NVP-BGT226
Catalog No. A11162 PI3K 抑制剂NVP-BGT226,新型磷酸肌醇3-激酶/mTOR双重抑制剂,作用于PI3Kα/β/γ,IC50为4 nM/63 nM/38 nM,在体外和体内对人的头颈癌细胞均显示出强大的生长抑制活性。 了解更多 -
PX-866 (Sonolisib)
Catalog No. A11261 -
NVP-BAG956
Catalog No. A11511 PI3K/PDK-1 抑制剂NVP-BAG956是一种强效、可逆和ATP竞争性PI3-K/PDK1双激酶抑制剂,对VEGFR 1(IC50 = 2.56 μM)的效力大大降低,对其他15种激酶(IC50 > 10 uM)的活性很小或没有活性。 了解更多 -
IPI-145 (Duvelisib, INK1197)
Catalog No. A12422 PI3K-δ/PI3K-γ 抑制剂IPI-145 (Duvelisib,INK1197)是磷酸肌醇-3激酶(PI3K)δ和γ亚型的生物可利用、高选择性和有效的小分子抑制剂,具有潜在的免疫调节和抗肿瘤活性。 了解更多 -
GDC-0032 (Taselisib)
Catalog No. A12831 -
ETP-46464
Catalog No. A13328 -
PF-04979064
Catalog No. A12935 -
GNE 477
Catalog No. A14114 -
PI3k-delta inhibitor 1
Catalog No. A14109 -
Miltefosine
Catalog No. A14138 -
GNE-493
Catalog No. A14432 -
PI4KIII beta inhibitor 3
Catalog No. A15430 -
VPS34-IN1
Catalog No. A15874 -
MLN1117 (Serabelisib)
Catalog No. A15529 p110α 抑制剂MLN1117,也称为INK1117和TAK-117,是具有潜在抗肿瘤活性的I类磷酸肌醇3激酶(PI3K)α同工型的生物利用抑制剂。 了解更多 -
Desmethyl-VS-5584
Catalog No. A10900 -
Tenalisib (RP6530)
Catalog No. A16799 dual PI3Kδ/γ 抑制剂Tenalisib (RP6530)是一种有效且选择性的双重PI3Kδ/PI3Kγ抑制剂,能抑制B细胞淋巴瘤细胞系的生长,同时降低下游生物标记物pAKT。 了解更多 -
Seletalisib (UCB-5857)
Catalog No. A16797 PI3K 抑制剂Seletalisib (UCB-5857)是一种新型的PI3Kδ小分子抑制剂,其IC50值为12 nM,相对于其他I类PI3K亚型(介于24-303倍之间),对PI3Kδ具有显著的选择性。 了解更多 -
leniolisib (CDZ 173)
Catalog No. A16796 PI3K 抑制剂Leniolisib (CDZ 173)是一种有效的、选择性的PI3Kδ抑制剂,对PI3Kα、PI3Kβ、PI3Kγ和PI3Kδ的生化IC50值分别为0.244、0.424、2.23和0.011 uM。 了解更多 -
Vps34-IN-2
Catalog No. A16933 Vps34 抑制剂Vps34-IN-2是一种新颖,有效和选择性的Vps34抑制剂,在Vps34酶促测定和GFP-FYVE细胞测定中的IC50分别为2和82 nM。 了解更多 -
SAR260301
Catalog No. A16877 -
Pictilisib dimethanesulfonate
Catalog No. A11444 PI3Kα/δ inhibitorPictilisib dimethanesulfonate (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). 了解更多 -
Dactolisib Tosylate
Catalog No. A11327 dual PI3K and mTOR kinase inhibitorDactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2. 了解更多