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.
-
PIK-75 hydrochloride
Catalog No. A10729 PI3K 抑制剂PIK-75是一种p110α抑制剂,IC50值为5.8nM。在p110γ和p110β的效果较差,IC50值为0.076 ?M和1.3 ?M。 了解更多 -
CUDC-907 (Fimepinostat)
Catalog No. A11153 PI3K/HDAC 抑制剂CUDC-907 (Fimepinostat)是针对PI3K和HDAC的单一小分子抑制剂,作用于PI3Kα和HDAC1/2/3/10,IC50分别为19 nM和1.7 nM/5 nM/1.8 nM/2.8 nM。 了解更多 -
BYL719 (Alpelisib)
Catalog No. A11328 PI3K 抑制剂BYL719 (Alpelisib)是一种口服生物可利用的磷脂酰肌醇3-激酶(PI3K)抑制剂,抑制 p110α/p110γ/p110δ/p110β 的 IC50 分别为 5 nM,250 nM,290 nM,1200 nM 。具有潜在的抗肿瘤活性。 了解更多 -
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